Livingston S J, Smith H J, Sewell R D, Ahmed S
Welsh School of Pharmacy, U.W.C.C., Cardiff, UK.
J Enzyme Inhib. 1992;6(2):165-73. doi: 10.3109/14756369209040748.
A range of penicillins have been examined as competitive reversible inhibitors of enkephalinase (neutral endopeptidase; EC 3.4.24.11). Carfecillin (Ki = 0.18 microM) was the most potent inhibitor in the series, whereas cloxacillin (27.5 microM), ampicillin (41.0 microM), nafcillin (58.7 microM) and carbenicillin (158 microM) had moderate potency and benzyl penicillin (885 microM), mezlocillin (473 microM) and azlocillin (556 microM) were weak inhibitors. Structure-activity relationships within the series have been rationalised from a consideration of molecular graphics analysis of the match between receptor binding groups with thiorphan as well as log P values.
一系列青霉素已被作为脑啡肽酶（中性内肽酶；EC 3.4.24.11）的竞争性可逆抑制剂进行了研究。羧苄青霉素（Ki = 0.18微摩尔）是该系列中最有效的抑制剂，而氯唑西林（27.5微摩尔）、氨苄西林（41.0微摩尔）、萘夫西林（58.7微摩尔）和羧苄青霉素（158微摩尔）具有中等效力，苄青霉素（885微摩尔）、美洛西林（473微摩尔）和阿洛西林（556微摩尔）是弱抑制剂。从受体结合基团与硫醚啡的匹配以及log P值的分子图形分析考虑，该系列内的构效关系已得到合理说明。
