2. Academic Validation
  3. Isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives as potent alpha(4)beta(1) integrin antagonists

Isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives as potent alpha(4)beta(1) integrin antagonists

  • Bioorg Med Chem Lett. 2001 Oct 8;11(19):2593-6. doi: 10.1016/s0960-894x(01)00511-x.
A J Duplantier 1,  G E Beckius,  R J Chambers,  L S Chupak,  T H Jenkinson,  A S Klein,  K G Kraus,  E M Kudlacz,  M W McKechney,  M P Pettersson,  C A Whitney,  A J Milici
Affiliations

Affiliation

  • 1 Pfizer Global Research and Development, Groton Labs, Eastern Point Road, Groton, CT 06340, USA. allen_j_duplantier@groton.pfizer.com
PMID: 11551757 DOI: 10.1016/s0960-894x(01)00511-x
Abstract

A series of isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives derived from LDV was found to be a potent antagonist of the alpha(4)beta(1) Integrin. The synthesis and SAR leading up to 3-[3-(1-[-[3-methoxy-4-(3-o-tolyl-ureido)-phenyl]-acetylamino]-3-methyl-butyl)-isoxazol-5-yl]-propionic acid (22) are reported. In an allergic mouse model, compound 22 was efficacious delivered systemically (58% inhib @ 10 mg/kg, sc) as well as by intra-tracheal instillation (ED(50)=2 microg/kg).

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