Synthesis, computational, and biological evaluation of novel indolophenyl carboxamides as potential antimalarial agents

Compounds 1, 7, 8, and 9 showed potent antimalarial activity against Pf3D7 and Pf C580Y with IC<sub>50</sub> values of 8.9 and 3.4 µM, 5.5 and 2.2 µM, 10.1 and 14.0 µM, and 12.2 and 28.6 µM, respectively, and were nontoxic to human cells. Further, in silico studies confirmed Plasmodium dihydrofolate reductase as the target of indolophenyl carboxamides. This study identifies indolophenyl carboxamides, including bisindole, as promising new antimalarial agents effective against sensitive and drug-resistant <i>P. falciparum</i>.

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Journal
Future Medicinal Chemistry
Published
2025-10-18
DOI
https://doi.org/10.1080/17568919.2025.2575755
Primary Topic
Computational Drug Discovery Methods
Type
article
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article

Synthesis, computational, and biological evaluation of novel indolophenyl carboxamides as potential antimalarial agents

Gautam Kumar, Priya Mondal, Kapil Vashisht, N. K. Tiwari et al.
Future Medicinal Chemistry
Computational Drug Discovery Methods
article

Synthesis, computational, and biological evaluation of novel indolophenyl carboxamides as potential antimalarial agents

Gautam Kumar, Priya Mondal, Kapil Vashisht, N. K. Tiwari, Asha Kiran Tudu, Rahul Kumar, Kailash C. Pandey, Priyanka Rani, Supriya Sharma, Tanish
article en

Abstract

Compounds 1, 7, 8, and 9 showed potent antimalarial activity against Pf3D7 and Pf C580Y with IC<sub>50</sub> values of 8.9 and 3.4 µM, 5.5 and 2.2 µM, 10.1 and 14.0 µM, and 12.2 and 28.6 µM, respectively, and were nontoxic to human cells. Further, in silico studies confirmed Plasmodium dihydrofolate reductase as the target of indolophenyl carboxamides. This study identifies indolophenyl carboxamides, including bisindole, as promising new antimalarial agents effective against sensitive and drug-resistant <i>P. falciparum</i>.

Future Medicinal ChemistryVol. 17(22)
National Institute of Pharmaceutical Education and Research - Ahmedabad (IN), National Institute of Pharmaceutical Education and Research (IN), Birla Institute of Technology and Science, Pilani (IN), National Institute of Malaria Research (IN)
Openalex Percentile: Top 69%
Computational Drug Discovery Methods
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Synthesis, computational, and biological evaluation of novel indolophenyl carboxamides as potential antimalarial agents — Gautam Kumar, Priya Mondal, et al. · Future Medicinal Chemistry (2025) | TGRS Research Map | TGRS