J Med Chem. 2008 Jun 12;51(11):3073-6. Epub 2008 May 9.

Novel substituted aminoalkylguanidines as potential antihyperglycemic and food intake-reducing agents.

Tassoni E, Giannessi F, Brunetti T, Pessotto P, Renzulli M, Travagli M, Rajamäki S, Prati S, Dottori S, Corelli F, Cabri W, Carminati P, Botta M.

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Chemistry and Analytical Department, Sigma-Tau SpA, Pomezia, Italy. emanuela.tassoni@sigma-tau.it

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.

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Novel substituted aminoalkylguanidines as potential antihyperglycemic and food i...
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J Med Chem. 2008 Jun 12 ;51(11):3073-6. Epub 2008 May 9 .

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