Synthesis and pharmacological evaluation of 4a-methyl-4,4a,5,6-tetrahydrothieno[2,3-h]cinnolin-3(2H)-ones.
A number of 4a-methyl-4,4a,5,6-tetrahydrothieno[2,3-h]cinnolin-3(2H)-one s (3-5) have been synthesized and tested for their pharmacological profile. These were compared with the 8-acetylamino-4, 4a,5,6-tetrahydrobenzo[h]cinnolin-3(2H)one 1 which we reported to be a potent antihypertensive agent. In vivo tests indicated that 3 displayed lower even if still significant levels of antihypertensive activity in respect to the lead compound, while all the new derivatives exhibited lower hypotensive activity. Tricyclic thienocinnolinones 3-5 demonstrated fairly potent plateled antiaggregatory activity.
Pinna
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Istituto di Chimica Farmaceutica e Tossicologica, Sassari.
Salis
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E
Berta
D
D
Gavini
E
E
D'Amico
M
M
D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D010974:Platelet Aggregation / Q000187:drug effects; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011918:Rats, Inbred SHR; D017207:Rats, Sprague-Dawley; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology
D000959:Antihypertensive Agents; D011724:Pyridazines; D013764:Tetrahydronaphthalenes