SYNTHESIS AND HYPOTENSIVE ACTIVITY OF PYRIMIDINE-2,4-(1H,3H)-DIONE DERIVATIVES CONTAINING THIETANE RINGS WITH SULFUR IN VARIOUS OXIDATION STATES

Publication date: 2014

Abstract:

Oxo- and dioxothietane derivatives of 6-methyl-1-(thietan-3-yl)pyrimidine-2,4-(1H,3H)-dione were synthesized by oxidation. N-Alkylation and CH-aminomethylation produced 3-alkyl- and 5-aminomethyl-substituted 6-methyl-1-(thietan-3-yl)pyrimidine-2,4-(1H,3H)-dione, 6-methyl-1-(1-oxothietan-3-yl)pyrimidine2,4-(1H,3H)-dione, and 1-(1,1-dioxothietan-3-yl)-6-methylpyrimidine-2,4-(1H,3H)-dione. The synthesized compounds showed hypotensive activity. Compounds causing pronounced, prolonged, and dose-dependent hypotensive effects that were comparable with those of reference drugs nebivolol (2 mg/kg), lisinopril (10 mg/kg), and amlodipine (1 mg/kg) were discovered.

Тип: Article

DOI 10.1007/s11094-014-1126-3