2. Academic Validation
  3. Synthesis and antiplasmodial activity of glyco-conjugate hybrids of phenylhydrazono-indolinones and glycosylated 1,2,3-triazolyl-methyl-indoline-2,3-diones

Synthesis and antiplasmodial activity of glyco-conjugate hybrids of phenylhydrazono-indolinones and glycosylated 1,2,3-triazolyl-methyl-indoline-2,3-diones

  • Eur J Med Chem. 2018 Jul 15:155:764-771. doi: 10.1016/j.ejmech.2018.06.042.
Ravi Kumar Thakur 1,  Prince Joshi 2,  Pragati Baranwal 1,  Gaurav Sharma 3,  Sanjeev K Shukla 4,  Renu Tripathi 5,  Rama Pati Tripathi 6
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.
  • 3 Sophisticated Analytical Instrument Facility, CSIR-Central Drug Research Institute, Lucknow 226031, India.
  • 4 Academy of Scientific and Innovative Research (AcSIR), New Delhi 110001, India; Sophisticated Analytical Instrument Facility, CSIR-Central Drug Research Institute, Lucknow 226031, India. Electronic address: skshukla@cdri.res.in.
  • 5 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.
  • 6 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: 29940466 DOI: 10.1016/j.ejmech.2018.06.042
Abstract

A small library of 36 new glycohybrids of phenylhydrazono-indolinones was synthesized employing glycosylated 1,2,3-triazolyl-methyl-indoline-2,3-diones and different phenylhydrazines via acid catalyzed reaction. All the compounds were screened for their antiplasmodial activity in vitro. Compounds 6c, 7c, and 7b showed significant activity with the IC50 values 1.27, 1.64 and 1.96 μM, respectively against CQ sensitive Pf3D7 strain while compounds 7b and 6f showed good activity with IC50 1.61 and 1.93 μM, respectively against CQ resistant PfK1 strain.

Keywords

Antiplasmodial activity; Glycosylation; Hydrazones; Isatin; Triazole.

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