A simple, efficient and rapid method for clay-catalyzed Knoevenagel condensation of heterocyclic aldehydes with active methylene compound under reflux condition is reported. This protocol offers high yield, shorter time and simple work procedure. The protocol does not require column chromatography for purification, and the process is environmentally benign. © 2014 Springer Science+Business Media.

Krishnakumar K

Department of Multimedia

School of Design

Vellore Campus

Nawaz Khan F

Department of Chemistry

School of Advanced Sciences

Badal Kumar Mandal

Jeong E.-D

Jin J.S.

Vellore Institute of Technology (VIT) is a private university located in&nbsp;Tamil Nadu, India. Founded in 1984, as Vellore Engineering College, the institution offers 20 undergraduate, 34 postgraduate, four integrated and four research programs. It has campuses in Vellore, Amravati, Bhopal and Chennai.

VIT is one of the top ranked private universities in India according to NIRF, THE and QS Rankings.&nbsp;Govt. of India has recognized&nbsp;VIT, Vellore as an&nbsp;Institution of Eminence. This has allowed VIT to take independent quality initiatives and move up in world ranking.

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VIT University

Research on Chemical Intermediates

A series of nicotinic acid conjugates with non-steroidal anti-inflammatory drugs (NSAID's) have been effectively synthesized using TBTU in high yield and purity. All the synthesized conjugates were evaluated for their in vitro anti-inflammatory activity.

European Journal of Pharmaceutical Sciences

Nicotinic acid conjugates of nonsteroidal anti-inflammatory drugs (NSAID’s) and their anti-inflammatory properties

Thyroxine, the main secretory hormone of thyroid gland, is produced from thyroglobulin by thyroid peroxidase/hydrogen peroxide/iodide system. The prohormone T4 is then converted to its potent form T3 by a selenocysteine- containing enzyme iodothyronine deiodinase. Autoantibodies which activate thyroid-stimulating hormone receptor are not under the pituitary feedback control system, and therefore, the uncontrolled production of thyroid hormones leads to a condition called "hyperthyroidism." The overproduction of T4 and T3 can be controlled by specific inhibitors, which either block the synthesis of thyroid hormone or reduce the conversion of T4-T3. Unique classes of such inhibitors are thiourea drugs, methimazole (MMI), 6-n-propyl-2- thiouracil, and carbimazole suggesting that thione moiety exhibit excellent antithyroid activity. We have carried out biomimetic studies by HPLC assay, which suggested that isochromene-1-thiones exhibit significant antithyroid activity by inhibiting the lactoperoxidase (LPO)-catalyzed iodination, comparable with MMI, and that the inhibitory effects of some of them were found to be much superior to those of MMI. Kinetic studies demonstrate that isochromene-1-thiones inhibit LPO irreversibly. Our inhibition studies suggest that isochromene-1-thiones might be another promising candidate with potential for developing therapeutics for hyperthyroidism. The quantitative structure-activity relationship (QSAR) was developed between the LPO-inhibitory activities of isochromene-1-thiones and their physiochemical properties. The statistical measures, such as r2 (0.81), r2adj (0.79), q2 (0.73), and F-ratio (39.05), were found to be within the acceptable range. © 2013 Springer Science+Business Media New York.

Medicinal Chemistry Research

Antithyroid agents and QSAR studies: Inhibition of lactoperoxidase- catalyzed iodination reaction by isochromene-1-thiones

The ethyl-2-chloroquinoline-3-carboxylates, 4, were achieved fromo-aminobenzophenones in two steps. i.e. initially, the ethyl-2-oxoquinoline- 3-carboxylates, 3, were obtained by base-catalyzed Friedlander condensations of o-aminobenzophenones, 1, and diethylmalonate, 2. The 2-chloroquinoline-3- carboxylates, 4, were then obtained by the reaction with POCl3 in good yields. The chemical structures were confirmed by FTIR, mass and 1H-NMR spectroscopic techniques. All the synthesized compounds were tested for their in vitro antibacterial activity against Bacillus subtilis and Vibrio cholera and found to possess moderate activity. © Springer Science+Business Media B.V. 2012.

Quinoline-3-carboxylates as potential antibacterial agents

Solvent-free, microwave-induced condensation of 2-aminoaryl alkyl ketones and ethyl 3-oxobutanoate in the presence of amberlite Na sr1L gave quinolinones in high yield when compared to other catalysts. Further, N-alkylation of the quinolinones was carried out effectively with various halides using amberlite Na sr1L. An N-alkylated quinolinone exhibited enhanced activities against B. subtilis, E. coli, and P. aeruginosa, similar to standard drug ampicillin. Two compounds showed effective activity against S. aureus, and one resulted in moderate activity against E. coli. © 2011 Springer-Verlag.

Monatshefte für Chemie - Chemical Monthly

Solvent-free synthesis and antibacterial studies of some quinolinones

An efficient and facile one-pot synthesis of 1,3-disubstituted isoquinolines 3 was accomplished from 3-substituted isocoumarins 1 through diketones, formed in situ via the Grignard reaction, in the presence of ammonium acetate, montmorillonite K-10 catalyst, and ethanol solvent. © Springer Science+Business Media B.V. 2011.

Journal	Data powered by TypesetResearch on Chemical Intermediates
Publisher	Data powered by TypesetSpringer Science and Business Media LLC
ISSN	0922-6168
Open Access	0