| Abstrakt: |
Oxo- and dioxothietane derivatives of 6-methyl-1-(thietan-3-yl)pyrimidine-2,4-(1 H,3 H)-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-(1 H,3 H)-dione, 6-methyl-1-(1-oxothietan-3-yl)pyrimidine-2,4-(1 H,3 H)-dione, and 1-(1,1-dioxothietan-3-yl)-6-methylpyrimidine-2,4-(1 H,3 H)-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. [ABSTRACT FROM AUTHOR] |
