158. Preparation of analogues of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine as antitubercular agents

The title compds. I or II [R = morpholinyl, thiomorpholinyl, N-methylpiperazinyl, N-isopropylpiperazinyl, N-acetylpiperazinyl, piperidinyl or imidazolyl; R1 = H, substituted Ph, 1-naphthyl; R2 = H, Me, Et, iso-Pr, (un)substituted CH2Ph; if the compd. has a general formula I, X = N and Y = N or CH; if the compd. has a general formula II, X = O, S or N and Y = N or CH; with provisos], useful as antitubercular agents having high activity and low toxicity, were prepd. E.g., a multi-step synthesis of III, starting from Me vinyl ketone and p-tolualdehyde, was given. III showed MIC of 0.4 μg/mL toward M. tuberculosis 103471. The invention concerns the use of the described compds. as antitubercular agents and process to obtain intermediates and final compds.