title: Synthesis, biological evaluation and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis.
abstract: As a continuation of our previous work that turned toward the identification of antimycobacterial compounds with innovative structures, two series of pyrazole derivatives were synthesized by parallel solution-phase synthesis and were assayed as inhibitors of Mycobacterium tuberculosis (MTB), which is the causative agent of tuberculosis. One of these compounds showed high activity against MTB (MIC = 4 microg/mL). The newly synthesized pyrazoles were also computationally investigated to analyze their fit properties to the pharmacophoric model for antitubercular compounds previously built by us and to refine structure-activity relationship analysis.
authors.affiliation: Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Via Aldo Moro, 53100 Siena, Italy.
authors.forename: Daniele
authors.initials: D
authors.lastname: Castagnolo
authors.forename: Alessandro
authors.initials: A
authors.lastname: De Logu
authors.forename: Marco
authors.initials: M
authors.lastname: Radi
authors.forename: Beatrice
authors.initials: B
authors.lastname: Bechi
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Manetti
authors.forename: Matteo
authors.initials: M
authors.lastname: Magnani
authors.forename: Sibilla
authors.initials: S
authors.lastname: Supino
authors.forename: Rita
authors.initials: R
authors.lastname: Meleddu
authors.forename: Lorenza
authors.initials: L
authors.lastname: Chisu
authors.forename: Maurizio
authors.initials: M
authors.lastname: Botta