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  3. Synthesis and antiplasmodial activity of novel indoleamide derivatives bearing sulfonamide and triazole pharmacophores

Synthesis and antiplasmodial activity of novel indoleamide derivatives bearing sulfonamide and triazole pharmacophores

  • Eur J Med Chem. 2017 May 5:131:171-184. doi: 10.1016/j.ejmech.2017.03.010.
N Devender 1,  Sarika Gunjan 2,  Renu Tripathi 3,  Rama Pati Tripathi 4
Affiliations

Affiliations

  • 1 Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow, 226031, India.
  • 2 Parasitology Division, CSIR-Central Drug Research Institute, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), New Delhi, 110001, India.
  • 3 Parasitology Division, CSIR-Central Drug Research Institute, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), New Delhi, 110001, India. Electronic address: renu1113@rediffmail.com.
  • 4 Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), New Delhi, 110001, India. Electronic address: rpt.cdri@gmail.com.
PMID: 28319782 DOI: 10.1016/j.ejmech.2017.03.010
Abstract

Due to the recent reports of growing Parasite resistance to artemisinins and Other antimalarial drugs, development of new antimalarial chemotypes is an urgent priority. Here in, we report a novel series of adamantyl/cycloheptyl indoleamide derivatives bearing sulfonamide and triazole pharmacophores adopting different chemical modifications and evaluated them for antiplasmodial activity in vitro. Among all the indoleamides, compounds 22, 24, 26 and 30 with sulfonamide pharmacophore showed promising activity with IC50 of 1.87, 1.93, 2.00, 2.17 μM against CQ sensitive Pf3D7 strain and 1.69, 2.12, 1.60, 2.19 μM against CQ resistant PfK1 strain, respectively.

Keywords

Antiplasmodial activity; Indoleamide; Sulfonamide; Triazole.

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