Title compds. [I; R = morpholino, thiomorpholino, oxane, thioxane, N-methylpiperazinyl, N-isopropylpiperazinyl, N-acetylpiperazinyl, piperidinyl, imidazolyl; R1 = substituted Ph, benzothienyl, benzothiazolyl, etc.; R2 = H, Me, Et, Me2CH, PhCH2, chlorobenzyl, fluorobenzyl, trifluoromethylbenzyl, methoxybenzyl, etc.; R3 = Me, Et, Pr, Me2CH, MeO, BuS, SOMe, SO2NHMe, SO2NMe2, etc.], were prepd. Thus, title compd. N-(4-fluorophenyl)-2-methyl-3-thiomorpholinomethyl-5-(4-methylthiophenyl)pyrrole (prepd. in 3 steps from Me vinyl ketone, 4-methylthiobenzaldehyde, 4-fluoroaniline, thiomorpholine, and H2CO), showed a min. inhibitory concn. of 0.25 μg/mL against M. tuberculosis RMP-R.
Biava, M., Porretta, G., Cesare, ., Pompei, R., Botta, M., Manetti, F., et al. (2009)Preparation of aryl heterocyclylmethyl pyrroles as inhibitors of mycobacteria. . Brevetto No. EP 2045237.
Preparation of aryl heterocyclylmethyl pyrroles as inhibitors of mycobacteria
BOTTA, MAURIZIO;MANETTI, FABRIZIO;
2009-01-01
Abstract
Title compds. [I; R = morpholino, thiomorpholino, oxane, thioxane, N-methylpiperazinyl, N-isopropylpiperazinyl, N-acetylpiperazinyl, piperidinyl, imidazolyl; R1 = substituted Ph, benzothienyl, benzothiazolyl, etc.; R2 = H, Me, Et, Me2CH, PhCH2, chlorobenzyl, fluorobenzyl, trifluoromethylbenzyl, methoxybenzyl, etc.; R3 = Me, Et, Pr, Me2CH, MeO, BuS, SOMe, SO2NHMe, SO2NMe2, etc.], were prepd. Thus, title compd. N-(4-fluorophenyl)-2-methyl-3-thiomorpholinomethyl-5-(4-methylthiophenyl)pyrrole (prepd. in 3 steps from Me vinyl ketone, 4-methylthiobenzaldehyde, 4-fluoroaniline, thiomorpholine, and H2CO), showed a min. inhibitory concn. of 0.25 μg/mL against M. tuberculosis RMP-R.
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https://hdl.handle.net/11365/28200
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