Design, synthesis and stability of N-acyloxymethyl- and N-aminocarbonyloxymethyl-2-azetidinones as human leukocyte elastase inhibitors

被引：51

作者：

Clemente, A

Domingos, A

Grancho, AP

Iley, J

Moreira, R

Neres, J

Palma, N

Santana, AB

Valente, E

机构：

[1] Univ Lisbon, Fac Farm, CECF, P-1600 Lisbon, Portugal

[2] INETI, Dept Biotecnol, Estrada Palmeiras, P-1649 Lisbon, Portugal

[3] Open Univ, Dept Chem, Milton Keynes MK7 6AA, Bucks, England

[4] Univ Nova Lisboa, Ctr Quim Fina & Biotecnol, P-2825 Monte De Caparica, Portugal

[5] Inst Super Ciencias Saude Sul, P-2829 Monte De Caparica, Portugal

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(01)00131-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of N-acyloxymethyl- and N-aminocarbonyloxymethyl derivatives of 2-azetidinones. 3, with different substituent patterns at the beta -lactam C-3 and C-4 positions, were designed as potential mechanism-based inhibitors for human leukocyte elastase and found to exhibit inhibitory potency and selectivity for the enzyme, (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1065 / 1068

页数：4

共 23 条

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