The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.

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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

The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.

Bioorg Med Chem Lett. 2008 Dec 15;18(24):6429-36. doi: 10.1016/j.bmcl.2008.10.072. Epub 2008 Oct 19.

PubMed ID
19006669 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
ErythromycinMotilin receptorEC 50 (nM)50.12N/AN/ADetails
ErythromycinMotilin receptorEC 50 (nM)630.96N/AN/ADetails