期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 51, 期 18, 页码 5736-5744出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm800570q
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资金
- Polish Ministry of Science and Higher Education [2 P04B 00729]
- Polish-Greek Scientific and Technological International Cooperation
- Polish Science
A new group of organophosphorus inhibitors of urease, P-methyl phosphinic acids was discovered by using the structure based inhibitor design approach. Several derivatives of the lead compound, aminomethyl(P-methyl)phosphinic acid, were synthesized successfully. Their potency was evaluated in vitro against urease from Bacillus pasteurii and Proteus vulgaris. The studied compounds constitute a group of competitive, reversible inhibitors of bacterial ureases. Obtained thiophosphinic analogues of the most effective structures exhibited kinetic characteristics of potent, slow binding urease inhibitors, with K-i = 170 nM (against B. pasteurii enzyme) for the most active N-(N'-benzyloxycarbonylglycyl)aminomethyl(P-methyl)phosphinothioic acid.
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