I found the field of Pharmacology & Pharmacy very interesting. Saw the article Discovery of thiosemicarbazone derivatives as effective New Delhi metallo-beta-lactamase-1 (NDM-1) inhibitors against NDM-1 producing clinical isolates published in 2021.0. Recommanded Product: 99-93-4, Reprint Addresses Ma, LY; Qin, SS (corresponding author), 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.; Ma, LY; Qin, SS (corresponding author), Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Peoples R China.; Yu, DQ (corresponding author), Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing 100050, Peoples R China.. The CAS is 99-93-4. Through research, I have a further understanding and discovery of 4′-Hydroxyacetophenone
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: 99-93-4. About 4′-Hydroxyacetophenone, 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:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles