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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.


Ahsan M.J.,New Drug Discovery Research | Ahsan M.J.,Jaipur National University | Samy J.G.,New Drug Discovery Research | Khalilullah H.,New Drug Discovery Research | And 2 more authors.
European Journal of Medicinal Chemistry | Year: 2011

In the present investigation, a series of 3a,4-dihydro-3H-indeno [1,2-c] pyrazole-2-carboxamide analogues were synthesized and were evaluated for antitubercular activity by two fold serial dilution technique. All the newly synthesized compounds showed low to good inhibitory activities against Mycobacterium tuberculosis H 37Rv and multi-drug resistant M. tuberculosis (MDR-TB). 3-(4-fluorophenyl)-N-(4-chlorophenyl)-6,7-dimethoxy-3a,4- dihydro-3H-indeno [1,2-c] pyrazole-2-carboxamide (4c) was found to be the most promising compound active against M. tuberculosis, H 37Rv and MDR-TB with minimum inhibitory concentrations 0.83 μM and 3.32 μM respectively. © 2011 Elsevier Masson SAS. All rights reserved.


Ahsan M.J.,New Drug Discovery Research | Ahsan M.J.,NIMS University
Letters in Drug Design and Discovery | Year: 2012

A series of 3-substituted-N-aryl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2- c]pyrazole-2-carboxamide analogues were synthesized and characterized by IR, NMR and elemental analysis. All the compounds were screened for anticancer activity as per National Cancer Institute (NCI US) Protocol on leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate and breast cancers cell lines. The compound 3-(4-fluorophenyl)-N-(2,6-dimethylphenyl)-6,7-dimethoxy-3a,4-dihydro- 3H-indeno[1,2-c]pyrazole-2-carboxamide (4h) was found to be the most active compound of the series highly active on Leukemia K-562 and SR cell line [Growth Percent (GP) = 26.95 and 33.45 respectively]. The molecular docking mode for compound, 3-(4-Fluorophenyl)-N-(2,6-dimethylphenyl)-6,7-dimethoxy-3a,4-dihydro- 3H-indeno[1,2-c]pyrazole-2-carboxamide (4h) showed efficient binding with EGFR tyrosine kinase. © 2012 Bentham Science Publishers.


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.


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.


Ahsan M.J.,New Drug Discovery Research | Ahsan M.J.,Jaipur National University | Samy J.G.,New Drug Discovery Research | Khalilullah H.,New Drug Discovery Research | And 4 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2011

In the present investigation, a series of 1,5-dimethyl-2-phenyl-4-{[(5- aryl-1,3,4-oxadiazol-2-yl)methyl]amino}-1,2-dihydro-3H-pyrazol-3-one were subjected to molecular properties prediction, drug-likeness by Molinspiration (Molinspiration, 2008) and MolSoft (MolSoft, 2007) software, lipophilicity and solubility parameters using ALOGPS 2.1 program. The compounds followed the Lipinski 'Rule of five' were synthesized for antimicrobial and antitubercular screening as oral bioavailable drugs/leads. Maximum drug-likeness model score (0.95) was found for compound, 4a. All the synthesized compounds were characterized by IR, NMR and mass spectral analysis followed by antimicrobial and antimycobacterial screening. Among the title compounds, compound 4d showed pronounced activity against Mycobacterium tuberculosis H37Rv and isoniazid resistant M. tuberculosis (INHR-TB) with minimum inhibitory concentrations (MICs) 0.78 μM and 1.52 μM, respectively. The compound, 4a showed maximum activity against all bacterial strains with MIC 4-8 μg/mL comparable to standard drug ciprofloxacin, while the compounds, 4e and 4k showed maximum antifungal activity with MIC 8-16 μg/mL less active than standard drug fluconazole. © 2011 Elsevier Ltd. All rights reserved.


Ahsan M.J.,New Drug Discovery Research | Ahsan M.J.,Jaipur National University | Samy J.G.,New Drug Discovery Research | Dutt K.R.,Jaipur National University | And 5 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2011

In the present investigation, a series of 3-substituted-N-aryl-6,7- dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide analogues were synthesized and were evaluated for antitubercular activity by two fold serial dilution technique. All the newly synthesized compounds showed moderate to high inhibitory activities against Mycobacterium tuberculosis H 37Rv and INH resistant M. tuberculosis. The compound N,3-bis(4-fluorophenyl)-6,7- dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide (4c) was found to be the most promising compound active against M. tuberculosis H 37Rv and isoniazid resistant M. tuberculosis with minimum inhibitory concentration 0.78 μM. © 2011 Elsevier Ltd. All rights reserved.


Jeyachandran V.,Madurai Kamaraj University | Kumar R.R.,Madurai Kamaraj University | Ali M.A.,Universiti Sains Malaysia | Ali M.A.,New Drug Discovery Research | And 2 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2013

A library of novel 5-amino-2,7-diaryl-2,3-dihydrobenzo[b]thiophene-4,6- dicarbonitriles have been synthesized regioselectively in good yields through the one-pot domino reactions of 5-aryldihydro-3(2H)-thiophenones, malononitrile and aromatic aldehydes in the presence of morpholine. This transformation presumably involves Knoevenagel condensation-Michael addition-intramolecular Thorpe-Ziegler cyclization-Tautomerization-Elimination sequence of reactions. These compounds were evaluated for their acetylcholinesterase (AChE) inhibitory activity and 5-amino-2,7-bis(4-methoxyphenyl)-2,3-dihydrobenzo[b]thiophene-4,6- dicarbonitrile was found to be the most potent against AChE with IC50 4.16 μmol/L. © 2013 Elsevier Ltd. All rights reserved.


Ahsan M.J.,New Drug Discovery Research | Ahsan M.J.,Jaipur National University | Samy J.G.,New Drug Discovery Research | Jain C.B.,Rajasthan University of Health Sciences | And 3 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2012

In search of potential therapeutics for tuberculosis, we describe herewith the synthesis, characterization and antimycobacterial activity of 1,5-dimethyl-2-phenyl-4-([5-(arylamino)-1,3,4-oxadiazol-2-yl]methylamino)-1, 2-dihydro-3H-pyrazol-3-one analogues. Among the synthesized compounds, 4-[(5-[(4-fluorophenylamino]-1,3,4-oxadiazol-2-yl)methylamino]-1,2-dihydro-1, 5-dimethyl-2-phenylpyrazol-3-one (4a) was found to be the most promising compound active against Mycobacterium tuberculosis H 37Rv and isoniazid resistant M. tuberculosis with minimum inhibitory concentrations, 0.78 and 3.12 μg/mL, respectively, free from any cytotoxicity (>62.5 μg/mL). © 2011 Elsevier Ltd. All rights reserved.


Ashraf Ali M.,Universiti Sains Malaysia | Ismail R.,Universiti Sains Malaysia | Choon T.S.,Universiti Sains Malaysia | Kumar R.S.,Universiti Sains Malaysia | And 5 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2012

Pyrrolothiazolyloxindole analogues share vital pharmacological properties, considered useful in Alzheimer's disease (AD). The aim of this study was synthesis and evaluate pyralothiazolyloxindole analogues if possess acetyl cholinesterase (AChE) inhibitory activity. The easily accessible one-pot synthesis of these compounds resulted to be significantly less difficult and expensive than that of donepezil. Several compounds possess anti-cholinesterase activity in the order of micro and sub-micromolar. Particularly, compound 6a was the most potent inhibitors of the series against acetyl cholinesterase enzyme with IC 50 0.11 μmol/L. © 2011 Elsevier Ltd. All rights reserved.

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