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Design of β-Lactams with Mechanism Based Nonantibacterial Activities

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The majority of nonantibacterial activities discovered for β-lactam derivatives during the last 15 years are based on their ability to form a stable covalent complex with nucleophile in the active site of enzymes regulating fundamental physiological processes in mammalian organism such as serine and cysteine proteases, LDL phospholipase A2, A-independent transacylase and some still indeciphered enzymes. Regulation of their catalytic activity both in vitro and in vivo by compounds designed on the cephalosporin, penicillin and 2-azetidinone base was successfully exploited in the treatment of inflammatory, respiratory, cardiovascular disorders, cancer and other pathologic processes. Availability of X-ray crystallographic data for target enzymes and computational molecular modelling in combination with wide possibilities of structural modifications for commercial natural and synthetic β-lactams and the chiral blocks allow to consider this class of organic compounds as a perspective source of mechanism based nonantibacterial drugs.
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Keywords: a-independent transacylase; nonantibacterial activities; phospholipase a2; synthetic

Document Type: Review Article

Affiliations: Latvian Institute of Organic Synthesis, 21 Aizkraukles Street, Riga, LV 1006, Latvia.

Publication date: 2003-09-01

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