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Mannich Ketones as Possible Antimycobacterial Agents
Author(s) -
Lutz Zsolt,
Orbán Katalin,
Bóna Ágnes,
Márk László,
Maász Gábor,
Prókai László,
Seress Lázló,
Lóránd Tamás
Publication year - 2017
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201700102
Subject(s) - antimycobacterial , chemistry , isoniazid , mode of action , antibacterial agent , mycobacterium tuberculosis , mass spectrometry , mechanism of action , minimum inhibitory concentration , stereochemistry , chromatography , combinatorial chemistry , antimicrobial , biochemistry , organic chemistry , in vitro , tuberculosis , antibiotics , medicine , pathology
Twenty‐three known unsaturated and fused Mannich ketones and their reduced derivatives (amino alcohols) were selected for an antituberculotic study. They were screened against several mycobacterial strains including Mycobacterium tuberculosis , M. xenopi , and M. gordonae , and minimum inhibitory concentration values were also determined using the standard antituberculotic drug isoniazid (INH) as a reference. Structure–activity relationships were also studied. The mode of action of the test compounds was investigated using transmission electron microscopy, high‐performance liquid chromatography, and matrix‐assisted desorption/ionization mass spectrometry. Several test substances proved to be as potent as INH, but their antimycobacterial spectra were broader than that of INH. Our findings suggest that their mode of action is probably through the inhibition of mycobacterial cell wall biosynthesis.