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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.,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.


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 | 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.

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