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 γ,γ-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, E., Giannessi, F., Brunetti, T., Pessotto, P., Renzulli, M.L., Travagli, M., et al. (2008). Novel Substituted Aminoalkylguanidines as Potential Antihyperglycemic and Food Intake-Reducing Agents. JOURNAL OF MEDICINAL CHEMISTRY, 51(11), 3073-3076 [10.1021/jm8001636].
Novel Substituted Aminoalkylguanidines as Potential Antihyperglycemic and Food Intake-Reducing Agents
Travagli, Massimiliano;Corelli, Federico;Botta, Maurizio
2008-01-01
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 γ,γ-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.
| File | Dimensione | Formato | |
|---|---|---|---|
|
jm8001636.pdf
non disponibili
Tipologia:
Post-print
Licenza:
NON PUBBLICO - Accesso privato/ristretto
Dimensione
136.7 kB
Formato
Adobe PDF
|
136.7 kB | Adobe PDF | Visualizza/Apri Richiedi una copia |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
https://hdl.handle.net/11365/21023
Attenzione
Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo