Title |
Design, synthesis, and characterization of (1-(4-aryl)-1H-1,2,3-triazol-4-yl)methyl, substituted phenyl-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylates against Mycobacterium tuberculosis
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Published in |
Drug Design, Development and Therapy, August 2016
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DOI | 10.2147/dddt.s109760 |
Pubmed ID | |
Authors |
Katharigatta N Venugopala, G B Dharma Rao, Subhrajyoti Bhandary, Melendhran Pillay, Deepak Chopra, Bandar E Aldhubiab, Mahesh Attimarad, Osama Ibrahim Alwassil, Sree Harsha, Koleka Mlisana |
Abstract |
The novel (1-(4-aryl)-1H-1,2,3-triazol-4-yl)methyl, substituted phenyl-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate derivatives were synthesized by the click reaction of the dihydropyrimidinones, bearing a terminal alkynyl group, with various substituted aryl azides at room temperature using a catalytic amount of Cu(OAc)2 and sodium ascorbate in a 1:2 ratio of acetone and water as a solvent. The newly synthesized compounds were characterized by a number of spectroscopic techniques, such as infrared, liquid chromatography-mass spectrometry, (1)H, and (13)C nuclear magnetic resonance along with single crystal X-ray diffraction. The current procedure for the synthesis of 1,2,3-triazole hybrids with dihydropyrimidinones is appropriate for the synthesis of a library of analogs 7a-l and the method accessible here is operationally simple and has excellent yields. The title compounds 7a-l were evaluated for their in vitro antitubercular activity against H37RV and multidrug-resistant strains of Mycobacterium tuberculosis by resazurin microplate assay plate method and it was found that compound 7d was promising against H37RV and multidrug-resistant strains of M. tuberculosis at 10 and 15 μg/mL, respectively. |
X Demographics
Geographical breakdown
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United Kingdom | 1 | 100% |
Demographic breakdown
Type | Count | As % |
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Members of the public | 1 | 100% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
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Unknown | 37 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
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Student > Ph. D. Student | 5 | 14% |
Lecturer | 4 | 11% |
Professor > Associate Professor | 4 | 11% |
Student > Doctoral Student | 3 | 8% |
Student > Master | 3 | 8% |
Other | 8 | 22% |
Unknown | 10 | 27% |
Readers by discipline | Count | As % |
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Pharmacology, Toxicology and Pharmaceutical Science | 6 | 16% |
Chemistry | 5 | 14% |
Medicine and Dentistry | 5 | 14% |
Nursing and Health Professions | 4 | 11% |
Immunology and Microbiology | 2 | 5% |
Other | 3 | 8% |
Unknown | 12 | 32% |