56643-75-5Relevant academic research and scientific papers
A Photoregulated Racemase Mimic
Saha, Monochura,Hossain, Munshi Sahid,Bandyopadhyay, Subhajit
, p. 5220 - 5224 (2021/01/18)
The racemase enzymes convert L-amino acids to their D-isomer. The reaction proceeds through a stepwise deprotonation–reprotonation mechanism that is assisted by a pyridoxal phosphate (PLP) coenzyme. This work reports a PLP–photoswitch–imidazole triad where the racemization reaction can be controlled by light by tweaking the distance between the basic residue and the reaction centre.
Reversible photoresponsive activity of a carbonic anhydrase mimic
Saha, Monochura,Bandyopadhyay, Subhajit
, p. 3294 - 3297 (2019/04/09)
The carbonic anhydrase (CA) enzyme reversibly transforms carbon dioxide and water to a carbonate ion and a proton. Photoresponsive enzyme mimics, where the CA-activity can be turned on and off reversibly with light, have not been reported so far. We have designed an active site mimic that offers reversible control of the catalytic activity using light. Moreover, in the presence of a cationic polymer, we have demonstrated that the CA-activity was further enhanced by stabilizing the transition state with the cis-form of the enzyme mimic which can catalyze the hydration of gaseous CO2.
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).
Preparation and characterization of a novel poly-geminal dicationic ionic liquid (PGDIL)
Guo, Yanni,He, Deliang,Xie, Aomei,Qu, Wei,Tang, Yining,Shang, Jun,Zhu, Rilong
, (2019/10/28)
1,4-bis(3-(m-aminobenzyl)imidazole-1-yl)butane bis(hexafluorinephosphate), a novel geminal dicationic ionic liquid (GDIL) containing anilino groups has been synthesized to prepare a novel poly-geminal dicationic ionic liquid film by electro-polymerization. The morphology and structure of the PGDIL film were analyzed by SEM and FTIR, and a possible polymerization mechanism of GDIL on an Au electrode surface was determined to be 3D instantaneous nucleation. The existence of polyaniline-like units in the PGDIL chain was confirmed by FTIR, indicating that the anilino groups of GDIL were electro-polymerized on the surface of the Au electrode using the chronoamperometry method. The electrochemical performance of the PGDIL film in phenol was studied by cyclic voltammetry, and it was determined that the PGDIL film electrode promoted enhanced phenol electrocatalysis compared to the untreated Au electrode. This work extends the application range of poly ionic liquids and associates ionic liquids with conductive polymers. Where further studies on other physical and chemical properties of polymers will be necessary.
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. identification of a suitable "back-up" compound for N-tert-butyl isoquine
O'Neill, Paul M.,Shone, Alison E.,Stanford, Deborah,Nixon, Gemma,Asadollahy, Eghbaleh,Park, B. Kevin,Maggs, James L.,Roberts, Phil,Stocks, Paul A.,Biagini, Giancarlo,Bray, Patrick G.,Davies, Jill,Berry, Neil,Hall, Charlotte,Rimmer, Karen,Winstanley, Peter A.,Hindley, Stephen,Bambal, Ramesh B.,Davis, Charles B.,Bates, Martin,Gresham, Stephanie L.,Brigandi, Richard A.,Gomez-de-las-Heras, Federico M.,Gargallo, Domingo V.,Parapini, Silvia,Vivas, Livia,Lander, Hollie,Taramelli, Donatella,Ward, Stephen A.
supporting information; experimental part, p. 1828 - 1844 (2009/12/31)
On the basis of a mechanistic understanding of the toxicity of the 4-aminoquinoline amodiaquine (1b), three series of amodiaquine analogues have been prepared where the 4-aminophenol "metabolic alert" has been modified by replacement of the 4'-hydroxy gro
Mono-nitration of aromatic compounds via nitrate salts
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Page/Page column 6; 11, (2008/06/13)
A method of nitrating a compound selected from the group consisting of is provided.
Mono-nitration of aromatic compounds via their nitric acid salts
Zhang, Pingsheng,Cedilote, Miall,Cleary, Thomas P.,Pierce, Michael E.
, p. 8659 - 8664 (2008/03/30)
Aromatic compounds bearing a basic nitrogen atom can be converted to the corresponding nitric acid salts. Mono-nitration of the compounds can be carried out by adding a dichloromethane solution of the salts to sulfuric acid, or by adding acetyl chloride (or trifluoroacetic anhydride) to a dichloromethane solution of the salts. This protocol provides, among other benefits, the most convenient and reliable way for the prevention of over-/under-nitration and is especially suitable for scale-up.
Novel benzimidazole derivatives and pharmaceutical compositions comprising these compounds
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, (2008/06/13)
The present invention relates to novel benzimidazole derivatives, pharmaceutical composition containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABA receptor complex, and in particular for inducing and maintaining anesthesia, sedation and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.
Research on anti-bacterial and anti-fungal agents II. Synthesis and anti-fungal activity of new (1H-imidazol-1-ylmethyl)benzenamine derivatives
Porretta, Giulio Cesare,Biava, Mariangela,Cerreto, Felice,Scalzo, Marcello,Panico, Salvatore,et al.
, p. 311 - 318 (2007/10/02)
The synthesis and in vivo and in vitro anti-fungal activities of new (1H-imidazol-1-ylmethyl)benzenamine derivatives are reported.Anti-microbial data in comparison with miconazole show that many compounds exhibit an interesting anti-mycotic activity.Keywo
