Journal of Biomedical and Pharmaceutical Research, Apr 29, 2013
Aliterature review studies of physicochemical properties and reactivity of naphthyridine derivati... more Aliterature review studies of physicochemical properties and reactivity of naphthyridine derivatives due to their broad spectrum activity. The research work still looking for the promising compound of these derivatives and also the aim of our studies to activate this area of research and propose these derivatives as a target compounds that could be oriented as pharmaceutical compounds in medicine.
Journal of Pharmaceutical and Scientific Innovation, Feb 19, 2014
Keeping in view of the biological potential of Schiff bases attached to heterocyclic ring system;... more Keeping in view of the biological potential of Schiff bases attached to heterocyclic ring system; a series of novel Schiff's base derivatives were synthesized 1-8 successfully in appreciable yields. The structures of all the synthesized derivatives were confirmed by physical and spectral analysis. Furthermore, all synthesized compounds were evaluated for antifungal activity against different strains of fungal organisms. Some of the compounds exhibited appreciable antifungal activity comparing to the reference compound (Nystatine).
Synthesis of some new 1,8-naphthyridines (out of which four are new) derivatives were described. ... more Synthesis of some new 1,8-naphthyridines (out of which four are new) derivatives were described. The synthesized compounds were prepared by the condensation of 2,6-diaminopyridine and 1,3-dicarbonyl compounds with various chemical reagents. However, there are significant effects on yields and isomer ratios depending on the use of perchloric or phosphoric acids in the condensation reaction. Based on the isomer ratios, some probable reaction mechanisms are proposed. The purity of the new synthesized compounds were checked by performing TLC using appropriate solvent and the spots were visualized in the UV light. The chemical structure of the compounds were confirmed by FT-IR, 1 H, 13 C-NMR spectroscopy.
We have tried to assess the acetylation process in tuberculosis a sample of Libyan patient, Simul... more We have tried to assess the acetylation process in tuberculosis a sample of Libyan patient, Simultaneous measurement of isoniazid (INH) and its main acetylated metabolite acetylisoniazid (AcINH) in plasma is realized by high-performance liquid chromatography (HPLC). INH and its main metabolite in human plasma were measured after taken single oral dose (200-300 mg), after 3 hours the samples of patient´s venous blood (4 ml) were collected into heparinized tubes and immediately centrifuged. The plasma samples were then deproteinized by trichloroacetic acid. The analytes separated by HPLC on pinnacle II C18 column (water). Nicotinamide is used as internal standard. The mobile phase is 0.05 M ammonium acetate buffer (pH 6) acetonitrile (99:1, v/v). The detection is by ultraviolet absorbance at 275 nm. Retention time recorded for INH, AcINH and the internal standard were 7.3, 9.9 and 14.2 min respectively. The result obtained showed that the plasma concentration of INH to 48% patient sho...
Biomedical Journal of Scientific & Technical Research, 2020
There are several ways by which organic compounds can interact with Deoxyribonucleic Acid (DNA), ... more There are several ways by which organic compounds can interact with Deoxyribonucleic Acid (DNA), including covalent bonding, electrostatic binding or intercalation. Intercalation occurs when the compound (ligand) of appropriate size and chemical nature fit between base pairs of DNAs [1,2]. In order for an intercalator to fit between base pairs, they must consist of planar polycyclic aromatic rings, and the DNA must dynamically open a space between its base pairs by unwinding [3]. The ability of intercalating agents to inhibit DNA replication and nucleic acid synthesis in vivo leads to their extensive use as mutagens, antibiotics, antibacterials, trypanocides, schistosomicides, and antitumor agents. The intercalative binding is non-covalent stacking interaction resulting from the insertion of a planar aromatic ring(s) between the base pairs of the DNA double helix [4,5]. Many classes of organic compounds have been reported to possess good DNA intercalating activity. Among these agents, Schiff's bases (imines) showed a large range of biological activities including antiviral, antibacterial, antiproliferative, antifungal, and antimalarial activities [6-8].
