The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.
Basic Information
ID: ALA1152208
Journal: Bioorg Med Chem Lett
Title: The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.
Authors: Westaway SM, Brown SL, Conway E, Heightman TD, Johnson CN, Lapsley K, Macdonald GJ, MacPherson DT, Mitchell DJ, Myatt JW, Seal JT, Stanway SJ, Stemp G, Thompson M, Celestini P, Colombo A, Consonni A, Gagliardi S, Riccaboni M, Ronzoni S, Briggs MA, Matthews KL, Stevens AJ, Bolton VJ, Boyfield I, Jarvie EM, Stratton SC, Sanger GJ.
Abstract: Optimisation of urea (5), identified from high throughput screening and subsequent array chemistry, has resulted in the identification of pyridine carboxamide (33) which is a potent motilin receptor agonist possessing favourable physicochemical and ADME profiles. Compound (33) has demonstrated prokinetic-like activity both in vitro and in vivo in the rabbit and therefore represents a promising novel small molecule motilin receptor agonist for further evaluation as a gastroprokinetic agent.
CiteXplore: 19006669
DOI: 10.1016/j.bmcl.2008.10.072
Patent ID: ┄