1,720,992 research outputs found
Derivatives of BM 212: synthesis and biological evaluation of new derivatives with improved antimycobacterial activity.
No full text
Builiding a pharmacophore model for a novel class of antitubercular compounds.
No full textStarting from a set of 32 antitubercular compounds, for the first time a three-dimensional pharmacophore model has been derived through a computational approach based on catalyst software. The model proved to be able to identify compounds belonging to classes of molecules already reported as antitubercular agents
BM212 and its derivatives: lead optimization of a new class of antimycobacterial agents.
No full textPyrrole compounds as inhibitors of mycobacteria, synthesis thereof ans intermediates thereto
No full textThe present invention concerns novel pyrrole compounds, derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine (BM212). The invention concerns the use of the described compounds as antitubercular agents and a process to obtain intermediates and final compounds. The compounds of the invention are found to be more active and much less toxic than previously known compounds
New pyrrole derivatives of BM 212: a new class of antimycobacterial agents.Design, synthesis, biological evaluation and study of their mode of action.
No full text
1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis and microbiological evaluation
No full textDuring the search of novel antitubercular drugs related to BM 212, new diarylpyrroles were designed and synthesized on the basis of a structure–activity relationship analysis of many pyrroles previously described by us. Among them, 1-(4-fluorophenyl)-2-ethyl-3-(thiomorpholin-4-yl)methyl-5-(4-methylphenyl)-1H-pyrrole (2b) proved to be particularly active, with a minimum inhibitory concentration (MIC, expressed as μg/mL) and a protection index (PI) better than or comparable to those of reference compounds. Also the remaining compounds were very active, although their MIC and PI were in general lower than those of their parent 2-methyl analogues
- …