The 2019 coronavirus (COVID-19) pandemic is spreading worldwide, with a spectacular increase in d... more The 2019 coronavirus (COVID-19) pandemic is spreading worldwide, with a spectacular increase in death missing any effective therapeutic treatment up to now. Molecular docking is a recognized computational tool to assist in early drug discovery and development. Molecular docking analysis was carried out using 2-(4-(aminomethyl)phenyl)isoindoline-1,3-dione Schiff base conjugates with SARS-CoV-2 protease enzyme and COVID-19 main protease in apo form (6M03). The compounds with the best normalized docking scores to protease enzyme (6LU7) were ARG3 (-8.1 kcal/mole), ARG7 (-8.1 kcal/mole) and ARG6 (-8.0 kcal/mole). The best docking ligands for main protease in apo form (6M03) were ARG7 (-8.7 kcal/mole), ARG6 (-8.6 kcal/mole) and ARG3 (-8.4 kcal/mole). The structural similarity between these conjugates inspired us to perform in silico studies to check their possible binding interactions with essential SARS-CoV-2 proteins. These studies provide insight into the potential binding between Schi...
A series of new Schiff's bases of Sulfanilamide 1a-8a were synthesized by condensation of sul... more A series of new Schiff's bases of Sulfanilamide 1a-8a were synthesized by condensation of sulfanilamide with different substituted aromatic aldehydes. The structures of these products were confirmed by physical and spectral analysis. Antibacterial and antifungal activity of the synthesized derivatives 1a-8a were done in comparison with Ciprofloxacin and Ketoconazole as standard compounds. All the 3 selected strains of bacteria and fungi namely S. Aureus, E. Coli and C. Albicans. Compounds 5a, 7a showed very good activity against C .Albicans while compounds 2a, 8a showed moderate activity when compared with standard drug Ketoconazole.
Most all tricyclic compounds derived from theophylline were investigated in the respect of their ... more Most all tricyclic compounds derived from theophylline were investigated in the respect of their anticancer, circulatory blood system activity and as anti-inflammatory agents. The synthesis of new tricyclic purine derivatives with anellated in 7,8-position of theophylline five, six, seven membered heterocyclic ring system. of lactam and non-lactam structure modified by a basic substituent at N8, N9 and N10 position. It has been shown that new tricyclic theophylline derivatives possess sedative, analgesic properties, neurolleptic-like activity and hypothermizing properties. Some structural elements modification influence the central nervous system activity in the respect of:-Kind of the additional ring.-Alkylamine substituent in 9 position of tricyclic system. Our goal was to give a wide scope literature review of the tricyclic and tetracyclic theophylline derivatives as adenosine, 5-HT, benzodiazpine receptors, and phosphodiaesterase inhibitors, because the new compounds are of inte...
drugs (NSAIDs) are widely used for reducing pain and swellings associated with inflammation and r... more drugs (NSAIDs) are widely used for reducing pain and swellings associated with inflammation and represent an area in continuous and ever growing development. To control pain due
There are many activities performed in a repeated way and in a risk positions that cause fatigue ... more There are many activities performed in a repeated way and in a risk positions that cause fatigue and subsequently may origin musculoskeletal disorders (MSD). Although the disorders may appear as a consequence of an intense effort...
A series of N-substituted benzimidazole derivatives (1-5) was synthesized. Benzimidazole nucleus ... more A series of N-substituted benzimidazole derivatives (1-5) was synthesized. Benzimidazole nucleus was acylated in 1-position with benzoyl chloride in basic medium at room temperature to form N-acylated benzimidazole (1). Reaction of the Nacylated benzimidazole (1) with different amines yields the desired N-substituted benzimidazole derivatives (2-5). All the synthesized compounds (1-5) were evaluated in vivo for analgesic activity by acetic acid induced writhing and hot plate tests in mice. In comparison to the standard drug aspirin at the same dose (50mg/kg), compound 4 was the most potent as it decreased the number of writings to 17% comparing to control. However, aspirin resulted in a decrease equal to 12% of the control. In addition, all the test compounds except 5 produced some reduction in reaction time for hot plate test. Markedly, the effect was statistically significant with compounds 3 and 4.
