Globally recognized genetic modification with time has supported the emergence of versatile and n... more Globally recognized genetic modification with time has supported the emergence of versatile and novel featured organisms in nature, some of which can be analogized with Pandora’s box elements; like Mycobacterium sp. which has revived itself again after again in a repetitive order over decades and, gradually, contriving a red alert on the world health graph. It needs to be rectified with the motivation of new drug approval considering the pipe line moieties or, apt a choice from the existing drug genera. Although, with genetic modification and advancement Mycobacterium tuberculosis has ruined the first-line therapy in ash, it also opens up different loops and wholes to drug susceptibility. New moieties: Tiliacorinine, 2′-nortiliacorinine, tiliacorine or Cyclohexylgriselimycin raised from different sources of nature, have given another opportunity for the survival, besides, new approved drugs, like bedaquiline, delamanid, pyrifazimine, telacebec, or the under focused pharmacophores; such as diarylquinoline, quinolones, ethylurea benzimidazole, etc. are the appreciable efforts achieved. Thereupon, InhA, KatG, Clp proteases, Menaquinone, DNA gyrase, VDR Fok1, etc. are the new target sets for the drug discovery which has immense potency to generate a number of targeted molecules with effective anti-TB activity. It is a critical discussion of the TB futuristic approach including, clinical trials, repurposed drugs, pipeline motifs, natural products, upcoming drug targets from the cell wall, protein, and DNA.
Carbohydrates in Drug Discovery and Development, 2020
Abstract In nature, all cells are covered with a complex array of carbohydrates particularly sial... more Abstract In nature, all cells are covered with a complex array of carbohydrates particularly sialic acids which is chemically a negatively charged nine-carbon α-keto aldonic acids. Because of their significant role on cell surfaces, the sialic acid-containing glycans certainly can mediate and modulate many important cellular interactions. Further, proteins having receptors to bind sialic acids are recognized to be involved in a wide variety of biological processes. Thus evaluation of carbohydrate-protein interaction and further their roles in vertebrates may results in enhanced understanding of normal physiology, pathological variance and human evolution. This chapter summarizes the structures and biological significance of sialic acid, their chemical diversity, biosynthesis followed by chemical modification and enzymatic synthesis of sialic acids, their impact in chemical biology, and also the neurobiology of sialic acid. Conclusively, this chapter highlights the recent advances and challenges at the interface of chemistry and biology of sialic acids in order to find out their scope in drug discovery and development.
Green Synthetic Approaches for Biologically Relevant Heterocycles, 2021
50 4.4.3 L'éducation (incluant la qualité de l'apprentissage, l'efficacité du système éducatif et... more 50 4.4.3 L'éducation (incluant la qualité de l'apprentissage, l'efficacité du système éducatif et l'accès aux compétences de base pour les jeunes déscolarisés et non scolarisés
Cu-catalyzed Ullmann coupling was performed for the facile synthesis of diverse benzoxazoles and ... more Cu-catalyzed Ullmann coupling was performed for the facile synthesis of diverse benzoxazoles and benzothiazoles in the presence of 1-(hydroxymethyl)-1H-benzotriazole as ligand and K 2 CO 3 as base in anhydrous DMF at 120 0 C.
, 21 cases of ruptured cerebral aneurysm accompanied by intraventricular hematoma with cast forma... more , 21 cases of ruptured cerebral aneurysm accompanied by intraventricular hematoma with cast formation (packed IVH) were considered. Excluding cases of deep coma accompanied by bilateral dilated pupils at the time of admission, radical surgery was performed in 13 patients in the extremely early phase, that is, within 12 h of hospital admission. The World Federation of Neurological Surgeons grades upon admission were Grade 5 in 11 cases and Grade 4 in two cases. All nonoperative cases died within a short period. The 6-month outcome of the 13 treated cases was good prognosis in 4 patients at modified Rankin Scale (mRS) 0-2, mRS 3 in 1, mRS 4 in 1, mRS-5 in 4, and death in 3. Treatment for aneurysm was performed with priority on clipping. All patients aged below 60 years receiving treatment regained consciousness; however, all elderly patients had poor prognosis. In cases of "long hour" unconsciousness, where 1 h or more had passed before emergency admission, prognosis was extremely poor, regardless of receiving treatment or not. For patients with ruptured cerebral aneurysm accompanied by packed IVH, who frequently exhibit a high level of disturbance of consciousness, the concept of a therapeutic time window should be kept in mind. In some cases, complete recovery has been achieved as a result of rapid treatment of aneurysm and excision of hematoma.
