Recommanded Product: Phenyl(pyridin-2-yl)methanone. In 2021.0 ACTA PHARMACOL SIN B published article about CELL-DEATH; IN-VITRO; CLASSIFICATION; ORGANIZATION; ANTIFUNGAL in [Zhao, Bing; Zhang, Xinhui; Yu, Tingting; Liu, Ying; Zhang, Xiaoling; Yao, Yongfang; Feng, Xuejian; Liu, Hongmin; Ma, Liying; Qin, Shangshang] Zhengzhou Univ, State Key Lab Esophageal Canc Prevent & Treament, Key Lab Technol Drug Preparat,Inst Pharmaceut Res, Minist Educ China,Key Lab Henan Prov Drug Qual &, Zhengzhou 450001, Henan, Peoples R China; [Zhao, Bing; Zhang, Xinhui; Yu, Tingting; Liu, Ying; Zhang, Xiaoling; Yao, Yongfang; Feng, Xuejian; Liu, Hongmin; Ma, Liying; Qin, Shangshang] Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Peoples R China; [Yu, Dequan] Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing 100050, Peoples R China in 2021.0, Cited 44.0. The Name is Phenyl(pyridin-2-yl)methanone. Through research, I have a further understanding and discovery of 91-02-1.
New Delhi metallo-beta-lactamase-1 (NDM-1) is capable of hydrolyzing nearly all beta-lactam antibiotics, posing an emerging threat to public health. There are currently less effective treatment options for treating NDM-1 positive superbug, and no promising NDM-1 inhibitors were used in clinical practice. In this study, structure-activity relationship based on thiosemicarbazone derivatives was systematically characterized and their potential activities combined with meropenem (MEM) were evaluated. Compounds 19bg and 19bh exhibited excellent activity against 10 NDM-positive isolate clinical isolates in reversing MEM resistance. Further studies demonstrated compounds 19bg and 19bh were uncompetitive NDM-1 inhibitors with Ki = 0.63 and 0.44 mu mol/L, respectively. Molecular docking speculated that compounds 19bg and 19bh were most likely to bind in the allosteric pocket which would affect the catalytic effect of NDM-1 on the substrate meropenem. Toxicity evaluation experiment showed that no hemolysis activities even at concentrations of 1000 mg/mL against red blood cells. In vivo experimental results showed combination of MEM and compound 19bh was markedly effective in treating infections caused by NDM-1 positive strain and prolonging the survival time of sepsis mice. Our finding showed that compound 19bh might be a promising lead in developing new inhibitor to treat NDM-1 producing superbug. (C) 2021 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
Recommanded Product: Phenyl(pyridin-2-yl)methanone. About Phenyl(pyridin-2-yl)methanone, If you have any questions, you can contact Zhao, B; Zhang, XH; Yu, TT; Liu, Y; Zhang, XL; Yao, YF; Feng, XJ; Liu, HM; Yu, DQ; Ma, LY; Qin, SS or concate me.
Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem