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Srikanth L.,Prasad Institute of Pharmaceutical science | Raghunandan N.,Balaji Institute of Pharmaceutical science
Der Pharma Chemica | Year: 2011

Benzimidazoles display a broad spectrum of potential pharmacological activities and are present in a number of pharmacologically active molecules such as Albendazole/ Mebendazole/ Thiabendazole (antihelmentic), Omeprazole (anti-ulcer). These compounds carrying different substituents in the benzimidazole structure are associated with a wide range of biological activities. Changes in their structure have offered a high degree of diversity that has proven useful for the development of new therapeutic agents having improved potency and lesser toxicity. In this context, the recently synthesized 2-Substituted benzimidazole derivatives possessing important pharmacological activities have been highlighted.

Srikanth L.,Prasad Institute of Pharmaceutical science | Raghunandan N.,Balaji Institute of Pharmaceutical science | Srinivas P.,Prasad Institute of Pharmaceutical science | Reddy G.A.,Prasad Institute of Pharmaceutical science
International Journal of Pharma and Bio Sciences | Year: 2010

In view of various biological activities of both thiazolidinediones and quinoline derivatives like antidiabetic, antifungal, antitumoral, anti-inflammatory, retinoidal, anti atherosclerotic activities, it was our interest to prepare various thiazolidinedione derivatives with a quinoline ring moiety and to evaluate them for antidiabetic activity. 5-(4-fluorobenzyl)-2,4-thiazolidinedione was synthesized by reaction of 4-fluoroaniline with methyl acrylate to give crude 2-Bromo-3-(4-fluoro-phenyl)-propionic acid methyl ester as an oil which was treated with thiourea in presence of sodium acetate and ethanol to give 5-(4-fluoro-benzyl)-2-imino-thiazolidine-4-one which on oxidation gave 5-(4-fluoro-benzyl)-thiazolidine-2,4-dione. This was condensed with the quinoline derivatives in presence of Tetrahydrofuran. Among the synthesized derivatives five of them were screened for oral hypoglycemic activity, the compounds SK, SK-3 were showing significant activity and compound SK-2 was showing moderate activity and compounds SK-4 and SK-5 were active. The structures of newly synthesized compounds were established on the basis of elemental analysis, TLC, IR and 1H NMR spectral studies.

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