Synthesis and antimalarial activity of novel chiral and achiral benzenesulfonamides bearing 1, 3, 4-oxadiazole moieties.
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.
Zareef
Muhammad
M
Department of Chemistry, Quaid-i-Azam University, Islamabad 45320, Pakistan. mkzareef@yahoo.com
Iqbal
Rashid
R
De Dominguez
Neira Gamboa
NG
Rodrigues
Juan
J
Zaidi
Javid H
JH
Arfan
Muhammad
M
Supuran
Claudiu T
CT
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D003460:Crystallization; D004353:Drug Evaluation, Preclinical; D006454:Hemoglobins / Q000737:chemistry / Q000187:drug effects; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008288:Malaria / Q000188:drug therapy / Q000469:parasitology; D008297:Male; D051379:Mice; D010069:Oxadiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D010962:Plasmodium berghei; D021241:Spectrometry, Mass, Electrospray Ionization; D013055:Spectrophotometry, Infrared; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000962:Antimalarials; D006454:Hemoglobins; D010069:Oxadiazoles; D013449:Sulfonamides