@article{Mejai_Rakotoarivelo_Najahi_Perio_Hollande_Pasca_Abidi_Nepveu_2019, title={The Clitocybins and 2-Substituted-Isoindolin-1-Ones: Synthesis and in Vitro Antimycobacterial Activities}, volume={16}, url={https://rajpub.com/index.php/jac/article/view/8476}, DOI={10.24297/jac.v16i0.8476}, abstractNote={<p>Despite strong indications of antimycobacterial activities for clitocybins reported since 1945, no reports linking chemical structure and activity have been reported in the literature since then. In this study, we synthesized some clitocybin derivatives (also called 2-substituted-isoindolinones), and tested their activities and carried out some chemical derivations. Isoindolinones were prepared from methyl 2-formyl-3,5-dimethoxybenzoate and various primary aromatic amines. Compounds were evaluated for <em>in vitro</em> activity against <em>Mycobacterium tuberculosis </em>H<sub>37</sub>Rv, as well as for cytotoxicity (CC<sub>50</sub>) on the Vero cell line. 4,6-dihydroxy-2-(4-hydroxyphenyl)isoindolin-1-one, <strong>7</strong>, and 4-hydroxy-2-(4-hydroxyphenyl)-6-methoxy-isoindol-1-one, <strong>5</strong>, exhibited the highest antimycobacterial activities (minimum inhibitory concentration = 19.45 µM and 18.45 µM, respectively) and were non-toxic (CC<sub>50</sub> = 30 µM and 29 µM, respectively).</p>}, journal={JOURNAL OF ADVANCES IN CHEMISTRY}, author={Mejai, Amani and Rakotoarivelo , Nambinina V. and Najahi , Ennaji and Perio , Pierre and Hollande, Etienne and Pasca, Maria Rosalia and Abidi, Rym and Nepveu , Françoise}, year={2019}, month={Oct.}, pages={5387–5394} }