Title
Biological evaluation of bisbenzaldehydes against four **Mycobacterium** species Biological evaluation of bisbenzaldehydes against four **Mycobacterium** species
Author
Faculty/Department
Faculty of Pharmaceutical, Biomedical and Veterinary Sciences . Biomedical Sciences
Publication type
article
Publication
Paris ,
Subject
Biology
Human medicine
Source (journal)
European journal of medicinal chemistry. - Paris, 1974, currens
Volume/pages
63(2013) , p. 731-738
ISSN
0223-5234
ISI
000322855400072
Carrier
E
Target language
English (eng)
Full text (Publishers DOI)
Affiliation
University of Antwerp
Abstract
A series of bisbenzaldehydes and structurally related analogs, conveniently synthesized via microwave-assisted reactions, were evaluated in vitro against drug susceptible and multi-drug resistant M. tb, against virulent M. bovis, against M. ulcerans and against two M. avium subspecies. Among the 33 substances that were tested, compound 12, i.e. 4,4-[1,12-dodecanediyl(oxy)]bisbenzaldehyde emerged as the most promising hit. Its activity was further confirmed in an intracellular growth inhibition assay of M. tb in murine J774 A.1 macrophages. None of the compounds showed significant cytotoxicity on human C3A hepatocytes in a neutral red dye uptake assay and no genotoxicity or mutagenicity was observed, as demonstrated by a VITOTOXTM test and confirmed with a comet assay.
E-info
https://repository.uantwerpen.be/docman/iruaauth/3f15c3/32e6539.pdf
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