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Synthesis and evaluation of novel 2,2-dimethylthiochromanones as anti-leishmanial agents

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posted on 30.07.2021, 15:53 by Sean Coll, Mohammad Alhazmi, Patricia de Aguiar Amaral, Sandra Bourgeade-Delmas, Anne-Cécile Le Lamer, James BarlowJames Barlow
Within this work, we describe the design and synthesis of a range of novel thiochromanones based on natural products reported to possess anti-leishmanial action, and their synthetic derivatives. All compounds were elaborated via the key intermediate 2,2,6-trimethoxythiochromanone, which was modified at the benzylic position to afford various ester, amine and amide analogues, substituted by chains of varying lipophilicity. Upon testing in Leishmania, IC values revealed the most potent compounds to be phenylalkenyl and haloalkyl amides 11a and 11e, with IC values of 10.5 and 7.2 µM, respectively.

Funding

CAPES-CSF-PVE-S (Programa Pesquisador Visitante Especial) Processo: 88881.064993/2014-01.

History

Comments

The original article is available at https://www.mdpi.com/

Published Citation

Coll S, Alhazmi M, de Aguiar Amaral P, Bourgeade-Delmas S, Le Lamer AC, Barlow JW. Synthesis and evaluation of novel 2,2-dimethylthiochromanones as anti-leishmanial agents. Molecules. 2021 12;26(8):2209.

Publication Date

12 Apr 2021

PubMed ID

33921252

Department/Unit

  • Chemistry

Research Area

  • Chemistry and Pharmaceutical Sciences

Publisher

MDPI AG (Multidisciplinary Digital Publishing Institute)

Version

  • Published Version (Version of Record)