Synthesis and antihypertensive activity of some thienylethanolamines.
Synthesis of a series of thienylethanolamines having varying substituents on the thiophene ring and on the nitrogen atom is described using the general procedure reported earlier. In the determination of their pharmacological profile, some of the derivatives showed marked antihypertensive activity in the spontaneously hypertensive rat model. Tests are also reported which demonstrated that some of these derivatives antagonized alpha- and/or beta-adrenoreceptor activities. The ability of this class of compounds to inhibit catecholamine-induced release of free fatty acids by adipose tissue was demonstrated. Structure-activity relationships in different tests were also determined.
D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis*; D001794:Blood Pressure / Q000187:drug effects; D004983:Ethanolamines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D006973:Hypertension / Q000188:drug therapy; D050356:Lipid Metabolism; D008297:Male; D051379:Mice; D009206:Myocardium / Q000378:metabolism; D009638:Norepinephrine / Q000378:metabolism; D051381:Rats; D013876:Thiophenes / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use
D000959:Antihypertensive Agents; D004983:Ethanolamines; D013876:Thiophenes; D009638:Norepinephrine