Indolizines II: search for potential oral hypoglycemic agents.
A few 1,2-bis(N-alkylaminomethyl)indolizines, simple indolizinecarboxylic acids, and several 6-alkoxyindolizine-2-carboxylic acids were synthesized and screened as possible oral hypoglycemic agents. The absence of any significant hypoglycemic activity excludes these compounds from the predicted structural lead provided by some hypoglycemic Vinca alkaloids, such as vincamine, vindoline, and vindolinine, having the indolizine ring as one structural component. But an extension of the rationale that indolizines are also the structural components of some carcinolytic Vinca alkaloids, such as vincristine and vinblastine, used in cancer chemotherapy provided encouraging results. One indolizine derivative showed significant antineoplastic activity in Ehrlich ascites carcinoma.
D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use; D001786:Blood Glucose; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy; D003864:Depression, Chemical; D006863:Hydrogen-Ion Concentration; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D007212:Indolizines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D051381:Rats; D014044:Tolbutamide / Q000494:pharmacology; D014748:Vinca Alkaloids
D000970:Antineoplastic Agents; D001786:Blood Glucose; D007004:Hypoglycemic Agents; D007212:Indolizines; D014748:Vinca Alkaloids; D014044:Tolbutamide