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ID: ALA1139679
Journal: Bioorg Med Chem Lett
Title: Design of inhibitors against guanase: synthesis and biochemical evaluation of analogues of azepinomycin.
Authors: Ujjinamatada RK, Bhan A, Hosmane RS.
Abstract: As part of a program to design rational, mechanism-based inhibitors of guanase, we report here the synthesis and biochemical screening of two analogues of azepinomycin (1 and 2), a naturally occurring inhibitor of guanase, known to mimic the transition-state of the enzyme-catalyzed reaction. Our biochemical results show that compounds 1 and 2 are competitive inhibitors with K(i) of 2.01+/-0.16 x 10(-5) and 5.36+/-0.14 x 10(-5) M, respectively.
CiteXplore: 16920357