Synthesis and antidiarrheal activity of N-(aminoiminomethyl)-1H-pyrrole-1-acetamides related to guanfacine.
A series of N-(aminoiminomethyl)-1H-pyrrole-1-acetamides, related to guanfacine, were prepared and tested for antidiarrheal activity in castor oil dosed rats. trans-N-(Aminoiminomethyl)-2,5-dihydro-2,5-dimethyl-1H-pyrrole-1-acetami de (2), in which the dichlorophenyl ring of guanfacine is replaced by 2,5-dimethyl-2,5-dihydropyrrole, showed potent antidiarrheal activity but possessed only minimal cardiovascular activity in rats.
D000818:Animals; D002319:Cardiovascular System / Q000187:drug effects; D002368:Castor Oil; D055598:Chemical Phenomena; D002621:Chemistry; D003967:Diarrhea / Q000139:chemically induced / Q000188:drug therapy*; D005260:Female; D016316:Guanfacine; D006146:Guanidines / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D008297:Male; D010648:Phenylacetates; D011758:Pyrroles / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D006146:Guanidines; D010648:Phenylacetates; D011758:Pyrroles; D016316:Guanfacine; D002368:Castor Oil