title: 1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation.
abstract: During 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 microg/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.
authors: Dipartimento di Chimica e Tecnologie del Farmaco, Università La Sapienza, I-00185 Roma, Italy. mariangela.biava@uniroma1.it
authors: Mariangela
authors: M
authors: Biava
authors: Giulio C
authors: GC
authors: Porretta
authors: Giovanna
authors: G
authors: Poce
authors: Alessandro
authors: A
authors: De Logu
authors: Rita
authors: R
authors: Meleddu
authors: Edda
authors: E
authors: De Rossi
authors: Fabrizio
authors: F
authors: Manetti
authors: Maurizio
authors: M
authors: Botta
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D008958:Models, Molecular; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D021281:Quantitative Structure-Activity Relationship; D014376:Tuberculosis / Q000188:drug therapy*; D014709:Vero Cells
chemical_list: D000995:Antitubercular Agents; D011758:Pyrroles