Copper(I)-catalyzed 1,3-dipolar cycloaddition between organic azides and terminal alkynes, common... more Copper(I)-catalyzed 1,3-dipolar cycloaddition between organic azides and terminal alkynes, commonly known as CuAAC or click chemistry, has been identified as one of the most successful, versatile, reliable, and modular strategies for the rapid and regioselective construction of 1,4-disubstituted 1,2,3-triazoles as diversely functionalized molecules. Carbohydrates, an integral part of living cells, have several fascinating features, including their structural diversity, biocompatibility, bioavailability, hydrophilicity, and superior ADME properties with minimal toxicity, which support increased demand to explore them as versatile scaffolds for easy access to diverse glycohybrids and well-defined glycoconjugates for complete chemical, biochemical, and pharmacological investigations. This review highlights the successful development of CuAAC or click chemistry in emerging areas of glycoscience, including the synthesis of triazole appended carbohydrate-containing molecular architectures (mainly glycohybrids, glycoconjugates, glycopolymers, glycopeptides, glycoproteins, glycolipids, glycoclusters, and glycodendrimers through regioselective triazole forming modular and bio-orthogonal coupling protocols). It discusses the widespread applications of these glycoproducts as enzyme inhibitors in drug discovery and development, sensing, gelation, chelation, glycosylation, and catalysis. This review also covers the impact of click chemistry and provides future perspectives on its role in various emerging disciplines of science and technology.
Globally recognized genetic modification with time has supported the emergence of versatile and n... more Globally recognized genetic modification with time has supported the emergence of versatile and novel featured organisms in nature, some of which can be analogized with Pandora’s box elements; like Mycobacterium sp. which has revived itself again after again in a repetitive order over decades and, gradually, contriving a red alert on the world health graph. It needs to be rectified with the motivation of new drug approval considering the pipe line moieties or, apt a choice from the existing drug genera. Although, with genetic modification and advancement Mycobacterium tuberculosis has ruined the first-line therapy in ash, it also opens up different loops and wholes to drug susceptibility. New moieties: Tiliacorinine, 2′-nortiliacorinine, tiliacorine or Cyclohexylgriselimycin raised from different sources of nature, have given another opportunity for the survival, besides, new approved drugs, like bedaquiline, delamanid, pyrifazimine, telacebec, or the under focused pharmacophores; such as diarylquinoline, quinolones, ethylurea benzimidazole, etc. are the appreciable efforts achieved. Thereupon, InhA, KatG, Clp proteases, Menaquinone, DNA gyrase, VDR Fok1, etc. are the new target sets for the drug discovery which has immense potency to generate a number of targeted molecules with effective anti-TB activity. It is a critical discussion of the TB futuristic approach including, clinical trials, repurposed drugs, pipeline motifs, natural products, upcoming drug targets from the cell wall, protein, and DNA.
Carbohydrates in Drug Discovery and Development, 2020
Abstract In nature, all cells are covered with a complex array of carbohydrates particularly sial... more Abstract In nature, all cells are covered with a complex array of carbohydrates particularly sialic acids which is chemically a negatively charged nine-carbon α-keto aldonic acids. Because of their significant role on cell surfaces, the sialic acid-containing glycans certainly can mediate and modulate many important cellular interactions. Further, proteins having receptors to bind sialic acids are recognized to be involved in a wide variety of biological processes. Thus evaluation of carbohydrate-protein interaction and further their roles in vertebrates may results in enhanced understanding of normal physiology, pathological variance and human evolution. This chapter summarizes the structures and biological significance of sialic acid, their chemical diversity, biosynthesis followed by chemical modification and enzymatic synthesis of sialic acids, their impact in chemical biology, and also the neurobiology of sialic acid. Conclusively, this chapter highlights the recent advances and challenges at the interface of chemistry and biology of sialic acids in order to find out their scope in drug discovery and development.
