1354047-20-3Relevant academic research and scientific papers
Synthesis and Kinetic Testing of Tetrahydropyrimidine-2-thione and Pyrrole Derivatives as Inhibitors of the Metallo-β-lactamase from Klebsiella pneumonia and Pseudomonas aeruginosa
Hussein, Waleed M.,Fatahala, Samar S.,Mohamed, Zainab M.,Mcgeary, Ross P.,Schenk, Gerhard,Ollis, David L.,Mohamed, Mosaad S.
, p. 500 - 515 (2012/11/07)
Metallo-β-lactamases (MBLs), produced by an increasing number of bacterial pathogens, facilitate the hydrolysis of many commonly used β-lactam antibiotics. There are no clinically useful antagonists against MBLs. Two sets of tetrahydropyrimidine-2-thione and pyrrole derivatives were synthesized and assayed for their inhibitory effects on the catalytic activity of the IMP-1 MBL from Pseudomonas aeruginosa and Klebsiella pneumoniae. Nine compounds tested (1a, 3b, 5c, 6b, 7a, 8a, 11c, 13a, and 16a) showed micromolar inhibition constants (Ki values range from ~20-80μm). Compounds 1c, 2b, and 15a showed only weak inhibition. In silico docking was employed to investigate the binding mode of each enantiomer of the strongest inhibitor, 5c (Ki=19±9μm), as well as 7a (Ki=21±10μm), the strongest inhibitor of the pyrrole series, in the active site of IMP-1.
Synthesis of new pyrroles of potential anti-inflammatory activity
Mohamed, Mosaad S.,Kamel, Rehab,Fathallah, Samar S.
experimental part, p. 830 - 839 (2012/03/08)
We herein disclose a series of novel pyrrole derivatives 1-4 and pyrrolo[2,3-d]pyrimidine derivatives 6-11 as novel potent anti-inflammatory compounds. The structures were confirmed by IR, 1H-NMR, and MS. Some newly synthesized compounds were e
