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)
Preparation and pharmacological profile of 7-(α-azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors
Aromatase (P450 arom) is a target of pharmacological interest for the treatment of breast cancer. New series of 7-(α-azolylbenzyl)-1H-indoles and indolines were synthesized as non-steroidal inhibitors of P450 arom. Selectivity was studied towards P450 17α enzyme. The most active compound, 1-ethyl-7-[(imidazol-1-yl)(4-chlorophenyl)methyl]-1H-indole 12c exhibited promising relative potency (rp) of 336 (rp of aminoglutethimide=1) and most of the described azoles were active and selective towards P450 arom.
Marchand, Pascal,Le Borgne, Marc,Palzer, Martina,Le Baut, Guillaume,Hartmann, Rolf W.
p. 1553 - 1555
(2007/10/03)
Process for the production of 7-acylindoles
A process for the production of 7-acylindoles of the general formula: STR1 starting from indoline of the formula: STR2 Indoline is cyanized in a first stage to 7-cyanoindoline of the formula: STR3 The latter is catalytically dehydrogenated in a second stage to 7-cyanindole of the formula: STR4 The latter is then acylated in a third stage with an organometallic compound of the formula: into the end product according to formula I.
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(2008/06/13)
Antiinflammatory agents. 3. Synthesis and pharmacological evaluation of 2-amino-3-benzoylphenylacetic acid and analogues
A series of substituted derivatives of 2-amino-3-benzoylphenylacetic acid (amfenac) has been synthesized and evaluated for antiinflammatory, analgesic, and cyclooxygenase inhibiting activity. Several derivatives including 4'-chloro, 4'-bromo and 5-chloro, 4'-bromo were more potent than indomethacin in these assays.