New antituberculotics originated from salicylanilides with promising in vitro activity against atypical mycobacterial strains
Language English Country England, Great Britain Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
19403314
DOI
10.1016/j.bmc.2009.04.008
PII: S0968-0896(09)00348-4
Knihovny.cz E-resources
- MeSH
- Antitubercular Agents chemistry pharmacology toxicity MeSH
- Esterification MeSH
- Hydrophobic and Hydrophilic Interactions MeSH
- Quantitative Structure-Activity Relationship MeSH
- Nontuberculous Mycobacteria drug effects MeSH
- Salicylanilides chemistry pharmacology toxicity MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Antitubercular Agents MeSH
- Salicylanilides MeSH
A new series of 30 N-protected amino acid esters were prepared as a part of ongoing search for new anti-tuberculosis active salicylanilides. The esters possess high in vitro activity against Mycobacterium tuberculosis, Mycobacterium avium, and two strains of Mycobacterium kansasii, where one is an isolate from the patient, with MIC in the range 1-32 micromol/L for all tested strains. The prepared esters can be considered as prodrugs with better bio-availability and as more efficient transport forms through the mycobacterial cell membranes due to the higher lipophilicity. The experimental and calculated lipophilicity, stability, antituberculotic activity, cytotoxicity as well as the quantitative structure-activity relationships (QSARs) explored by the Intelligent Problem Solver (IPS) in Trajan Neural Network Simulator 6.0 are presented.
References provided by Crossref.org
Salicylanilides and Their Anticancer Properties
N-Alkoxyphenylhydroxynaphthalenecarboxamides and Their Antimycobacterial Activity
Synthesis and Biological Evaluation of N-Alkoxyphenyl-3-hydroxynaphthalene-2-carboxanilides
Preparation and biological properties of ring-substituted naphthalene-1-carboxanilides
Antibacterial and herbicidal activity of ring-substituted 2-hydroxynaphthalene-1-carboxanilides
Antibacterial and herbicidal activity of ring-substituted 3-hydroxynaphthalene-2-carboxanilides
Antibacterial activity of salicylanilide 4-(trifluoromethyl)-benzoates
Antimycobacterial activity of salicylanilide benzenesulfonates
