N-and C-terminal modifications of negamycin

B Raju, K Mortell, S Anandan, H O'Dowd, H Gao…

Index: Raju; Mortell, Kathleen; Anandan, Sampathkumar; O'Dowd, Hardwin; Gao, Hongwu; Gomez, Marcela; Hackbarth, Corinne; Wu, Charlotte; Wang, Wen; Yuan, Zhengyu; White, Richard; Trias, Joaquim; Patel, Dinesh V. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 14 p. 2413 - 2418

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Citation Number: 32

Abstract

Negamycin 1 is a bactericidal antibiotic with activity against Gram-negative bacteria, and served as a template in an antibiotic discovery program. An orthogonally protected β-amino acid derivative 3a was synthesized and used in parallel synthesis of negamycin derivatives on solid support. This advanced intermediate was also used for N-and C-terminal modifications using solution-phase methodologies. The N-terminal modifications have ...