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The NSAIDs have known to cause serious problems such as gastric ulceration, bleeding and renal disorders on long term medication. These severe side effects are partially due to their nonselectivity towards to COX-2 enzyme. Hence, newer, selective COX-2 enzyme inhibitors have been developed to overcome the toxicity problems. Recently, Rofecoxib and Celecoxib were withdrawn due to cardiac toxicity.1,2-disubstituted five-membered heterocyclic compounds have shown selectivity towards COX-2 inhibition. But, the toxicity reports of drugs like Rofecoxib and Celecoxib in this category prompted us to synthesize 1,2-diaryl diazepines (E) and their derivatives as, survey of literature indicated the diazepine heterocyclic system to have anti-inflammatory activity.
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The NSAIDs have known to cause serious problems such as gastric ulceration, bleeding and renal disorders on long term medication. These severe side effects are partially due to their nonselectivity towards to COX-2 enzyme. Hence, newer, selective COX-2 enzyme inhibitors have been developed to overcome the toxicity problems. Recently, Rofecoxib and Celecoxib were withdrawn due to cardiac toxicity.1,2-disubstituted five-membered heterocyclic compounds have shown selectivity towards COX-2 inhibition. But, the toxicity reports of drugs like Rofecoxib and Celecoxib in this category prompted us to synthesize 1,2-diaryl diazepines (E) and their derivatives as, survey of literature indicated the diazepine heterocyclic system to have anti-inflammatory activity.
Biografía del autor
Prof. Chirag J. Patel, Ph.D. fellow in Pharmaceutical Sciences at K.S.K.V. Kachchh University, Bhuj-Kachchh, Gujarat, INDIA. Field of Study: Phytopharmacoligal Screening of Some Laticiferous Plants & Drug Design with Development. Presently working as an Associate Professor at Veerayatan Institute of Pharmacy, India from last seven years.
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Design and Synthesis of 1,4-Diazepines as Selective Cox-II Inhibitors
Verlag:
LAP LAMBERT Academic Publishing Feb 2013, 2013
ISBN 10: 3659337862
ISBN 13: 9783659337864
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Taschenbuch
Anbieter: buchversandmimpf2000, Emtmannsberg, BAYE, Deutschland
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Taschenbuch. Zustand: Neu. Neuware -The NSAIDs have known to cause serious problems such as gastric ulceration, bleeding and renal disorders on long term medication. These severe side effects are partially due to their nonselectivity towards to COX-2 enzyme. Hence, newer, selective COX-2 enzyme inhibitors have been developed to overcome the toxicity problems. Recently, Rofecoxib and Celecoxib were withdrawn due to cardiac toxicity.1,2-disubstituted five-membered heterocyclic compounds have shown selectivity towards COX-2 inhibition. But, the toxicity reports of drugs like Rofecoxib and Celecoxib in this category prompted us to synthesize 1,2-diaryl diazepines (E) and their derivatives as, survey of literature indicated the diazepine heterocyclic system to have anti-inflammatory activity.Books on Demand GmbH, Überseering 33, 22297 Hamburg 68 pp. Englisch. Artikel-Nr. 9783659337864
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