342592-68-1Relevant articles and documents
In vitro, in vivo and in silico-driven identification of novel benzimidazole derivatives as anticancer and anti-inflammatory agents
Sathyanarayana, Reshma,Poojary, Boja,Srinivasa, Sudhanva M.,Merugumolu, Vijay K.,Chandrashekarappa, Revanasiddappa B.,Rangappa, Shobith
, p. 1301 - 1317 (2021/08/24)
The synthesis of novel benzimidazole derivatives with varied carbon chain length was achieved via “one-pot” nitro reductive cyclization (6a–o). In each case, compounds were determined by the elemental analyses, FT-IR, mass, 1H and 13
Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents
Liu, Hongyan,Sun, Danwen,Du, Hang,Zheng, Changji,Li, Jingya,Piao, Huri,Li, Jia,Sun, Liangpeng
, p. 163 - 173 (2019/04/13)
Several series of novel tryptophan-derived rhodanine derivatives were synthesized and identified as potential competitive PTP1B inhibitors and antibacterial agents. Among the compounds studied, 10b was found to have the best in vitro inhibition activity against PTP1B (IC50 = 0.36 ± 0.02 μM). In addition, the compounds also showed potent inhibition against other PTPs, especially CDC25B. Molecular docking analysis demonstrated that compounds 7c and 10b could occupy both the catalytic site and the adjacent pTyr binding site simultaneously. The compounds also showed higher levels of activity against gram-positive strains, the gram-negative strain Escherichia coli 1924, and multidrug-resistant gram-positive bacterial strains. Compounds 7c, 8c, 9e, 10a, and 10c had comparable or more potent antibacterial activity than the positive controls.
First Discovery of Novel Pyrido[1,2- a]pyrimidinone Mesoionic Compounds as Antibacterial Agents
Liu, Dengyue,Zhang, Jian,Zhao, Lei,He, Wengjing,Liu, Zhengjun,Gan, Xiuhai,Song, Baoan
, (2019/10/21)
Plant bacterial diseases cause tremendous decreases in crop yield and quality, and there is a lack of highly effective and low-risk antibacterial agents. A series of novel pyrido[1,2-a]pyrimidinone mesoionic compounds containing vanillin moieties were synthesized, and the application of these mesoionic compounds as plant antibacterial agents was reported here for the first time. The bioassay results revealed that the mesoionic compounds had good antibacterial activity. Of these compounds, compound 11 showed excellent in vitro activity against Xanthomonas oryzae pv. oryzae, with an EC50 value of 1.1 μg/mL, which was substantially better than that of bismerthiazol (92.7 μg/mL) and thiodiazole copper (105.4 μg/mL). Moreover, greenhouse condition trials indicated that the protective and curative activities of compound 11 against rice bacterial leaf blight were 75.12 and 72.04%, respectively, which were better than those of bismerthiazol (62.24 and 50.83%, respectively) and thiodiazole copper (53.35 and 65.04%, respectively). These results provide a basis for the application of mesoionic vanillin moieties as new antibacterial agents.
