Synthesis of n-(Heteroaryl Substituted) Benzene Sulphonamides and their Biological Activities

Synthesis of n-(Heteroaryl Substituted) Benzene Sulphonamides and their Biological Activities

Abstract

The synthesis of N-heteroaryl substituted benzene sulphonamides and evaluation of their biological activities are reported. Synthesis was achieved by the reaction of benzene sulphonyl chloride and substituted amino heterocycle in dry pyridine. The structures of synthesized compounds were assigned by spectroscopic methods. The eight (8) synthesized compounds were evaluated for antibacterial and antifungal activities. The results showed that some of the new compounds exhibited activities comparable to ciprofloxacin and ketoconazole. Acute toxicity (LD50) of the synthesized samples was carried out. Malaria parasitaemia was inoculated in the mice using parasitized blood from infected mice. The synthesized compounds were used at dose 2000 mg/kg body weight of mice. The antioxidant effects were determined using the antioxidant enzymes: superoxide dismutase (SOD), catalase and glutathione. Some of the new compounds displayed significant antioxidant properties. The parameters; alanine aminotransferase (ALT) and aspartate aminotransferase (AST) enzymes activities were used for liver function test while serum urea and creatinine tests were used as markers for renal function. The results of the activities of the synthesized compounds showed appreciable inhibition of the growth of test organism. The liver and kidney function tests showed improved activity when compared with the positive control.