Synthesis of Azetidin-2-One Derivatives as Inhibitor of Secretory Phospholipase A2 with Anti-Inflammatory Activity

Authors: Yerigeri, Mayur C.; Murari, Satish K.; Mohammed, Salahuddin; Math, Shanta K.S.; Thimmaiah, Kuntebommanahalli N.; Vishwanath, Bannikuppe S.a.n.n.a.n.a.i.k.

Source: Letters in Drug Design & Discovery, Volume 2, Number 4, June 2005 , pp. 307-310(4)

Publisher: Bentham Science Publishers

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Abstract:

The title compounds have been synthesized and tested for structure activity relationship for Phospholipase A2 (PLA2) [E.C. 3.1.1.4] enzyme inhibition. The in vitro PLA2 enzyme inhibitory activity of azetidin-2-one derivatives and in vivo anti-inflammatory activity studies using mice are highlighted. The results show that some azetidin-2-one derivatives are very good PLA2 inhibitors and can also be used as antiinflammatory drugs.

Keywords: phospholipase; anti-inflammatory; azetidin-one derivatives

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1570180054038404

Affiliations: 1: Department of Medicinal Chemistry, V.L. College of Pharmacy, Raichur 584103, India.

Publication date: 2005-06-01

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Letters in Drug Design & Discovery publishes original letters on all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis will be on publishing quality papers very rapidly. Letters will be processed rapidly by taking full advantage of Internet technology for both the submission and review of manuscripts. The journal is essential reading to all pharmaceutical scientists involved in research in drug design and discovery.