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Synthesis and antimalarial activity of novel chiral and achiral benzenesulfonamides bearing 1, 3, 4-oxadiazole moieties

descriptionPublicationkeyboard_double_arrow_right Article 01 Jan 2007 Italy English Publisher:Informa UK LimitedJournal:Journal of Enzyme Inhibition and Medicinal Chemistry, volume 22, pages 301-308 (issn: 1475-6366, eissn: 1475-6374,

Authors: M. Zareef; R. Iqbal; N. G. De; J. Rodrigues; J. H. Zaidi; M. Arfan; SUPURAN, CLAUDIU TRANDAFIR;

doi: 10.1080/14756360601114569

pmid: 17674812

handle: 2158/776037

Synthesis and antimalarial activity of novel chiral and achiral benzenesulfonamides bearing 1, 3, 4-oxadiazole moieties

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Abstract

A series of new benzenesulfonamides, most of which are chiral, incorporating 1, 3, 4-oxadiazole and amino acid moieties have been synthesized. Some of these compounds were screened for antimalarial activity and also evaluated for their ability to inhibit hem polymerization. The electrophoretic analysis indicated that one compound was effective in inhibiting the degradation of hemoglobin. The synthesized compounds were tested in mice infected with Plasmodium berghei. These derivatives have the potential for the development of novel antimalarial lead compounds.

Country

Italy

Related Organizations

Università degli studi di Salerno
Italy
University of Florence
Italy
Quaid-i-Azam University
Pakistan
Central University of Venezuela
Venezuela
National Institute for Nuclear Physics
Italy

Keywords

Pharmacology, Male, Oxadiazoles, Spectrometry, Mass, Electrospray Ionization, Sulfonamides, Magnetic Resonance Spectroscopy, Spectrophotometry, Infrared, Plasmodium berghei, Drug Evaluation, Preclinical, Animals, Antimalarials; chemical synthesis/chemistry/pharmacology, Crystallization, Drug Evaluation; Preclinical, Hemoglobins; chemistry/drug effects, Magnetic Resonance Spectroscopy, Malaria; drug therapy/parasitology, Male, Mice, Oxadiazoles; chemical synthesis/chemistry/pharmacology, Plasmodium berghei, Spectrometry; Mass; Electrospray Ionization, Spectrophotometry; Infrared, Stereoisomerism, Structure-Activity Relationship, Sulfonamides; chemical synthesis/chemistry/pharmacology, Stereoisomerism, General Medicine, In Vitro Techniques, Malaria, Antimalarials, Hemoglobins, Mice, Structure-Activity Relationship, Drug Discovery, Animals, Crystallization

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	influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).	Top 10%
	impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.	Top 10%