Poce, Giovanna; Cocozza, Martina; Alfonso, Salvatore; Consalvi, Sara; Venditti, Giulia; Fernandez-Menendez, Raquel; Bates, Robert H.; Barros Aguirre, David; Ballell, Lluis; De Logu, Alessandro; Vistoli, Giulio; Biava, Mariangela published the artcile< In vivo potent BM635 analogue with improved drug-like properties>, COA of Formula: C6H13NO, the main research area is pyrrolyl methanamine preparation antimycobacterial antitumor human SAR docking pharmacokinetics; Anti-mycobacterials; Drug discovery; MmpL3; Pyrroles; Tuberculosis.
Herein an efficient method was reported for the design, synthesis, biol. evaluation, pharmacokinetic anal. as well as in vivo TB mouse efficacy studies of novel (2-methyl-1H-pyrrol-3-yl)methanamines I [R = Me, 4-i-PrC6H4, 4-F3CC6H4, etc.; R1 = i-Pr, cyclohexyl, 4-FC6H4, etc.; R2 = 4-morpholinyl, 3-hydroxy-1-piperidyl, 3-methoxy-1-piperidyl] from 2-methyl-1H-pyrroles, formaldehyde and amines under Mannich reaction conditions. These BM635 analogs I showed improved physicochem. properties and excellent antimycobacterial activity. This hit-to-lead campaign led to the identification of a new compound I [R = 4-i-PrC6H4, R1 = i-Pr, R2 = 4-morpholinyl] that showed excellent activity (MIC = 0.15 μM; SI = 133) against drug-sensitive Mycobacterium tuberculosis strains as well as efficacy in a murine model of TB infection.
European Journal of Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 6850-39-1 belongs to class alcohols-buliding-blocks, and the molecular formula is C6H13NO, COA of Formula: C6H13NO.
Referemce:
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Alcohols – Chemistry LibreTexts