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Synthesis and antituberculosis activity of new acylthiosemicarbazides designed by structural modification
Author(s) -
Martínez Roberto,
EspitiaPinzón Clara I.,
Silva Miranda Mayra,
ChávezSantos Rosa María,
PretelinCastillo Gustavo,
RamosOrea Aldahir,
HernándezBáez Ángela M.,
CotlamePérez Sandra,
PedrazaRodríguez Rogelio
Publication year - 2020
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.21626
Subject(s) - substituent , amide , mycobacterium tuberculosis , chemistry , combinatorial chemistry , ring (chemistry) , stereochemistry , structure–activity relationship , tuberculosis , chlorine atom , derivative (finance) , biochemistry , in vitro , medicinal chemistry , organic chemistry , medicine , pathology , economics , financial economics
Acylthiosemicarbazides 8a–n were designed by structural modification of lead Compound 7 . The syntheses of 8a–n involve a five‐step procedure starting from carboxylic acids. Compounds 8a–n were tested against three Mycobacterium tuberculosis strains to measure their inhibitory antituberculosis activities. These activities could be explained according to the presence or absence of the chlorine substituent in the aromatic ring of the amide joined to the thiosemicarbazide core. Thiosemicarbazide derivative 8n is a candidate for the development of novel antitubercular agents. Ongoing studies are focused on exploring the mechanism by which these compounds inhibit M. tuberculosis cell growth.