Bioorganic and Medicinal Chemistry Letters p. 6429 - 6436 (2008)
Update date:2022-07-30
Topics: Novel Discovery Agonists Experimental Small molecule
Westaway, Susan M.
Brown, Samantha L.
Conway, Elizabeth
Heightman, Tom D.
Johnson, Christopher N.
Lapsley, Kate
Macdonald, Gregor J.
MacPherson, David T.
Mitchell, Darren J.
Myatt, James W.
Seal, Jon T.
Stanway, Steven J.
Stemp, Geoffrey
Thompson, Mervyn
Celestini, Paolo
Colombo, Andrea
Consonni, Alessandra
Gagliardi, Stefania
Riccaboni, Mauro
Ronzoni, Silvano
Briggs, Michael A.
Matthews, Kim L.
Stevens, Alexander J.
Bolton, Victoria J.
Boyfield, Izzy
Jarvie, Emma M.
Stratton, Sharon C.
Sanger, Gareth J.
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.
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