Conformationally restricted analogs of deoxynegamycin

…, S Gu, P Herradura, H O'Dowd, B Kim, M Gomez…

Index: Raju; Anandan, Sampathkumar; Gu, Shihai; Herradura, Prudencio; O'Dowd, Hardwin; Kim, Bum; Gomez, Marcela; Hackbarth, Corinne; Wu, Charlotte; Wang, Wen; Yuan, Zhengyu; White, Richard; Trias, Joaquim; Patel, Dinesh V. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 12 p. 3103 - 3107

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Citation Number: 15

Abstract

Deoxynegamycin (1b) is a protein synthesis inhibitor with activity against Gram-negative (GN) bacteria. A series of conformationally restricted analogs were synthesized to probe its bioactive conformation. Indeed, some of the constrained analogs were found to be equal or better than deoxynegamycin in protein synthesis assay (1b, IC50= 8.2 μM; 44, IC50= 6.6 μM; 35e2, IC50= 1μM). However, deoxynegamycin had the best in vitro whole cell ...