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Synthesis, in vitro, and in vivo antibacterial activity of nocathiacin I thiol-Michael adducts
Authors:Naidu B Narasimhulu  Sorenson Margaret E  Bronson Joanne J  Pucci Michael J  Clark Junius M  Ueda Yasutsugu
Institution:The Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. b.narasimhulunaidu@bms.com
Abstract:The synthesis and antibacterial activity of a series of nocathiacin I derivatives (4-20) containing polar water solubilizing groups is described. Thiol-Michael adducts containing acidic polar groups have reduced antibacterial activity whereas those with basic polar groups have retained very good antibacterial activity.
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