Hina Siddiqui
1H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan
Title: Sulphamethazine Derivatives as Immunomodulating Agents: New Therapeutic Strategies for Inflammatory Diseases
Biography
Biography: Hina Siddiqui
Abstract
Sulfamethazine (SMZ) (1) is an antibacterial sulfur drug which suppresses the dihydrofolic acid synthesis. It is used for the treatment of infections in livestock; such as gastrointestinal, and respiratory tract infections. During the current study, synthesis and characterization of sulfamethazine (SMZ) derivatives 3–39 were achieved. They were synthesized by the reaction of sulfamethazine with a range of acid chlorides. All the compounds were characterized by spectroscopic techniques, such as 1H-, 13C-NMR, EI-MS and HRFAB-MS. Among their compounds 3-10, 14, and 15 were identified as new analogues. These compounds were not previously reported for their immunomodulatory activities. In this study, immunomodulatory effect of compounds 3-39 on different parameters of innate immune response were examined, including effect on production of intracellular reactive (ROS) from human whole blood and isolated polymorphonuclear neutrophils (PMNs), nitric oxide (NO), and pro-inflammatory cytokine TNF-α. All the new compounds except 14 and 15 showed a promising anti-inflammatory activity. The compounds 3–39 were also evaluated for their cytotoxicity against the normal mouse fibroblast NIH-3T3 cell line. All the compounds were found to be non-cytotoxic.