In the present study a new ester–ether phenol derivatives 2-5 have been synthesized and character... more In the present study a new ester–ether phenol derivatives 2-5 have been synthesized and characterized. Their structures have been established on the physical and spectral analysis. The synthetic compounds were screened in vitro for their antimicrobial activity against: Metacillin resistance staphylococcus aureus, Escherichia coli ATCC 11934, Extended spectrum B-lactamase (12,54,70), staphylococcus aureus, Bacillus subtales and Candida albicans (669,1047, 772, 1057, 660). The best result obtained at the concentration 100μg with compound phenyl benzoate 2 and 1Nitro-4(phenoxymethyl)benzene 5 against fungus (Candida albicans 660, 1047, 1057 ). While Compound 5 possess significant active against gram positive and gram negative bacteria comparable to that of the standard drugs.
The present study was aimed to study the analgesic and antiepileptic potency of some New succinim... more The present study was aimed to study the analgesic and antiepileptic potency of some New succinimide derivatives. Various aromatic amines clubbed succinimide derivative compounds 2-13 were synthesized by using succinic anhydride and various amines in reflux synthesizer. The structures of the synthesized derivatives were confirmed by means of physical and spectral analysis. All the synthesized compounds were evaluated in vivo for analgesic and antiepileptic activities by using standard experimental models. The results indicated that most of them were found to exhibit good activity.
The synthesis, characterization and spectroscopic s tudies of new N-substituted pthalimide analog... more The synthesis, characterization and spectroscopic s tudies of new N-substituted pthalimide analogues 2 – 5 with antibacterial activity were described. The compound s were synthesized using phthalic anhydride with va rious amines (aminoethanol , aminopropanol,amino ethyl mo rphline, amino ethyl morphline iodide)in reflux syn thesizer. The purity of the synthesized products were monitor ed by using TLC in an appropriate developing system . The structures of the new synthesized compounds were co nfirmed byusing physical and spectral analysis. Ant ibacterial activity of the synthesized derivatives 2-5 were done in comparison with Phenol as standard com pound. All the selected compounds 2-5 showed very good activity against staphylococcus a ureus(S.aureus), Escherichia coli ( E. Coli ) when compared with Phenol.
International Journal of Pharmaceutical & Biological Archive, 2012
Most all tricyclic compounds derived from theophylline were investigated in the respect of their ... more Most all tricyclic compounds derived from theophylline were investigated in the respect of their anticancer, circulatory blood system activity and as anti-inflammatory agents. The synthesis of new tricyclic purine derivatives with anellated in 7,8-position of theophylline five, six, seven membered heterocyclic ring system. of lactam and non-lactam structure modified by a basic substituent at N8, N9 and N10 position. It has been shown that new tricyclic theophylline derivatives possess sedative, analgesic properties, neurolleptic-like activity and hypothermizing properties. Some structural elements modification influence the central nervous system activity in the respect of: - Kind of the additional ring. - Alkylamine substituent in 9 position of tricyclic system. Our goal was to give a wide scope literature review of the tricyclic and tetracyclic theophylline derivatives as adenosine, 5-HT, benzodiazpine receptors, and phosphodiaesterase inhibitors, because the new compounds are of ...
INTRODUCTION The imidazole ring is containing five membered ring systems have been described for ... more INTRODUCTION The imidazole ring is containing five membered ring systems have been described for their biological activity against various micro organisms 1,2. It is commonly found as a part of structure substances such as histamine and purine, also in a number of pharmaceutical drugs, such as antifungal agent 1 (ketoconazole), antiprotozoal agentsmetronidazole 3 (1) and antihistamine cimetidine 4 (2). N-hydroxyimidazoles are analogous of imidazole, have been prepared and tested biologically. Besides this, apesticidal screening was carried out by Allan 5 on a series of Nhydroxyimidazoles (3) and found them to have herbicide and insecticide activities. Antihypertensive 6 activity was observed in some ABSTRACT The imidazole ring is containing one of the important heterocyclic compounds found in endogenous biomolecules and pharmaceutical preparations. Different methods have been reported for the synthesis of 1-Hydroxyimidazoles and a number of them reported to possess significant biological activity, thus synthesis of some new derivatives are introduced for better antibacterial activity.