Green Synthetic Approaches for Biologically Relevant Heterocycles, 2021
50 4.4.3 L'éducation (incluant la qualité de l'apprentissage, l'efficacité du système éducatif et... more 50 4.4.3 L'éducation (incluant la qualité de l'apprentissage, l'efficacité du système éducatif et l'accès aux compétences de base pour les jeunes déscolarisés et non scolarisés
Cu-catalyzed Ullmann coupling was performed for the facile synthesis of diverse benzoxazoles and ... more Cu-catalyzed Ullmann coupling was performed for the facile synthesis of diverse benzoxazoles and benzothiazoles in the presence of 1-(hydroxymethyl)-1H-benzotriazole as ligand and K 2 CO 3 as base in anhydrous DMF at 120 0 C.
, 21 cases of ruptured cerebral aneurysm accompanied by intraventricular hematoma with cast forma... more , 21 cases of ruptured cerebral aneurysm accompanied by intraventricular hematoma with cast formation (packed IVH) were considered. Excluding cases of deep coma accompanied by bilateral dilated pupils at the time of admission, radical surgery was performed in 13 patients in the extremely early phase, that is, within 12 h of hospital admission. The World Federation of Neurological Surgeons grades upon admission were Grade 5 in 11 cases and Grade 4 in two cases. All nonoperative cases died within a short period. The 6-month outcome of the 13 treated cases was good prognosis in 4 patients at modified Rankin Scale (mRS) 0-2, mRS 3 in 1, mRS 4 in 1, mRS-5 in 4, and death in 3. Treatment for aneurysm was performed with priority on clipping. All patients aged below 60 years receiving treatment regained consciousness; however, all elderly patients had poor prognosis. In cases of "long hour" unconsciousness, where 1 h or more had passed before emergency admission, prognosis was extremely poor, regardless of receiving treatment or not. For patients with ruptured cerebral aneurysm accompanied by packed IVH, who frequently exhibit a high level of disturbance of consciousness, the concept of a therapeutic time window should be kept in mind. In some cases, complete recovery has been achieved as a result of rapid treatment of aneurysm and excision of hematoma.
Copper(I)-catalyzed 1,3-dipolar cycloaddition between organic azides and terminal alkynes, common... more Copper(I)-catalyzed 1,3-dipolar cycloaddition between organic azides and terminal alkynes, commonly known as CuAAC or click chemistry, has been identified as one of the most successful, versatile, reliable, and modular strategies for the rapid and regioselective construction of 1,4-disubstituted 1,2,3-triazoles as diversely functionalized molecules. Carbohydrates, an integral part of living cells, have several fascinating features, including their structural diversity, biocompatibility, bioavailability, hydrophilicity, and superior ADME properties with minimal toxicity, which support increased demand to explore them as versatile scaffolds for easy access to diverse glycohybrids and well-defined glycoconjugates for complete chemical, biochemical, and pharmacological investigations. This review highlights the successful development of CuAAC or click chemistry in emerging areas of glycoscience, including the synthesis of triazole appended carbohydrate-containing molecular architectures (mainly glycohybrids, glycoconjugates, glycopolymers, glycopeptides, glycoproteins, glycolipids, glycoclusters, and glycodendrimers through regioselective triazole forming modular and bio-orthogonal coupling protocols). It discusses the widespread applications of these glycoproducts as enzyme inhibitors in drug discovery and development, sensing, gelation, chelation, glycosylation, and catalysis. This review also covers the impact of click chemistry and provides future perspectives on its role in various emerging disciplines of science and technology.
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