Indole

Sumatriptan is a potent and selective 5-HT 1B and 5-HT 1D agonist used in the symptomatic treatment of migraine; it shows poor oral bioavailability ascribed, in part, to its low lipophilicity. In an attempt to develop acyloxymethyl prodrugs of sumatriptan suitable for oral administration, we carried out the reaction of sumatriptan with chloromethyl esters. To our surprise, acyloxymethylation occurred preferentially at the indole nitrogen rather than at sulfonamide nitrogen, reflecting a difference either in product stability or in the nucleophilicities of the indole and sulfonamide anions. The hydrolysis of the corresponding N 1 -acyloxymethyl derivatives was studied in aqueous buffers and in human plasma, by HPLC. N 1 -Acyloxymethyl derivatives of sumatriptan are rapidly hydrolysed to the chemically stable N 1 -hydroxymethylsumatriptan at pH 1-13. Slow formation of the parent drug was observed only at high pH values. Hydrolysis of sumatriptan derivatives is slower in human plasma than in phosphate buffer and also generates N 1hydroxymethylsumatriptan rather than the parent drug. These results indicate that N 1 -acyloxymethyl derivatives of sumatriptan cannot be considered as true prodrugs of sumatriptan.

RESUMEN
El uso de Rizobacterias promotoras de crecimiento vegetal (PGPR, por sus siglas en ingles) constituye una alternativa al uso de fertilizantes químicos favoreciendo el rendimiento de los cultivos. La presente investigación tuvo como objetivo la búsqueda, se-lección y caracterización de PGPR de los géneros Azotobacter, Azospirillum y Pseudomonas nativas de la rizósfera de cultivos de Ipomoea batatas de zonas productoras representativas del Caribe Colombiano. Los aislados seleccionados se caracterizaron mole-cularmente y realizaron pruebas de solubilización de fósforo, producción de índoles y reducción de acetileno. Las cepas fueron probadas a nivel de invernadero en plántulas de Ipomoea batatas producidas in vitro en las que se evaluó la altura, longitud radicu-lar, masa seca de la parte aérea y radicular. Asociada a la rizósfera de Ipomoea batatas se obtuvieron cepas de Azotobacter vine-landii, Azotobacter chroococcum, Azospirillum lipoferum, Azospirillum brasilense y Pseudomonas denitrificans, las cepas fueron capaces de solubilizar fósforo, producir índoles y reducir acetileno. Se obtuvo incrementos en parámetros de crecimiento como longitud radicular, altura, peso seco aéreo y radicular en plántulas de Ipomoea batatas en invernadero con la inoculación de las bacterias seleccionadas frente a plántulas sin inocular. Los resultados catalogan a los aislados obtenidos como posibles microorga-nismos con potencial como biofertilizantes en batata.

The newly synthesized thirteen disperse disazo dyes 3a–3m were prepared by diazotization of 5-amino-4-arylazo-3-methyl-1H-pyrazoles 2a–2m and coupling with 2-methyl indole. Their structures were characterized by UV–vis, FT-IR, 1 H NMR and elemental analysis. Solvatochromic properties in different solvents were studied. Also, the effects of acid and base on the visible absorption spectra of the dyes were informed. Besides, the theoretical vibrational frequencies have been scaled and compared with the corresponding experimental data. 1 H NMR spectra were recorded and chemical shifts of the molecules were compared to TMS by using the Gauge-Independent Atomic Orbital (GIAO) method. A study on the electronic and optical properties, absorption wavelengths, excitation energy and dipole moment is performed using DFT method. NBO analysis is carried out to picture the charge transfer between the localized bonds and lone pairs. All spectroscopic properties examined with the experimental techniques were supported with the computed results.

The capacity to solubilize phosphate and to produce indole compounds Indole Acetic Acid type, was evaluated in 15 strains isolated
from castor bean lignocellulosic residues (Ricinus communis). To determine the solubilizing activity of phosphates a qualitative test by
using Pikovskaya culture medium was employed and for the evaluation of the production of indole compounds (IAA) a Salkowsky
colorimetric analysis technique was applied. Among the microorganisms tested, the Bacillus pumilus GIBI 206 demonstrated capacity
to solubilize phosphates and Bacillus subtilis GIBI 200 showed of capacity to solubilize phosphates and to produce Indoleacetic Acid
(IAA). To determine the effect of the Bacillus subtilis strain on germination and growth promotion, tomato seeds (Solanum lycopersicum
‘Santa Clara’) were inoculated; the inoculation of the seeds along with the microorganism revealed statistically significant differences,
during the germination stage compared to the control treatment. Nevertheless, it revealed a positive influence on the development
of tomato plants, originating a significant increase on the mass and length of its stem and root. The results of this research offer the
possibility of using the Bacillus subtilis as a growth promoter in tomato seedlings and in the formulation of bio-products.
RESUMEN
La capacidad para solubilizar fosfatos y producir compuestos indólicos del tipo Ácido Indol Acético, se evaluó en 15 cepas aisladas
de residuos lignocelulósicos de higuerilla (Ricinus communis). Para determinar la actividad solubilizadora de fosfatos se realizó una
prueba cualitativa utilizando medio de cultivo Pikovskaya y para evaluar la producción de compuestos indólicos (AIA) se empleó
la técnica colorimétrica de Salkowsky. Entre los microorganismos evaluados, Bacillus pumilus GIBI 206 mostró tener la capacidad
para solubilizar fosfatos y Bacillus subtilis GIBI 200 evidenció capacidad para solubilizar fosfatos y producir Ácido Indolacético
(AIA). Para determinar el efecto de la cepa Bacillus subtilis sobre la germinación y promoción de crecimiento, se inoculó en semillas
de tomate (Solanum lycopersicum cultivar Santa Clara); la inoculación de las semillas con el microorganismo no mostró diferencias
estadísticamente significativas en el tiempo de germinación en comparación con el tratamiento control, sin embargo mostró influir
positivamente en el desarrollo de las plantas de tomate generando un aumento significativo sobre la masa y longitud del tallo y de
la raíz. Los resultados de esta investigación ofrecen la posibilidad de utilizar a Bacillus subtilis como promotora de crecimiento en
plántulas de tomate y en la formulación de bioinsumos.

