Baldwin, John J.; Christy, Marcia E.; Denny, George H.; Habecker, Charles N.; Freedman, Mark B.; Lyle, Paulette A.; Ponticello, Gerald S.; Varga, Sandor L.; Gross, Dennis M.; Sweet, Charles S. published the artcile< 尾1-Selective adrenoceptor antagonists: examples of the 2-[4-[3-(substituted amino)-2-hydroxypropoxy]phenyl]imidazole class. II>, SDS of cas: 112-63-0, the main research area is imidazole aminohydroxypropoxyphenyl; aminohydroxypropoxyphenylimidazole preparation adrenoceptor antagonist.
An attempt to develop a highly cardioselective 尾-adrenoceptor antagonist devoid of intrinsic sympathetic activity (ISA) focused on exploring structure-activity relationships around imidazole (S)-I (R = 2-thienyl, X = bond). Strategies to reduce or eliminate ISA centered on structural changes that could influence activation of the receptor by the drug itself or by a metabolite. The approaches involved eliminating the acidic imidazole N-H proton, incorporating substituents ortho to the 尾-adrenergic blocking side chain, increasing steric bulk around the N-H moiety, decreasing lipophilicity, introducing intramol. hydrogen bonding involving the imidazole N-H, and displacing the imidazole ring from an activating position by the incorporation of a spacer element. The compounds were investigated in vitro for 尾-adrenoceptor antagonism and in vivo for ISA. From these studies, the most successful variation involved the insertion of a spacer between the imidazole and aryl rings. (S)-I.HCl (R = MeCO, X = CH2) was highly cardioselective (dose ratio 尾2/尾1 > 9333) and devoid of ISA.
Journal of Medicinal Chemistry published new progress about 尾1-Adrenoceptor antagonists. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, SDS of cas: 112-63-0.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics