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Alwar, India

Hadda T.B.,University Mohammed Premier | Ali M.A.,SunRise University | Ali M.A.,Universiti Sains Malaysia | Masand V.,Vidya Bharati College | And 3 more authors.
Medicinal Chemistry Research | Year: 2013

In this study, we have amalgamated computational methodologies, viz. Petra, Osiris and Molinspiration (POM) to identify pharmacophores and antipharmacophores for antibacterial/antiviral activities of some 2-pyrazolines derivatives. Lipophilicity and the presence of tautomerism process are the major factors that govern the orientation to antibacterial and/or antiviral activity. On other hand, it was observed that these compounds have two different active sites and can inhibit both antiviral and antibacterial strains. Further, we have carried out receptor-based electrostatic analysis to confirm the electronic, steric and hydrophobic requirements for future modifications. The analyses provide substantial idea about the structural features responsible for their combined antibacterial/antiviral activity and provide guidelines for further modifications, with the aim of improving the activity and selectivity of designed drugs targeting HIV and tuberculosis microorganisms. © 2012 Springer Science+Business Media, LLC. Source


Wei A.C.,Universiti Sains Malaysia | Ali M.A.,Universiti Sains Malaysia | Ali M.A.,New Drug Discovery Research | Ali M.A.,SunRise University | And 7 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2012

A series of twelve dispiropyrrolidines were synthesized using [3+2]-cycloaddition reactions. The synthesized compounds were screened for their antimycobacterial activity against M. tuberculosis H37Rv and INH resistant M. tuberculosis strains using agar dilution method, four of them showed good activity with MIC of less than 1 μM. Compound 4′-[5-(4-fluorophenyl)pyridin-3-yl]-1′-methyldispiro[indan-2, 2′ pyrrolidine-3′,2″-indan]-1,3,1″-trione (4b) was found to be the most active with MIC of 0.1215 and 5.121 μM, respectively. © 2012 Elsevier Ltd. All rights reserved. Source


Wei A.C.,Universiti Sains Malaysia | Ali M.A.,Universiti Sains Malaysia | Ali M.A.,New Drug Discovery Research | Ali M.A.,SunRise University | And 4 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2013

A series of fourteen dispiropyrrolidines were synthesized using [3+2]-cycloaddition reactions and were screened for their antimycobacterial activity against Mycobacterium tuberculosis H37Rv in HTS (High Throughput Screen). Most of the compounds showed moderate to good activity with MIC of less than 20 μM. Compound 4′-(4-bromophenyl)-1′- methyldispiro[acenaphthylene-1,2′-pyrrolidine-3′,2″-indane]-2, 1″(1H)-dione (4c) was found to be the most active with MIC of 12.50 μM. © 2012 Elsevier Ltd. All rights reserved. Source


Yoon Y.K.,Universiti Sains Malaysia | Ali M.A.,Universiti Sains Malaysia | Ali M.A.,New Drug Discovery Research | Ali M.A.,SunRise University | And 5 more authors.
Bioorganic and Medicinal Chemistry | Year: 2014

A total of 15 novel benzimidazole derivatives were designed, synthesized and evaluated for their SIRT1 and SIRT2 inhibitory activity. All compounds showed better inhibition on SIRT2 as compared to SIRT1. Among these, compound 5j displayed the best inhibitory activity for SIRT1 (IC50 = 58.43 μM) as well as for SIRT2 (IC50 = 45.12 μM). Cell cytotoxicity assays also showed that compound 5j possesses good antitumor activity against two different cancer cell lines derived from breast cancer (MCF-7 and MDA-MB-468). A simple structure-activity-relationship (SAR) study of the newly synthesized benzimidazole derivatives was also discussed. © 2013 Elsevier Ltd. All rights reserved. Source


Sivakumar S.,Madurai Kamaraj University | Ranjith Kumar R.,Madurai Kamaraj University | Ashraf Ali M.,Universiti Sains Malaysia | Ashraf Ali M.,New Drug Discovery Research | And 2 more authors.
European Journal of Medicinal Chemistry | Year: 2013

The 1,3-dipolar cycloaddition of azomethine ylides generated in situ from acenaphthenequinone and α-amino acids viz. 1,3-thiazolone-4-carboxylic acid and piperidine-2-carboxylic acid to a series of 1-methyl-3,5-bis[(E)- arylmethylidene]tetrahydro-4(1H)-pyridinones afforded novel spiro[5.2″] acenaphthene-1″-onespiro[6.3′]-5′-arylmethylidene-1′- methylpiperidin-4′-one-7-aryltetrahydro-1H-pyrrolo[1,2-c] [1,3]thiazoles and spiro[2.2″]acenaphthene-1″-onespiro[3.3′]-5′- arylmethylidene-1′-methylpiperidin-4′-one-4- aryloctahydroindolizines respectively in quantitative yields. These compounds were evaluated for their AChE inhibitory activity and compound 3c was found to be the most potent with IC50 1.86 μmol/L. © 2013 Elsevier Masson SAS. All rights reserved. Source

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