title: Novel substituted aminoalkylguanidines as potential antihyperglycemic and food intake-reducing agents.
abstract: We report the synthesis and evaluation of aminoalkylguanidine analogues and derivatives in C57BL/KsJ db/db diabetic mice, following identification by random screening of 1a and 1b as potential antihyperglycemics and/or modulators of food intake. These compounds are related to galegine, a gamma,gamma-dimethylallylguanidine. Between the newly identified compounds, 1h N-(cyclopropylmethyl)- N'-(4-(aminomethyl)cyclohexylmethyl)guanidine showed the most balanced activity as antihyperglycemic and food intake-reducing agent.
authors.affiliation: Chemistry and Analytical Department, Sigma-Tau SpA, Pomezia, Italy. emanuela.tassoni@sigma-tau.it
authors.forename: Emanuela
authors.initials: E
authors.lastname: Tassoni
authors.forename: Fabio
authors.initials: F
authors.lastname: Giannessi
authors.forename: Tiziana
authors.initials: T
authors.lastname: Brunetti
authors.forename: Pompeo
authors.initials: P
authors.lastname: Pessotto
authors.forename: Michela
authors.initials: M
authors.lastname: Renzulli
authors.forename: Massimiliano
authors.initials: M
authors.lastname: Travagli
authors.forename: Suvi
authors.initials: S
authors.lastname: Rajamäki
authors.forename: Samanta
authors.initials: S
authors.lastname: Prati
authors.forename: Secondo
authors.initials: S
authors.lastname: Dottori
authors.forename: Federico
authors.initials: F
authors.lastname: Corelli
authors.forename: Walter
authors.initials: W
authors.lastname: Cabri
authors.forename: Paolo
authors.initials: P
authors.lastname: Carminati
authors.forename: Maurizio
authors.initials: M
authors.lastname: Botta
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004326:Drinking / Q000187:drug effects; D004435:Eating / Q000187:drug effects*; D006146:Guanidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D008810:Mice, Inbred C57BL; D013329:Structure-Activity Relationship
chemical_list: D019440:Anti-Obesity Agents; D006146:Guanidines; D007004:Hypoglycemic Agents; C530300:N-(cyclopropylmethyl)-N'-(4-(aminomethyl)cyclohexylmethyl)guanidine