Novel substituted aminoalkylguanidines as potential antihyperglycemic and food intake-reducing agents.
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.
Tassoni
Emanuela
E
Chemistry and Analytical Department, Sigma-Tau SpA, Pomezia, Italy. emanuela.tassoni@sigma-tau.it
Giannessi
Fabio
F
Brunetti
Tiziana
T
Pessotto
Pompeo
P
Renzulli
Michela
M
Travagli
Massimiliano
M
Rajamäki
Suvi
S
Prati
Samanta
S
Dottori
Secondo
S
Corelli
Federico
F
Cabri
Walter
W
Carminati
Paolo
P
Botta
Maurizio
M
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
D019440:Anti-Obesity Agents; D006146:Guanidines; D007004:Hypoglycemic Agents; C530300:N-(cyclopropylmethyl)-N'-(4-(aminomethyl)cyclohexylmethyl)guanidine