Pharmacochemistry of the furoxan ring: recent developments.
In the present work recent results obtained in the pharmacochemistry of the furoxan system are reported. In particular, after a brief description of the salient points of the furoxan chemistry, the synthesis and the properties of a series of Nifedipine and Prazosin analogues, containing this heterocyclic system, are described. Since we observed that a few furoxan derivatives are able to elicit both a dose-dependent rise in platelet cGMP levels and to promote a dose-dependent inhibition of AA-induced [Ca++] rise, and that many substituted furoxans show potent vasodilating and antiaggregatory activity, the possibility of using the furoxan system as a lead in the design of new vasodilators is also discussed.
Dipartimento di Scienza e Technologia del Farmaco, Università di Torino, Italy.
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Calvino
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Fruttero
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Gasco
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Sorba
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D000818:Animals; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000494:pharmacology; D006152:Cyclic GMP / Q000097:blood; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D009200:Myocardial Contraction / Q000187:drug effects; D009543:Nifedipine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D010069:Oxadiazoles / Q000737:chemistry / Q000494:pharmacology*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D011224:Prazosin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D014665:Vasodilator Agents / Q000138:chemical synthesis / Q000494:pharmacology
D002121:Calcium Channel Blockers; D010069:Oxadiazoles; D010975:Platelet Aggregation Inhibitors; D014665:Vasodilator Agents; C010166:furoxans; D006152:Cyclic GMP; D009543:Nifedipine; D011224:Prazosin