Literature DB >> 20206517

Comparison of the antiplasmodial and falcipain-2 inhibitory activity of beta-amino alcohol thiolactone-chalcone and isatin-chalcone hybrids.

Renate H Hans1, Jiri Gut, Philip J Rosenthal, Kelly Chibale.   

Abstract

The synthesis and biological evaluation of two novel series of natural-product-like hybrids based on the chalcone, thiolactone and isatin scaffolds is herein described. Results for a 36-member beta-amino alcohol triazole library showed that the thiolactone-chalcones, with IC(50)s ranging from 0.68 to 6.08 microM, were more active against W2 strain Plasmodium falciparum than the isatin-chalcones with IC(50)s of 14.9 microM or less. Also of interest is falcipain-2 inhibitory activity displayed by the latter, whereas the thiolactone-chalcones lacked enzyme inhibitory activity. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20206517     DOI： 10.1016/j.bmcl.2010.02.017

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  8 in total

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6.  Virtual design of novel Plasmodium falciparum cysteine protease falcipain-2 hybrid lactone-chalcone and isatin-chalcone inhibitors probing the S2 active site pocket.

Authors:  Koffi N'Guessan Placide Gabin Allangba; Mélalie Keita; Raymond Kre N'Guessan; Eugene Megnassan; Vladimir Frecer; Stanislav Miertus
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7.  β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: synthesis and antimalarial evaluation.

Authors:  Jiri Gut; Philip J Rosenthal; Vipan Kumar
Journal:  Eur J Med Chem       Date:  2014-07-21       Impact factor: 6.514

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  8 in total

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