Natural and synthetic geiparvarins are strong and selective MAO-B inhibitors. Synthesis and SAR studies

被引：86

作者：

Carotti, A

Carrieri, A

Chimichi, S

Boccalini, M

Cosimelli, B

Gnerre, C

Carotti, A

Carrupt, PA

Testa, B

机构：

[1] Dipartimento Farmaco Chim, I-70125 Bari, Italy

[2] Dipartimento Chim Organ U Schiff, I-50019 Sesto Fiorentino, Firenze, Italy

[3] Dipartimento Chim Organ A Mangini, I-40127 Bologna, Italy

[4] Univ Lausanne, Inst Chim Therapeut, CH-1015 Lausanne, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(02)00798-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Natural geiparvarin 1 and a number of its analogues were prepared and tested as inhibitors of both monoamine oxidase isoforms, MAO-B and MAO-A. The desmethyl congener 6 of geiparvarin, proved potent and selective MAO-B inhibitor (PIC50 = 7.55 vs 4.62). X-ray crystallography and molecular modelling studies helped the understanding of the observed structure-activity relationships. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：3551 / 3555

页数：5

共 33 条

[1] QUANTITATIVE STRUCTURE METABOLISM RELATIONSHIP ANALYSES OF MAO-MEDIATED TOXICATION OF 1-METHYL-4-PHENYL-1,2,3,6-TETRAHYDROPYRIDINE AND ANALOGS [J].