87629-12-7Relevant academic research and scientific papers
Dipeptidyl peptidase IV inhibitors derived from β-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole
Ashton, Wallace T.,Sisco, Rosemary M.,Dong, Hong,Lyons, Kathryn A.,He, Huaibing,Doss, George A.,Leiting, Barbara,Patel, Reshma A.,Wu, Joseph K.,Marsilio, Frank,Thornberry, Nancy A.,Weber, Ann E.
, p. 2253 - 2258 (2007/10/03)
A series of β-aminoacylpiperidines bearing various fused five-membered heterocyclic rings was synthesized as dipeptidyl peptidase IV inhibitors. Potent and relatively selective inhibition could be obtained, depending on choice of heterocycle, regioisomerism, and substitution. In particular, one analog (74, DPP-IV IC50 = 26 nM) exhibited good oral bioavailability and acceptable half-life in the rat, albeit with rather high clearance.
Synthesis, in Vitro 3H>Prazosin Displacement, and in Vivo Activity of 3-Aryl-4,5,6,7-tetrahydropyrazolopyridines, a New Class of Antihypertensive Agents
Winters, Giorgio,Sala, Alberto,Barone, Domenico,Baldoli, Emiliana
, p. 934 - 940 (2007/10/02)
A series of a new 3-aryl-4,5,6,7-tetrahydropyrazolopyridines was synthesized and screened for in vitro 3H>prazosin displacement activity.The results correlated well with their antihypertensive activity in spontaneous hypertensive rats.
