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Antibacterial Nicotinamide Adenine Dinucleotide Synthetase Inhibitors:  Amide- and Ether-Linked Tethered Dimers with α-Amino Acid End Groups

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posted on 2007-05-31, 00:00 authored by Sadanandan E. Velu, Liyuan Mou, Chi-Hao Luan, Zhengrong W. Yang, Lawrence J. DeLucas, Christie G. Brouillette, Wayne J. Brouillette
Tethered dimers incorporating natural α-amino acid end groups were synthesized, including examples in which the previously reported esterase-sensitive ester linker was replaced with more stable amide or ether linkers. These compounds remained effective both as inhibitors of NAD synthetase and as potent antibacterial agents for Gram-positive strains. Studies on nonspecific effects, including detergent properties and promiscuous inhibition, suggested little contribution to observed activities.

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