Indole compounds are important class of therapeutic molecules, which have excellent pharmaceutical applications. The objective of present research was to investigate the influence of biofield treatment on physical and thermal properties of indole. The study was performed in two groups (control and treated). The control group remained as untreated, and biofield treatment was given to treated group. The control and treated samples were characterized by X-ray diffraction (XRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Fourier transform infrared (FT-IR) spectroscopy and ultraviolet-visible (UV-Vis) spectroscopy. XRD study demonstrated the increase in crystalline nature of treated indole as compared to control. Additionally, the treated indole showed increase in crystallite size by 2.53% as compared to control. DSC analysis of treated indole (54.45ºC) showed no significant change in melting temperature (Tm) in comparison with control sample (54.76ºC). A significant increase in latent heat of fusion (ΔH) by 30.86% was observed in treated indole with respect to control. Derivative thermogravimetry (DTG) of treated indole showed elevation in maximum thermal decomposition temperature (Tmax) 166.49ºC as compared to control (163.37ºC). This was due to increase in thermal stability of indole after biofield treatment. FT-IR analysis of treated indole showed increase in frequency of N-H stretching vibrational peak by 6 cm-1 as compared to control sample. UV spectroscopy analysis showed no alteration in absorption wavelength (λmax) of treated indole with respect to control. The present study showed that biofield has substantially affected the physical and thermal nature of indole.

A combined DFT and experimental study of the structure and the harmonic vibrational frequencies of free and solvated indole was performed. The DFT study included full geometry optimizations, as well as numerical harmonic vibrational UU Ž analyses at BLYPr6-31G level of theory. The solvent influence was included via the SCRF methodology within the . Onsager model . The FTIR spectra of indole solutions in CCl were recorded and compared with the theoretical results. The 4 BLYP formalism was shown to be very suitable for vibrational assignments without scaling in the 1600-1000 cm y1 Ž y1 . frequency range. The computed higher frequency modes 3500-3000 cm overestimate the experimental values, and scaling with a constant factor of about 0.98 is required. The continuum solvation has only a subtle influence on both the structure and harmonic force field. However, especially for the frequency range in which no scaling is needed, the gradient-corrected form of the DFT methodology is much more useful for vibrational assignments than the standard HF procedures that include scaling. On the basis of these more accurate DFT calculations, several reassignments were suggested Ž . in the vibrational spectra of the vapour specimen compared to the HFr3-21G ones , which improved the convergence of the subsequent force fields fitting. q

Montmorillonite K-10 clay catalyzed solvent-free synthesis of bis-indolylindane-1,3-dione, 2-(1 0 ,3 0 -dihydro-1H-[2,3 0 ]biindolyl-2 0 -ylidene)-indan-1,3-dione and bisindolylindeno[1,2-b]quinoxaline under microwave irradiation a b s t r a c t An environmentally benign protocol has been described for the synthesis of novel 2-(1 0 ,3 0 -dihydro-1H-[2,3 0 ] biindolyl-2 0 -ylidene)-indan-1,3-diones/bis-indolylindane-1,3-diones from ninhydrin and 3-substituted/ unsubstituted indoles. It uses montmorillonite K-10 as catalyst in a solvent-free condition under microwave irradiation. The method was also used for the synthesis of novel bisindolylindeno[1,2-b]quinoxaline derivatives.

Boar taint is an off-odour that entails negative consumer reactions. In this study two extraction and UHPLC-HRMS analysis methods, valuable for evaluation of consumer acceptance towards boar meat, were developed for quantification of indole, skatole, and androstenone in different meat products. Sample pretreatment consisted of extraction with methanol and a homogenising step (cooked ham, minced meat, tenderloin, bacon, cutlets, blade loin, uncooked ham) or a melting step (salami sausage and liver paste). Both methods were validated according to CD 2002/657/EC and ISO 17025 guidelines. Good performance characteristics were obtained. Good linearity (R 2 P 0.99) and no lack of fit was observed (95% confidence interval; F-test, p > 0.05). Also good recovery (89–110%) and satisfactory precision: repeatability (RSD 6 14.9%) and within-laboratory reproducibility (RSD 6 17.2%) were obtained. Analysis of cooked ham and salami sausage samples proved the applicability of both methods for routine analysis.