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Discovery of melanin-concentrating hormone receptor R1 antagonists using high-throughput synthesis.

Abstract：

:A structure-activity study on benzylpiperidine 1 was accomplished by utilizing high-throughput synthesis. Three focused libraries were designed and synthesized to quickly develop SAR. Further optimization led to the discovery of compound 2, an MCH receptor R1 antagonist with over 400-fold improvement in biological activity over the original lead.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Su J,McKittrick BA,Tang H,Czarniecki M,Greenlee WJ,Hawes BE,O'Neill K

doi

10.1016/j.bmc.2004.11.046

subject

Has Abstract

pub_date

2005-03-01 00:00:00

pages

1829-36

issue

5

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(04)00947-2

journal_volume

13

pub_type

杂志文章

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