539805-83-9Relevant academic research and scientific papers
Diaryl-Substituted Azolylthioacetamides: Inhibitor Discovery of New Delhi Metallo-β-Lactamase-1 (NDM-1)
Zhang, Yi-Lin,Yang, Ke-Wu,Zhou, Ya-Jun,LaCuran, Alecander E.,Oelschlaeger, Peter,Crowder, Michael W.
, p. 2445 - 2448 (2015/08/24)
The emergence and spread of antibiotic-resistant pathogens is a global public health problem. Metallo-β-lactamases (MβLs) such as New Delhi MβL-1 (NDM-1) are principle contributors to the emergence of resistance because of their ability to hydrolyze almost all known β-lactam antibiotics including penicillins, cephalosporins, and carbapenems. A clinical inhibitor of MBLs has not yet been found. In this study we developed eighteen new diaryl-substituted azolylthioacetamides and found all of them to be inhibitors of the MβL L1 from Stenotrophomonas maltophilia (KiiiII ion(s) preferentially via the triazole moiety, while other moieties interact mostly with the conserved active site residues Lys224 (CcrA, NDM-1, and ImiS) or Ser221 (L1).
Synthesis and biological studies of N-phenyl substituted 2-(-5-(pyridine-4-yl)-1,3,4-oxadiazole-2-yl thio)acetamides
Rao, M.E. Bhanoji,Rajurkar, Vikas G.
, p. 2648 - 2652 (2012/01/05)
As oxadiazole have proven to be good antimicrobial agents, Antitubercular, analgesic (peripheral and central) and antiinflammatory agents. A new series of oxadiazole derivatives were synthesized and characterized by 1H NMR, IR, GCMS sophisticated analytical instruments and were evaluated for their antimicrobial activity, antitubercular activity, toxicity as per standard guidelines, analgesic (peripheral and central) and antiinflammatory activity. Out of several derivatives synthesized a few of N-phenyl substituted 2-(5-(pyridine-4- yl)-1,3,4-oxadiazole-2-yl thio)acetamide explores good antimicrobial activity by using Cup-Plate method, antitubercular activity by middle brook 7H9 agar medium against H37Rv, analgesic activity by Writhing and Tail immersion method and antiinflammatory by rat paw edema method.
