56643-69-7Relevant articles and documents
Synthesis and investigation of inhibitory activities of imidazole derivatives against the metallo-β-lactamase IMP-1
Khalili Arjomandi, Omid,Kavoosi, Mahboubeh,Adibi, Hadi
, (2019/09/19)
Mutations in bacteria can result in antibiotic resistance due to the overuse or abuse of β-lactam antibiotics. One strategy which bacteria can become resistance toward antibiotics is secreting of metallo β-lactamase enzymes that can open the lactam ring of the β-lactam antibiotic and inactivate them. This issue is a threat for human health and one strategy to overcome this situation is co-administration of β-lactam antibiotics with an inhibitor. So far, no clinically available inhibitors of metallo β-lactamases (MBLs) reported and the clinically inhibitors of serine β-lactamase are useless for MBLs. Accordingly, finding a potent inhibitor of the MBLs being very important. In this study, imidazole derivatives primarily were synthesized and their inhibitory activity were measured. Later in silico binding model was used to predict the configuration and conformation of the ligands into the active site of enzyme. Two molecules demonstrated with IC50 of 39 μM and 46 μM against MBL (IMP-1).
Synthesis of 5H-Imidazoisoindole: Photocyclization of N,N'-Bis(o-chlorobenzyl)imidazolium Chloride and N-(o-Chlorobenzyl)imidazole
Byun, Young-Seok,Jung, Chang-Hee,Park, Yong-Tae
, p. 1835 - 1838 (2007/10/03)
A N-heterocyclic compound containing two hetero atoms, imidazoisoindole, was synthesized in 40percent yield by the intramolecular photocyclization of N,N'-bis(o-chlorobenzyl)imidazolium salts 1 in water (neutral or pH ca. 4) or of N-(o-chlorobenzyl)imidazole 2, in aqueous acid (pH ca. 4).However, the photocyclized compound 3 was not formed effectively in basic aqueous solution (3 equivalents of sodium hydroxide or pyridine) or in acetonitrile by the photochemical reaction of N,N'-bis(o-chlorobenzyl)imidazolium salts 1 or N-(o-chlorobenzyl)imidazole (2).
Substituted 5-(alkyl)carboxamide imidazoles
-
, (2008/06/13)
Angiotensin II receptor antagonists having the formula: STR1 which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma pharmaceutical compositions including these antagonists, and methods of
