- Benzylguanidines and other galegine analogues inducing weight loss in mice
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Dimethylallylguanidine, also known as galegine, isolated from Galega officinalis, has been shown to have weight reducing properties in vivo. Substitution of the guanidine group with an N-cyano group and replacement of guanidine with amidine, pyrimidine, pyridine, or the imidazole moieties removed the weight reducing properties when evaluated in BALB/c mice. However, retention of the guanidine and replacement of the dimethylallyl group by a series of functionalized benzyl substituents was shown to exhibit, and in some cases significantly improve, the weight reducing properties of these molecules in BALB/c, ob/ob, and diet induced obesity (DIO) mice models. The lead compound identified, across all models, was 1-(4-chlorobenzyl)guanidine hemisulfate, which gave an average daily weight difference (% from time-matched controls; ± SEM) of -19.7 ± 1.0, -11.0 ± 0.7, and -7.3 ± 0.8 in BALB/c, ob/ob, and DIO models, respectively.
- Coxon, Geoffrey D.,Furman, Brian L.,Harvey, Alan L.,McTavish, John,Mooney, Mark H.,Arastoo, Mahmoud,Kennedy, Alan R.,Tettey, Justice M.,Waigh, Roger D.
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supporting information; experimental part
p. 3457 - 3463
(2010/03/25)
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