Siemann Stefan, Evanoff Darryl P, Marrone Laura, Clarke Anthony J, Viswanatha Thammaiah, Dmitrienko Gary I
Department of Chemistry, University of Waterloo, 200 University Avenue W., Waterloo, Ontario N2L 3G1, Canada.
Antimicrob Agents Chemother. 2002 Aug;46(8):2450-7. doi: 10.1128/AAC.46.8.2450-2457.2002.
Members of a family of N-arylsulfonyl hydrazones have been identified as novel inhibitors of IMP-1, a metallo-beta-lactamase of increasing prevalence. Structure-activity relationship studies have indicated a requirement for bulky aromatic substituents on each side of the sulfonyl hydrazone backbone for these compounds to serve as efficient inhibitors of IMP-1. Molecular modeling has provided insight into the structural basis for the anti-metallo-beta-lactamase activity exhibited by this class of compounds.
N-芳基磺酰腙家族的成员已被鉴定为IMP-1的新型抑制剂,IMP-1是一种越来越普遍的金属β-内酰胺酶。构效关系研究表明,对于这些化合物作为IMP-1的有效抑制剂而言,磺酰腙主链两侧需要有庞大的芳族取代基。分子建模为这类化合物所表现出的抗金属β-内酰胺酶活性的结构基础提供了深入了解。