title: Anti-inflammatory, anti-bacterial activity and structure-activity relationships of substitutions on 4-thiazolidinone derivatives - Part-1.
abstract: Environmentally benign and economically feasible procedures have been adopted for the synthesis of novel biologically potential 4-thiazolidinone derivatives. Purpose built microwave oven and ionic liquids (PTCs) showed wrack improvements in yield, time and cost. The yield of 1st series (01-08) obtained in the ranged from 82.4-94.2% and for 2nd series (09-16) obtained 80.6-92.8%. The compounds (01-16) were applied for anti-inflammatory activity at concentrations of 0.5 and 01 mg/kg in carrageenan induced acute and formalin induced chronic inflammatory procedures in mice and better results were obtained at 0.5 mg/kg dose. Some of the compounds 03, 04, 07, 12, 13 showed remarkable anti-inflammatory activity in both procedures as compared to the standard reference drug 2-(2,6-dichloranilino) phenyl acetic acid (diclofenac). Particularly compound 12 and 13 may be used as a non-steroidal anti-inflammatory drug (NSAID) to reduce inflammation. The compounds (01-16) were screened for their antimicrobial activity (in-vivo) and found that the compounds 12, 13 and 14 exhibited comparable or higher antibacterial activity then ciprofloxacin (standard) against E. coli, S. enteritidis, P. aeruginosa, S. aureus and B. subtilis. The compounds of series-2 showed significant activity as compared with ciprofloxacin. These compounds could be lead to the selection and use as efficient antimicrobial agents, especially for the treatment of multi-drug resistant infections.
authors.affiliation: Applied Chemistry Research Center, PCSIR Labs Complex, Lahore, Pakistan. chmnaeem32@yahoo.com
authors.forename: Muhammad
authors.initials: M
authors.lastname: Naeem
authors.forename: Muhammad Nawaz
authors.initials: MN
authors.lastname: Chadhury
authors.forename: Rana
authors.initials: R
authors.lastname: Amjad
authors.forename: Salma
authors.initials: S
authors.lastname: Rehaman
authors.forename: Kahlida
authors.initials: K
authors.lastname: Khan
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects* / Q000254:growth & development; D002351:Carrageenan; D004195:Disease Models, Animal; D052978:Disk Diffusion Antimicrobial Tests; D005557:Formaldehyde; D007249:Inflammation / Q000139:chemically induced / Q000517:prevention & control*; D008297:Male; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D053778:Thiazolidines / Q000138:chemical synthesis / Q000494:pharmacology*; D013997:Time Factors
chemical_list: D000900:Anti-Bacterial Agents; D000893:Anti-Inflammatory Agents; D053778:Thiazolidines; D005557:Formaldehyde; D002351:Carrageenan