ABSTRACT N-Hydroxyamide, alkanoloamides, dialkylamino-alkylamides and some of morpholinealkylamid... more ABSTRACT N-Hydroxyamide, alkanoloamides, dialkylamino-alkylamides and some of morpholinealkylamides of pyrimidin-8-on[2,1-f]theophylline-9-alkylcarboxylic acids were prepared and preliminary tested for their cardiovascular activity. Some of the tested compounds presented effects on arrhythmia parameters and blood pressure. The most interesting were dialkylamino-alkylamides and their morpholine analogs (4a-10a), which protected the heart against the bradycardia and diminished mortality of animals. In comparison to the chinidini sulfas the strongest activity was observed for diethylaminoethylamide of pyrimidin-8-on[2,1- f]theophylline-9-acetic acid (4a). Amides (1-3) without the basic center in the substituent showed weak antihypertensive properties.
The naturally occuring methylxanthines, caffeine and theophylline are classical adenosine recepto... more The naturally occuring methylxanthines, caffeine and theophylline are classical adenosine receptor antagonists. Caffeine is widely consumed in beverages, theophylline is used as a drug in the treatment of bronchial asthma while several other xanthines derived from caffeine and theophylline are therapeutically used as analeptics, antiasthmatics, vasodilators, antihypertensives and diuretics. Besides adenosine receptor antagonistic activities, they have other mechanisms of action including inhibition of phosphodiesterases, and mobilization of intracellular calcium ions are reported.
Journal of Biomedical and Pharmaceutical Research, Apr 29, 2013
Aliterature review studies of physicochemical properties and reactivity of naphthyridine derivati... more Aliterature review studies of physicochemical properties and reactivity of naphthyridine derivatives due to their broad spectrum activity. The research work still looking for the promising compound of these derivatives and also the aim of our studies to activate this area of research and propose these derivatives as a target compounds that could be oriented as pharmaceutical compounds in medicine.
Journal of Pharmaceutical and Scientific Innovation, Feb 19, 2014
Keeping in view of the biological potential of Schiff bases attached to heterocyclic ring system;... more Keeping in view of the biological potential of Schiff bases attached to heterocyclic ring system; a series of novel Schiff's base derivatives were synthesized 1-8 successfully in appreciable yields. The structures of all the synthesized derivatives were confirmed by physical and spectral analysis. Furthermore, all synthesized compounds were evaluated for antifungal activity against different strains of fungal organisms. Some of the compounds exhibited appreciable antifungal activity comparing to the reference compound (Nystatine).
Synthesis of some new 1,8-naphthyridines (out of which four are new) derivatives were described. ... more Synthesis of some new 1,8-naphthyridines (out of which four are new) derivatives were described. The synthesized compounds were prepared by the condensation of 2,6-diaminopyridine and 1,3-dicarbonyl compounds with various chemical reagents. However, there are significant effects on yields and isomer ratios depending on the use of perchloric or phosphoric acids in the condensation reaction. Based on the isomer ratios, some probable reaction mechanisms are proposed. The purity of the new synthesized compounds were checked by performing TLC using appropriate solvent and the spots were visualized in the UV light. The chemical structure of the compounds were confirmed by FT-IR, 1 H, 13 C-NMR spectroscopy.
