Antifungal and/or antiparasitic pharmaceutical composition and novel indole derivatives as active principle of such a composition
The present invention relates to novel indole derivatives, their method of preparation and their pharmacological activity as antimycotic and/or antiparasitic compounds.
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Page/Page column 20
(2010/02/06)
New selective nonsteroidal aromatase inhibitors: Synthesis and inhibitory activity of 2, 3 or 5-(α-azolylbenzyl)-1H-indoles
Six azolyl substituted indoles were synthesized and tested for their activity to inhibit two P450 enzymes: P450 arom and P450 17α. It was observed that the introduction of α-imidazolylbenzyl chain at carbon 3 or 5 on indole nucleus led to very active molecules. Compounds 22, 23 and especially 33 demonstrate very high potential against P450 arom. Under our assay conditions of high substrate concentration the IC50 are 0.057, 0.0785 and 0.041 μM, respectively. These compounds are moderate inhibitors against P450 17α.
Le Borgne, Marc,Marchand, Pascal,Delevoye-Seiller, Benedicte,Robert, Jean-Michel,Le Baut, Guillaume,Hartmann, Rolf W.,Palzer, Martina
p. 333 - 336
(2007/10/03)
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