41833-17-4Relevant academic research and scientific papers
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).
DEGRADABLE IMIDAZOLIUM OLIGOMER AND POLYMER FOR ANTIMICROBIAL APPLICATIONS
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Page/Page column 37, (2019/01/16)
The present invention relates to an imidazolium oligomer of formula (I) and an imidazolium oligomer or a polymer of formula (II) where the various groups are as defined in the specification. The present invention also relates to the methods for their preparation, antimicrobial composition, antimicrobial gel containing these oligomers and/or polymers of Formula (I) and (II), and uses of these oligomers and/or polymers in the treatment of a microbial infection or disease.
NITROGEN-CONTAINING HETEROCYCLIC RING SUBSTITUTED DIHYDROARTEMISININ DERIVATIVES AND USE THEREOF
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Paragraph 0054; 0055, (2016/03/01)
The present invention belongs to the field of medicinal technique, specifically relates to nitrogen-containing heterocyclic ring-substituted dihydroartemisinin derivatives and their optical isomers according to formula I or II; wherein substituent X, Y, r
AZOLIUM AND PURINIUM SALT ANTICANCER AND ANTIMICROBIAL AGENTS
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Page/Page column 23, (2012/11/13)
Singly and multiply charged imidazolium cations (ICs) have been identified as a class of chemical compositions that possess potent antineoplastic, antibacterial and antimicrobial properties. The imidazolium cations disclosed demonstrate greater or equival
Synthesis and biochemical evaluation of a range of (4-substituted phenyl)sulfonate derivatives of 4-hydroxybenzyl imidazole-based compounds as potent inhibitors of 17α-hydroxylase/17,20-lyase (P450 17α) derived from rat testicular microsomes
Owen, Caroline P.,Shahid, Imran,Lee, Wai-Yee,Ahmed, Sabbir
scheme or table, p. 5345 - 5348 (2010/11/04)
We report the synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of (4-substituted phenyl)sulfonate derivatives of 4-hydroxybenzyl imidazole against the two components of 17α-hydroxylase/ 17,20-lyase (P45017α), namely, 17α-hydroxylase (17α-OHase) and 17,20-lyase (lyase). The results show the compounds to be highly potent inhibitors with limited selectivity towards the lyase component [e.g., toluene-4-sulfonic acid 4-imidazol-1-ylmethyl-phenyl ester (4) possessed an IC50 value of 40 nM against 17α-OHase and 30 nM against lyase].
Synthesis and biochemical evaluation of a range of sulfonated derivatives of 4-hydroxybenzyl imidazole as highly potent inhibitors of rat testicular 17α-hydroxylase/17,20-lyase (P-45017α)
Ahmed, Sabbir,Shahid, Imran,Dhanani, Sachin,Owen, Caroline P.
experimental part, p. 4698 - 4701 (2010/04/28)
We report the synthesis and biochemical evaluation of a range of 4-sulfonated derivatives of 4-hydroxybenzyl imidazole which has been targetted against the two components of 17α-hydroxylase/17,20-lyase (P-45017α), namely, 17α-hydroxylase (17α-OHase) and 17,20-lyase (lyase). The results from the biochemical testing suggest that the compounds synthesised are highly potent inhibitors possessing excellent selectivity towards the lyase component.
Synthesis and biochemical evaluation of a range of potent benzyl imidazole-based compounds as potential inhibitors of the enzyme complex 17α-hydroxylase/17,20-lyase (P45017α)
Owen, Caroline P.,Dhanani, Sachin,Patel, Chirag H.,Shahid, Imran,Ahmed, Sabbir
, p. 4011 - 4015 (2007/10/03)
The cytochrome P-450 enzyme, 17α-hydroxylase/17,20-lyase (P45017α), is a potential target in hormone-dependent cancers. Here, we report the synthesis and biochemical evaluation of a range of benzyl imidazole-based compounds which have been targeted against the two components of this enzyme, that is, 17α-hydroxylase (17α-OHase) and 17,20-lyase (lyase). The results from the biochemical testing suggest that the compounds synthesised are good inhibitors, with N-4-iodobenzyl imidazole (5) (IC50 = 10.06 μM against 17α-OHase and IC50 = 1.58 μM against lyase) showing equipotent activity against lyase compared to the standard compound, ketoconazole (KTZ) (IC50 = 3.76 ± 0.01 μM against 17α-OHase and IC50 = 1.66 ± 0.15 μM against lyase). Furthermore, the compounds tested are less potent towards the 17α-OHase component, a desirable property in the development of novel inhibitors of P45017α.
NOVEL COMPOUNDS USEFUL AS NEURO-PROTECTIVE AGENTS
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, (2008/06/13)
This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
Compounds useful as neuro-protective agents
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, (2008/06/13)
This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
Use of phenyl oxazole or phenyl thiazole derivatives for treating neuropathic pain
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, (2008/06/13)
The present invention provides a method for treating neuropathic pain comprising administering an analgesic dosage of a compound of formula I to an animal in need of such treatment certain phenyl oxazoles or phenyl thiazoles.