We have tried to assess the acetylation process in tuberculosis a sample of Libyan patient, Simul... more We have tried to assess the acetylation process in tuberculosis a sample of Libyan patient, Simultaneous measurement of isoniazid (INH) and its main acetylated metabolite acetylisoniazid (AcINH) in plasma is realized by high-performance liquid chromatography (HPLC). INH and its main metabolite in human plasma were measured after taken single oral dose (200-300 mg), after 3 hours the samples of patient´s venous blood (4 ml) were collected into heparinized tubes and immediately centrifuged. The plasma samples were then deproteinized by trichloroacetic acid. The analytes separated by HPLC on pinnacle II C18 column (water). Nicotinamide is used as internal standard. The mobile phase is 0.05 M ammonium acetate buffer (pH 6) acetonitrile (99:1, v/v). The detection is by ultraviolet absorbance at 275 nm. Retention time recorded for INH, AcINH and the internal standard were 7.3, 9.9 and 14.2 min respectively. The result obtained showed that the plasma concentration of INH to 48% patient sho...
Biomedical Journal of Scientific & Technical Research, 2020
There are several ways by which organic compounds can interact with Deoxyribonucleic Acid (DNA), ... more There are several ways by which organic compounds can interact with Deoxyribonucleic Acid (DNA), including covalent bonding, electrostatic binding or intercalation. Intercalation occurs when the compound (ligand) of appropriate size and chemical nature fit between base pairs of DNAs [1,2]. In order for an intercalator to fit between base pairs, they must consist of planar polycyclic aromatic rings, and the DNA must dynamically open a space between its base pairs by unwinding [3]. The ability of intercalating agents to inhibit DNA replication and nucleic acid synthesis in vivo leads to their extensive use as mutagens, antibiotics, antibacterials, trypanocides, schistosomicides, and antitumor agents. The intercalative binding is non-covalent stacking interaction resulting from the insertion of a planar aromatic ring(s) between the base pairs of the DNA double helix [4,5]. Many classes of organic compounds have been reported to possess good DNA intercalating activity. Among these agents, Schiff's bases (imines) showed a large range of biological activities including antiviral, antibacterial, antiproliferative, antifungal, and antimalarial activities [6-8].
The 2019 coronavirus (COVID-19) pandemic is spreading worldwide, with a spectacular increase in d... more The 2019 coronavirus (COVID-19) pandemic is spreading worldwide, with a spectacular increase in death missing any effective therapeutic treatment up to now. Molecular docking is a recognized computational tool to assist in early drug discovery and development. Molecular docking analysis was carried out using 2-(4-(aminomethyl)phenyl)isoindoline-1,3-dione Schiff base conjugates with SARS-CoV-2 protease enzyme and COVID-19 main protease in apo form (6M03). The compounds with the best normalized docking scores to protease enzyme (6LU7) were ARG3 (-8.1 kcal/mole), ARG7 (-8.1 kcal/mole) and ARG6 (-8.0 kcal/mole). The best docking ligands for main protease in apo form (6M03) were ARG7 (-8.7 kcal/mole), ARG6 (-8.6 kcal/mole) and ARG3 (-8.4 kcal/mole). The structural similarity between these conjugates inspired us to perform in silico studies to check their possible binding interactions with essential SARS-CoV-2 proteins. These studies provide insight into the potential binding between Schi...
A series of new Schiff's bases of Sulfanilamide 1a-8a were synthesized by condensation of sul... more A series of new Schiff's bases of Sulfanilamide 1a-8a were synthesized by condensation of sulfanilamide with different substituted aromatic aldehydes. The structures of these products were confirmed by physical and spectral analysis. Antibacterial and antifungal activity of the synthesized derivatives 1a-8a were done in comparison with Ciprofloxacin and Ketoconazole as standard compounds. All the 3 selected strains of bacteria and fungi namely S. Aureus, E. Coli and C. Albicans. Compounds 5a, 7a showed very good activity against C .Albicans while compounds 2a, 8a showed moderate activity when compared with standard drug Ketoconazole.
