Consensus Pharmacophore identification for antimycobacterial DprE1 inhibitory activity of substituted hydantoins.
نویسندگان
چکیده
منابع مشابه
Pharmacophore modeling and 3D-QSAR studies on substituted benzothiazole / benzimidazole analogues as DHFR inhibitors with antimycobacterial activity
The resurgence of tuberculosis and the emergence of multidrug-resistant strains of Mycobacteria drugs has propelled the development of new structural classes of antitubercular agents. The present study was undertaken to investigate the opportunities which the enzyme dihydrofolate reductase, a promising drug target for treatment of Mycobacterial infections offers for the development of new TB dr...
متن کاملANtIMYcoBActeRIAL ActIVItY oF 4- AND 3,4-sUBstItUteD coUMARINs
The present article describes the evaluation of the in vitro activity against M. tuberculosis H37Rv of eight coumarin-derived aminoalcohols and amidoamines. Seven of the compounds display activity between 10 and 20 times higher than the classicall anti-TB drug ethambutol. The combination of coumarin scaffold with aminoalcohol fragments gave the most promising activities with MICs up to 0.32 μM.
متن کاملSynthesis of substituted hydantoins in low melting mixtures.
A novel domino synthesis of 1,3,5-trisubstituted hydantoin derivatives has been developed in low melting L-(+)-tartaric acid-DMU melt mixtures. The functionalized hydantoins are obtained in good yields from β,γ-unsaturated ketoacids and urea under environmentally benign and simple reaction conditions.
متن کاملFacile one-pot synthesis of 5-substituted hydantoins.
5-Substituted and 5,5-disubstituted hydantoins are synthesised from the corresponding aldehydes or ketones, using a one-pot, gallium(III) triflate-catalysed procedure that is compatible with a range of substrates and solvents.
متن کامل3D- Quantitative Structure-Activity Relationship Analysis of Some 2-Substituted Halogenbenzimidazoles Analogues with Antimycobacterial activity
A three dimensional quantitative structure-activity relationship study using the k-nearest neighbor analysis method was performed on a series of -polyfluoroalkyl and 2-Nitrobenzylsulphanyl benzimidazoles for their Antimycobacterial, activity. This study was performed using 28 compounds, for which k-nearest neighbor analysis models were developed using a training set of 22 compounds. Database al...
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ژورنال
عنوان ژورنال: Journal of Current Pharma Research
سال: 2019
ISSN: 2230-7834,2230-7842
DOI: 10.33786/jcpr.2019.v09i02.002