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Synthesis, spectral characterization, antibacterial, cytotoxic evaluation and docking studies of new urea and thiourea derivatives

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Title Synthesis, spectral characterization, antibacterial, cytotoxic evaluation and docking studies of new urea and thiourea derivatives
 
Creator Ramaswamy, Shanmugam
Kongara, Deepak
Priyanka, DL
Gade, Ramya
R, Krishna Raj
R, Gayathri
 
Subject Antimicrobial activity
Cytotoxicity studies
Disc diffusion method
Isoniazid
Molecular docking
Thiourea
Urea
 
Description 767-776
Isoniazid is one of the main API’s used in the combination treatment of tuberculosis recommended by the WHO. Urea
and its derivatives are an important class of heterocyclic compounds that possess a wide range of therapeutic and
pharmacological properties, while thiourea is an organosulphur compound in that it resembles urea except that the atom
oxygen has been replaced by a Sulphur atom, but the properties of urea and thiourea are significantly different. The current
work concerns the synthesis of a new class of urea and thiourea derivatives of isoniazid with various isocyanates and
isothiocyanates in the presence of trimethylamine. The IR and NMR spectral data were performed for the urea and thiourea
derivatives of the compounds [(3c & 3f) & (3d & 3e)], respectively. Molecular docking studies of the compounds (3a-h)
revealed the binding mode involved in the active site of DNA gyrase. The synthesized urea and thiourea derivatives of
isoniazid with various isocyanates and isothiocyanates were tested for their antibacterial activity against gram-positive and
gram-negative bacteria using the “disc diffusion method”. Of all compounds tested, the urea derivatives (3a &3d), the
thiourea derivatives (3e & 3g) showed more potent activity than the other compounds. The MTT assay revealed
concentration dependent cytotoxic effects over a concentration range 25-200 μg/mL.
 
Date 2022-08-01T06:38:12Z
2022-08-01T06:38:12Z
2022-07
 
Type Article
 
Identifier 0975-0959 (Online); 0301-1208 (Print)
http://nopr.niscpr.res.in/handle/123456789/60223
 
Language en
 
Publisher NIScPR-CSIR,India
 
Source IJBB Vol.59(7) [July 2022]