Most all tricyclic compounds derived from theophylline were investigated in the respect of their ... more Most all tricyclic compounds derived from theophylline were investigated in the respect of their anticancer, circulatory blood system activity and as anti-inflammatory agents. The synthesis of new tricyclic purine derivatives with anellated in 7,8-position of theophylline five, six, seven membered heterocyclic ring system. of lactam and non-lactam structure modified by a basic substituent at N8, N9 and N10 position. It has been shown that new tricyclic theophylline derivatives possess sedative, analgesic properties, neurolleptic-like activity and hypothermizing properties. Some structural elements modification influence the central nervous system activity in the respect of:-Kind of the additional ring.-Alkylamine substituent in 9 position of tricyclic system. Our goal was to give a wide scope literature review of the tricyclic and tetracyclic theophylline derivatives as adenosine, 5-HT, benzodiazpine receptors, and phosphodiaesterase inhibitors, because the new compounds are of inte...
drugs (NSAIDs) are widely used for reducing pain and swellings associated with inflammation and r... more drugs (NSAIDs) are widely used for reducing pain and swellings associated with inflammation and represent an area in continuous and ever growing development. To control pain due
There are many activities performed in a repeated way and in a risk positions that cause fatigue ... more There are many activities performed in a repeated way and in a risk positions that cause fatigue and subsequently may origin musculoskeletal disorders (MSD). Although the disorders may appear as a consequence of an intense effort...
A series of N-substituted benzimidazole derivatives (1-5) was synthesized. Benzimidazole nucleus ... more A series of N-substituted benzimidazole derivatives (1-5) was synthesized. Benzimidazole nucleus was acylated in 1-position with benzoyl chloride in basic medium at room temperature to form N-acylated benzimidazole (1). Reaction of the Nacylated benzimidazole (1) with different amines yields the desired N-substituted benzimidazole derivatives (2-5). All the synthesized compounds (1-5) were evaluated in vivo for analgesic activity by acetic acid induced writhing and hot plate tests in mice. In comparison to the standard drug aspirin at the same dose (50mg/kg), compound 4 was the most potent as it decreased the number of writings to 17% comparing to control. However, aspirin resulted in a decrease equal to 12% of the control. In addition, all the test compounds except 5 produced some reduction in reaction time for hot plate test. Markedly, the effect was statistically significant with compounds 3 and 4.
In the present study a new ester–ether phenol derivatives 2-5 have been synthesized and character... more In the present study a new ester–ether phenol derivatives 2-5 have been synthesized and characterized. Their structures have been established on the physical and spectral analysis. The synthetic compounds were screened in vitro for their antimicrobial activity against: Metacillin resistance staphylococcus aureus, Escherichia coli ATCC 11934, Extended spectrum B-lactamase (12,54,70), staphylococcus aureus, Bacillus subtales and Candida albicans (669,1047, 772, 1057, 660). The best result obtained at the concentration 100μg with compound phenyl benzoate 2 and 1Nitro-4(phenoxymethyl)benzene 5 against fungus (Candida albicans 660, 1047, 1057 ). While Compound 5 possess significant active against gram positive and gram negative bacteria comparable to that of the standard drugs.
The present study was aimed to study the analgesic and antiepileptic potency of some New succinim... more The present study was aimed to study the analgesic and antiepileptic potency of some New succinimide derivatives. Various aromatic amines clubbed succinimide derivative compounds 2-13 were synthesized by using succinic anhydride and various amines in reflux synthesizer. The structures of the synthesized derivatives were confirmed by means of physical and spectral analysis. All the synthesized compounds were evaluated in vivo for analgesic and antiepileptic activities by using standard experimental models. The results indicated that most of them were found to exhibit good activity.
