170687-87-3Relevant academic research and scientific papers
Beta 3 agonists. Part 1: Evolution from inception to BMS-194449
Washburn,Sher,Poss,Girotra,McCann,Gavai,Mikkilineni,Mathur,Cheng,Dejneka,Sun,Wang,Harper,Russell,Slusarchyk,Skwish,Allen,Hillyer,Frohlich,Abboa-Offei,Cap,Waldron,George,Tesfamariam,Ciosek Jr.,Ryono,Young,Dickinson,Seymour,Arbeeny,Gregg
, p. 3035 - 3039 (2001)
Screening of the BMS collection identified 4-hydroxy-3-methylsulfonanilidoethanolamines as full beta 3 agonists. Substitution of the ethanolamine nitrogen with a benzyl group bearing a para hydrogen bond acceptor promoted β3 selectivity. SAR elucidation established that highly selective β3 agonists were generated upon substitution of Cα with either benzyl to form (R)-1,2-diarylethylamines or with aryl to generate 1,1-diarylmethylamines. This latter subset yielded a clinical candidate, BMS-194449 (35).
