反式-5-氧代-六氢-吡咯并[3,2 - b]吡咯和反式-5-氧代-六氢-呋喃并[3,2 - b]吡咯（吡咯烷反式内酰胺和反式内酯）的合成：用于弹性蛋白酶抑制的新药效基团。 - Suppr

Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.

作者信息

Macdonald S J, Belton D J, Buckley D M, Spooner J E, Anson M S, Harrison L A, Mills K, Upton R J, Dowle M D, Smith R A, Molloy C R, Risley C

机构信息

Enzyme Chemistry 2, Development Chemistry 3, Physical Sciences, and Enzyme Pharmacology, GlaxoWellcome Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, U.K.

出版信息

J Med Chem. 1998 Oct 8;41(21):3919-22. doi: 10.1021/jm981026s.

DOI:10.1021/jm981026s

PMID:9767628

Abstract

摘要

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Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.反式-5-氧代-六氢-吡咯并[3,2 - b]吡咯和反式-5-氧代-六氢-呋喃并[3,2 - b]吡咯（吡咯烷反式内酰胺和反式内酯）的合成：用于弹性蛋白酶抑制的新药效基团。

J Med Chem. 1998 Oct 8;41(21):3919-22. doi: 10.1021/jm981026s.

Design and synthesis of pyrrolidine-5,5-trans-lactams (5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 1. The alpha-methyl-trans-lactam template.吡咯烷-5,5-反式内酰胺（5-氧代-六氢-吡咯并[3,2-b]吡咯）作为人巨细胞病毒蛋白酶新型基于机制的抑制剂的设计与合成。1. α-甲基-反式内酰胺模板。

J Med Chem. 2000 Nov 16;43(23):4452-64. doi: 10.1021/jm000078q.

4-Oxo-beta-lactams (azetidine-2,4-diones) are potent and selective inhibitors of human leukocyte elastase.4-氧代-β-内酰胺（氮杂环丁烷-2,4-二酮）是人类白细胞弹性蛋白酶的有效且选择性抑制剂。

J Med Chem. 2010 Jan 14;53(1):241-53. doi: 10.1021/jm901082k.

5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.含5,5-反式内酯的丝氨酸蛋白酶抑制剂：一种新型酰化凝血酶抑制剂的鉴定

Bioorg Med Chem Lett. 1998 Nov 3;8(21):2955-60. doi: 10.1016/S0960-894X(98)00531-9.

Design and synthesis of pyrrolidine-5,5'-trans-lactams (5-oxo-hexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 4. Antiviral activity and plasma stability.吡咯烷-5,5'-反式内酰胺（5-氧代-六氢吡咯并[3,2 - b]吡咯）作为人巨细胞病毒蛋白酶新型基于机制的抑制剂的设计与合成。4. 抗病毒活性和血浆稳定性。

J Med Chem. 2003 Oct 9;46(21):4428-49. doi: 10.1021/jm030810w.

Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151).发现更多吡咯烷转内酰胺作为人中性粒细胞弹性蛋白酶（HNE）抑制剂的潜在开发候选物以及HNE与一种抑制剂（GW475151）复合的晶体结构。

J Med Chem. 2002 Aug 29;45(18):3878-90. doi: 10.1021/jm020881f.

Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams.口服活性吡咯烷反式内酰胺对人中性粒细胞弹性蛋白酶的细胞内抑制作用

Bioorg Med Chem Lett. 2001 Jan 22;11(2):243-6. doi: 10.1016/s0960-894x(00)00632-6.

4-alkylidene-azetidin-2-ones: novel inhibitors of leukocyte elastase and gelatinase.4-亚烷基氮杂环丁烷-2-酮：新型白细胞弹性蛋白酶和明胶酶抑制剂。

Bioorg Med Chem. 2003 Dec 1;11(24):5391-9. doi: 10.1016/j.bmc.2003.09.035.

5,5-Fused thiophene gamma-lactams as templates for serine protease inhibition.5,5-稠合噻吩γ-内酰胺作为丝氨酸蛋白酶抑制的模板

Chem Commun (Camb). 2002 Jun 21(12):1274-5. doi: 10.1039/b111627d.

Synthesis and mechanism of action of novel thiocarbamate inhibitors of human leukocyte elastase.

J Enzyme Inhib. 2000;15(1):63-77.

引用本文的文献

Thiophene-fused γ-lactams inhibit the SARS-CoV-2 main protease reversible covalent acylation.噻吩稠合γ-内酰胺抑制严重急性呼吸综合征冠状病毒2主蛋白酶的可逆共价酰化作用。

Chem Sci. 2024 Apr 16;15(20):7667-7678. doi: 10.1039/d4sc01027b. eCollection 2024 May 22.

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Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.

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