jm061349l_si_001.pdf (19.69 kB)
Antibacterial Nicotinamide Adenine Dinucleotide Synthetase Inhibitors: Amide- and Ether-Linked Tethered Dimers with α-Amino Acid End Groups
journal contribution
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. BrouilletteTethered 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.