| 摘要 |
<p>3-A-imino-1,5,10,10a-thiazolo (3,4-b)-isoquinoline derivs. of formula (I), in the (S) or (R,S) form or their mixts. are new, (where A is 8-isoquinolyl, 3-methyl-8-isoquinolyl, 3-hydroxymethyl-5-isoquinolyl, 3-carboxymethyl-5-isoquinolyl, 5-quinolyl, thienopyridyl, benzimidazolyl, thienyl, thiazolyl, 4- (or 5)-carboxyalkyl-2-thiazolyl (where the alkyl part is opt. branched, 1-4C), 1,3,4-thiadiazol-2-yl, pyrazolyl, imidazoyl, pyrimidinyl, pyridazinyl or pyrazinyl. The monocyclic heterocyclics may be substd. by an opt. branched, 1-4C alkyl. When A is other than thienyl, acid addn. salts are included and when A contains a carboxy gp., metallic salts and salts with nitrogen-containing bases are included). (I) have antiviral activity and are esp. active against rhinoviruses. In MRC-5 human fibroblast cellular cultures infected with human IB rhinovirus (strain R1112) the cpds. has a MICof0.016-30micrograms/mlandamax.non-cytotoxicconcn.of M-125 micrograms/ml. Some of the cpds. have analgesic, anti-pyretic and antiinflammatory activity (20-200 mg/kg). The oral LD50 in mice is 300-900 or more mg/kg.</p> |
