Quinoline fused Benzimidazoles and their Pharmacological Evaluations

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Bioactivities of Quinoline fused Benzimidazoles

ISBN: 3659614408
ISBN 13: 9783659614408
Autor: Patel, Amit/Chikhalia, Kishor/Kumari, Premlata
Verlag: LAP LAMBERT Academic Publishing
Umfang: 68 S.
Erscheinungsdatum: 24.10.2014
Auflage: 1/2014
Format: 0.5 x 22 x 15
Gewicht: 119 g
Produktform: Kartoniert
Einband: Kartoniert
Artikelnummer: 7415148 Kategorie:

Beschreibung

The present book describes the one pot route for quinoline fused azeto[1,2-a]benzimidazole derivatives, involving condensation of o-phenylenediamine with 2-chloroquinoline-3-aldehydes and subsequent Pd-catalyzed cross coupling of resulting benzimidazole NH with 2-choloroquinoline leading to the formation of four-membered azetidine ring as a key step. Synthesized analogs were further tested for antimicrobial, antimycobacterial and anti-prostate cancer activity to observe the variation in biological activity. The bioassay results revealed that the majority of final analogs exhibited potential bio efficacies with the remarkable level of MICs comparable to control drugs. Considering the excellent reaction efficiency, wide substrate scope and very mild reaction conditions, the mentioned synthetic protocols may be attractive routes for the synthesis of other heterocycles. It is worth concluding that insertions of various functional groups are essential to increase the different pharmacological activities of the resultant scaffolds by lowering the MICs in all the cases evaluated. In short, our findings might be beneficial as leads to designing new potential bioactive agents.

Autorenporträt

Dr. Amit B. Patel is currently working as an Asst. Professor at HVHP Institute of PG Studies and Research, KSV, Kadi, India. His research interest is mainly concerned with the development of Transition-Metal mediated synthesis of variety of new organic and heterocyclic scaffolds, as well as the development of new catalytic systems.

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