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

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:

Published: July 2018

AI Article Synopsis

Article 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 IC values 1.27, 1.64 and 1.96 μM, respectively against CQ sensitive Pf3D7 strain while compounds 7b and 6f showed good activity with IC 1.61 and 1.93 μM, respectively against CQ resistant PfK1 strain.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejmech.2018.06.042DOI Listing

Publication Analysis

Top Keywords

antiplasmodial activity
8
glycosylated 123-triazolyl-methyl-indoline-23-diones
8
synthesis antiplasmodial
4
activity
4
activity glyco-conjugate
4
glyco-conjugate hybrids
4
hybrids phenylhydrazono-indolinones
4
phenylhydrazono-indolinones glycosylated
4
123-triazolyl-methyl-indoline-23-diones small
4
small library
4

Similar Publications

A chemical examination of a root extract of led to the isolation and identification of 23 compounds, including oxazole-type alkaloids and isoflavonoid derivatives. Notably, three oxazole-type alkaloids (, , and ) and two isoflavonoid derivatives ( and ) were obtained from a natural source for the first time. In addition, derived 2,5-diphenyloxazoles and their derivatives were synthesized.

View Article and Find Full Text PDF

Natural products (NPs) play a crucial role in drug discovery, with over 30% of recent FDA-approved drugs derived from them. Plants from the genus Goniothalamus, belonging to the Annonaceae family, have garnered significant interest as potential sources of active lead compounds. Over the past five decades, researchers have isolated 357 compounds from Goniothalamus species (GCs), which exhibit a wide range of pharmacological properties, including cytotoxicity, antibacterial, antifungal, antiplasmodial, antioxidant, and other activities.

View Article and Find Full Text PDF

Background: Malaria is one of the leading causes of morbidity and/or mortality in tropical Africa. The spread and development of resistance to chemical antimalarial drugs and the relatively high cost of the latter are problems associated with malaria control and are reasons to promote the use of plants to meet healthcare needs to treat malaria. The aim of this study was to evaluate antiplasmodial activities of extracts of (Mah quat), which is traditionally used for the treatment of malaria in the western region of Cameroon.

View Article and Find Full Text PDF

Bioactive Sulfonamides Derived from Amino Acids: Their Synthesis and Pharmacological Activities.

Mini Rev Med Chem

January 2025

Department of Physiology and Pharmacology Vittorio Erspamer, Sapienza University of Rome, 00161, Rome, Italy.

Currently, the synthesis of bioactive sulfonamides using amino acid as a starting reagent has become an area of research interest in organic chemistry. Over the years, an amine-sulfonyl chloride reaction has been adopted as a common step in traditional sulfonamide synthetic methods. However, recent developments have shown amino acids to be better precursors than amines in the synthesis of sulfonamides.

View Article and Find Full Text PDF

In this study, we built on the known inhibitory potential of diaminoquinazolines (DAQs) against different stages of Plasmodium development and designed a convenient two-step synthesis to combine DAQ with the primaquine (PQ) pharmacophore. The PQ-DAQ hybrids displayed potent in vitro activities in the low nanomolar range (IC50 of 135.20-398.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!