Synthesis and biological evaluation of triazepane derivatives as DPP-IV inhibitors

…, KY Kim, S Dal Rhee, MA Bae, B Narsaiah…

Index: Park, Woul Seong; Jun, Mi Ae; Shin, Mi Sik; Kwon, Sung Wook; Kang, Seung Kyu; Kim, Ki Young; Dal Rhee, Sang; Bae, Myung Ae; Narsaiah, Banda; Lee, Duck Hyung; Cheon, Hyae Gyeong; Ahn, Jin Hee; Kim, Sung Soo Journal of Fluorine Chemistry, 2009 , vol. 130, # 11 p. 1001 - 1010

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Citation Number: 9

Abstract

A series of triazepane derivatives such as (R)-3-amino-1-(1, 2, 5-triazepan-1-yl)-4-(2, 4, 5- trifluorophenyl) butan-1-ones (7, 13a–p) and (R)-3-amino-1-(1, 2, 5-triazepan-5-yl)-4-(2, 4, 5- trifluorophenyl) butan-1-ones (17a–e) was synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV (DPP-IV) enzyme. Compounds with the acid moiety were found to be potent inhibitors of DPP-IV without inhibiting CYP 3A4. Among them, ...