2-(3-Pyridyl)thiazolidine-4-carboxamides. 1. Novel Orally Active Antagonists of Platelet-Activating Factor (PAF).

• NAGAOKA Hitoshi

• HARA Hiromu

• SUZUKI Takeshi

• TAKAHASHI Takumi

• TAKEUCHI Makoto

• MATSUHISA Akira

• SAITO Munetoshi

• YAMADA Toshimitsu

• TOMIOKA Kenichi

• MASE Toshiyasu

Bibliographic Information

Other Title

• 2 3 Pyridyl thiazolidine 4 carboxamides

Abstract

In a search for novel platelet-activating factor (PAF) antagonists, we found that 1-(3-phenylpropyl)-4-[2-(3-pyridyl)thiazolidine-4-carboyl]piperazine (3%) showed in vitro and in vivo PAF-antagonistic activities. Introduction of functional groups at the benzylic methylene carbon of 3x afforded some compounds with more potent PAF-antagonistic activity than 3x. Among them 1-(3-methyl-3-phenylbutyl)-4-[2-(3-pyridyl)thiazolidine-4-carbonyl]-piperazine fumarate (3al, YM264) was found to be one of the most potent PAF antagonists.

Journal

• Chemical and Pharmaceutical Bulletin

  Chemical and Pharmaceutical Bulletin 45 (10), 1659-1664, 1997

  The Pharmaceutical Society of Japan

Keywords

• [2-(3-pyridyl)thiazolidine-4-yl]carboxamide
• PAF antagonist
• structure-activity relationship
• YM264

Details

• CRID: 1390282679141046656
• NII Article ID: 130003773634
• NII Article ID: 110003616417
• NII Book ID: AA00602100
• DOI: 10.1248/cpb.45.1659
• ISSN: 13475223
• ISSN: 00092363
• NDL BIB ID: 4326390
• PubMed: 9353894
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I4326390
• Web Site: http://www.jstage.jst.go.jp/article/cpb1958/45/10/45_10_1659/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/1998066708
• Text Lang: en
• Data Source:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
• Abstract License Flag: Disallowed