摘要 |
<p>Heterocycles of formula (I) and their acid addition salts are new: In (I) X is N and n is 1 or 2 or X is VH and n is 1. R is H, 1-5C alkylcarbonyl or alkoxycarbonyl, heterocyclylcarbonyl (heterocyclyl is furyl, thienyl, tetrahydrofuryl, pyridyl or 2-methylthio 1,3,4-oxadiazol-5-yl) benzoyl, 3,4,5-trimethoxy cinnamoyl, allyloxycarbonyl, 2-methyl 1-propen-3-yloxycarbonyl, benzyloxycarbonyl or phenoxycarbonyl; R can also be phenylthio provided X is not CH; Ar is 4(7)-benzimidazolyl (opt. 2-substd. by 1-4C alkyl, phenyl or benzyl); 6-purinyl (provided X is not N and H), 4(7)-benzotriazolyl; 7-indolyl; or, when X is N and n is 1, 4-indolyl. (I) are useful as cardiovascular agents, particularly antihypertensives. Typical cpds. have intravenous LD50 in mice 125 mg per kg or more, and can be formulated for daily doses of up to 0.5g.</p> |