Mantlo, Nathan B.; Chakravarty, Prasun K.; Ondeyka, Debra L.; Siegl, Peter K. S.; Chang, Raymond S.; Lotti, Victor J.; Faust, Kristie A.; Schorn, Terry W.; Chen, Tsing Bau published the artcile< Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists>, Name: 2-Amino-3-nitro-6-picoline, the main research area is Angiotensin II antagonist tetrazolylbiphenylylimidazopyridine; imidazopyridine tetrazolylbiphenylyl Angiotensin II antagonist; structure activity antihypertensive tetrazolylbiphenylylimidazopyridine.
Several title Angiotensin II (AII) antagonists I (R = Et, Pr, Bu, R1 = R2 = H, Me; R1 = Me, R2 = H; R1 = H, R2 = Me) were prepared Substituents at the 2, 5, and 7-positions of the imidazopyridine have a profound effect on the in vitro binding affinity to AII receptors (rabbit aorta membrane preparation) and on the inhibition of the AII-induced pressor responses in conscious rats. The most active compound, I (R = Et, R1 = R2 = Me) is extremely potent in vitro (IC50 = 0.3 nM, rabbit aorta), and in vivo (ED50 = 0.048 mg/Kg i.v. and 0.026 mg/Kg p.o., conscious rat). This compound is a specific AT1 antagonist, and substantially lowers the blood pressure of high renin hypertensive rats upon oral dosing (0.1 and 0.3 mg/Kg) with a duration of action exceeding 24 h.
Journal of Medicinal Chemistry published new progress about Antihypertensives. 21901-29-1 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Name: 2-Amino-3-nitro-6-picoline.