Literature DB >> 15893024

Development of a prostaglandin D2 receptor antagonist: discovery of a new chemical lead.

Kazuhiko Torisu1, Kaoru Kobayashi, Maki Iwahashi, Hiromu Egashira, Yoshihiko Nakai, Yutaka Okada, Fumio Nanbu, Shuichi Ohuchida, Hisao Nakai, Masaaki Toda.   

Abstract

A series of N-(p-alkoxy)benzoyl-5-methoxy-2-methylindole-3-acetic acids and N-(p-butoxy)benzoyl-2-methylindole-4-acetic acid were discovered as new chemical leads for a prostaglandin D2 (PGD2) receptor antagonist. Most of them exhibited PGD2 receptor binding and blocked cyclic adenosine 3',5'-monophosphate (cAMP) formation in vitro. In particular, 2-methylindole-4-acetic acid analog 1 showed markedly increased receptor affinity and cAMP antagonist activity. Chemistry and structure activity relationship (SAR) data are also presented.

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Year:  2005        PMID: 15893024     DOI: 10.1016/j.ejmech.2004.11.011

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  3 in total

1.  Lipocalin-type prostaglandin D synthase produces prostaglandin D2 involved in regulation of physiological sleep.

Authors:  Wei-Min Qu; Zhi-Li Huang; Xin-Hong Xu; Kosuke Aritake; Naomi Eguchi; Fumio Nambu; Shu Narumiya; Yoshihiro Urade; Osamu Hayaishi
Journal:  Proc Natl Acad Sci U S A       Date:  2006-11-08       Impact factor: 11.205

Review 2.  Prostanoid receptor antagonists: development strategies and therapeutic applications.

Authors:  R L Jones; M A Giembycz; D F Woodward
Journal:  Br J Pharmacol       Date:  2009-07-15       Impact factor: 8.739

3.  Straightforward protocol for the efficient synthesis of varied N(1)-acylated (aza)indole 2-/3-alkanoic acids and esters: optimization and scale-up.

Authors:  Andy J Liedtke; Kwangho Kim; Donald F Stec; Gary A Sulikowski; Lawrence J Marnett
Journal:  Tetrahedron       Date:  2012-12-02       Impact factor: 2.457

  3 in total

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