The synthesis, characterization and spectroscopic s tudies of new N-substituted pthalimide analog... more The synthesis, characterization and spectroscopic s tudies of new N-substituted pthalimide analogues 2 – 5 with antibacterial activity were described. The compound s were synthesized using phthalic anhydride with va rious amines (aminoethanol , aminopropanol,amino ethyl mo rphline, amino ethyl morphline iodide)in reflux syn thesizer. The purity of the synthesized products were monitor ed by using TLC in an appropriate developing system . The structures of the new synthesized compounds were co nfirmed byusing physical and spectral analysis. Ant ibacterial activity of the synthesized derivatives 2-5 were done in comparison with Phenol as standard com pound. All the selected compounds 2-5 showed very good activity against staphylococcus a ureus(S.aureus), Escherichia coli ( E. Coli ) when compared with Phenol.
International Journal of Pharmaceutical & Biological Archive, 2012
Most all tricyclic compounds derived from theophylline were investigated in the respect of their ... more Most all tricyclic compounds derived from theophylline were investigated in the respect of their anticancer, circulatory blood system activity and as anti-inflammatory agents. The synthesis of new tricyclic purine derivatives with anellated in 7,8-position of theophylline five, six, seven membered heterocyclic ring system. of lactam and non-lactam structure modified by a basic substituent at N8, N9 and N10 position. It has been shown that new tricyclic theophylline derivatives possess sedative, analgesic properties, neurolleptic-like activity and hypothermizing properties. Some structural elements modification influence the central nervous system activity in the respect of: - Kind of the additional ring. - Alkylamine substituent in 9 position of tricyclic system. Our goal was to give a wide scope literature review of the tricyclic and tetracyclic theophylline derivatives as adenosine, 5-HT, benzodiazpine receptors, and phosphodiaesterase inhibitors, because the new compounds are of ...
INTRODUCTION The imidazole ring is containing five membered ring systems have been described for ... more INTRODUCTION The imidazole ring is containing five membered ring systems have been described for their biological activity against various micro organisms 1,2. It is commonly found as a part of structure substances such as histamine and purine, also in a number of pharmaceutical drugs, such as antifungal agent 1 (ketoconazole), antiprotozoal agentsmetronidazole 3 (1) and antihistamine cimetidine 4 (2). N-hydroxyimidazoles are analogous of imidazole, have been prepared and tested biologically. Besides this, apesticidal screening was carried out by Allan 5 on a series of Nhydroxyimidazoles (3) and found them to have herbicide and insecticide activities. Antihypertensive 6 activity was observed in some ABSTRACT The imidazole ring is containing one of the important heterocyclic compounds found in endogenous biomolecules and pharmaceutical preparations. Different methods have been reported for the synthesis of 1-Hydroxyimidazoles and a number of them reported to possess significant biological activity, thus synthesis of some new derivatives are introduced for better antibacterial activity.
ABSTRACT N-Hydroxyamide, alkanoloamides, dialkylamino-alkylamides and some of morpholinealkylamid... more ABSTRACT N-Hydroxyamide, alkanoloamides, dialkylamino-alkylamides and some of morpholinealkylamides of pyrimidin-8-on[2,1-f]theophylline-9-alkylcarboxylic acids were prepared and preliminary tested for their cardiovascular activity. Some of the tested compounds presented effects on arrhythmia parameters and blood pressure. The most interesting were dialkylamino-alkylamides and their morpholine analogs (4a-10a), which protected the heart against the bradycardia and diminished mortality of animals. In comparison to the chinidini sulfas the strongest activity was observed for diethylaminoethylamide of pyrimidin-8-on[2,1- f]theophylline-9-acetic acid (4a). Amides (1-3) without the basic center in the substituent showed weak antihypertensive properties.
The naturally occuring methylxanthines, caffeine and theophylline are classical adenosine recepto... more The naturally occuring methylxanthines, caffeine and theophylline are classical adenosine receptor antagonists. Caffeine is widely consumed in beverages, theophylline is used as a drug in the treatment of bronchial asthma while several other xanthines derived from caffeine and theophylline are therapeutically used as analeptics, antiasthmatics, vasodilators, antihypertensives and diuretics. Besides adenosine receptor antagonistic activities, they have other mechanisms of action including inhibition of phosphodiesterases, and mobilization of intracellular calcium ions are reported.
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Papers by Omran Fhid