145626-26-2Relevant articles and documents
Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis
Dixit, Prasad P.,Dixit, Prashant P.,Thore, Shivajirao N.
, p. 38 - 47 (2016)
Efflux inhibition is proven bacterial machinery responsible for removal of bacterial wastage including antibiotics. Recently, efflux inhibitors (EI) have been tested with encouraging results as an adjuvant therapy for treatment of tuberculosis (TB). Although, EI have emerged as innovative approach of treatment for multi drug resistant (MDR) & extensively drug resistant tuberculosis (XDR-TB), toxicity profile limits their wider use. To address this issue, we have attempted synthesizing hybrid molecules those results by combining known EI and triazole. This synthesis was aimed to arrive at structure that possesses pharmacophore from known EI. Synthesized molecules were evaluated as growth inhibitors (GI) and Efflux inhibitor of TB initially against Mycobacterium smegmatis mc2155. Pharmacologically active compounds were then tested for their cytotoxicity to further narrow down search. Most active compounds 144, 145, 154 and 163 were then tested for their GEI action against Mycobacterium tuberculosis (Mtb). Synthesized compounds were also tested for their synergistic action with first line and second line anti-TB drugs and ethidium bromide (EtBr). We arrived at compound 135 as most potent dual inhibitor of tuberculosis.
X-ray characterization, Hirshfeld surface analysis, DFT calculations,in vitroandin silicolipoxygenase inhibition (LOX) studies of dichlorophenyl substituted 3-hydroxy-chromenones
Ahmed, Muhammad Naeem,Andleeb, Hina,Ashfaq, Muhammad,Frontera, Antonio,Ghias, Mehreen,Gil, Diego M.,Ibrahim, Mahmoud A. A.,Shah, Syed Wadood Ali,Shoaib, Mohammad,Tahir, Muhammad Nawaz
, p. 19928 - 19940 (2021/11/12)
This work reports the synthesis and X-ray characterization of three dichlorophenyl substituted 3-hydroxy-chromen-4-one derivatives,i.e., 2-(2,4-dichlorophenyl)-3-hydroxy-4H-chromen-4-one (1), 2-(2,3-dichlorophenyl)-3-hydroxy-4H-chromen-4-one (2), and 2-(2
Synthesis and antibacterial activity of chalcone derivatives containing thioether triazole
Chen, Mei,Chen, Ying,He, Jun,He, Ming,Li, Pu,Su, Shijun,Wang, Hua,Xue, Wei
, (2020/01/22)
The infection of Xanthomonas oryzae pv. Oryzae (Xoo), Ralstonia solanacearum (Rs), and Xanthomonas axonopodis pv. Citri (Xac) has become a major problem in agricultural production. In this study, a series of novel chalcone derivatives containing thioether triazoles were designed and synthesized. The structures of the novel compounds were systematically characterized via 1H-NMR, 13C-NMR, and HRMS. Moreover, the antibacterial activity results showed that E10, E11, E15, and E16 have adequate antibacterial activities against Xoo, Rs, and Xac. Among the different compounds, E15 exhibited remarkable inhibitory effect against Xac with an EC50 of 9.1 μg.mL-1, which was better than that of commercial agent bismerthiazol (54.9 μg.mL-1). In addition, the possible antibacterial mechanism of the target compound E15 against Xac was studied via scanning electron microscopy (SEM).