Students from different academic backgrounds are an important part of our Nano-Biosensors for Diagnostics and Healthcare research group. They bring new ideas and diverse perspectives that support our work in developing innovative biosensing technologies for improved disease detection and healthcare solutions. Their involvement encourages collaboration and helps translate research into real-world impact for both local communities and global health.
3- DESIGN AND SYNTHESIS OF NOVEL COX-2 SELECTIVE INHIBITORS
By
Aseel Khaled Mohd Nawafleh
Supervisor
Dr. Ghadeer Abdul Rahman Suaifan, Prof.
Co-Supervisor
Dr. Mayaddah Bashir Shehadeh, Prof.
ABSTRACT
NSAIDs have been widely used in the treatment of inflammation, but limited NSAIDs clinical usefulness attributed to their adverse effects forced medicinal chemists to focus on synthesizing newer derivatives. This work implemented the design and synthesis of glycosylated-based NSAIDs carboxamide mefenamic acid and tolmetin derivatives with the aim of enhancing specificity, overcoming GI side effects and obtaining inexpensive anti-inflammatory agents. Novel glycosylated NSAID carboxamides were designed and synthesized using a simple synthetic pathway. Synthesized compounds were screened for anti-inflammatory using carrageenan-induced paw edema model.
Results revealed that novel compounds exhibited good anti-inflammatory activity against edema formation. The results revealed that the combination of 1,3,4,6-O-acetyl-D-(+)-glucosamine moiety with NSAIDs by amidation did not potentiate parent drug anti-inflammatory activity. On the other hand, derivatization of their carboxylic acid group with the bulky 1,3,4,6-O-propyl-D-(+)-glucosamine moiety obliterates analogue anti-inflammatory activity.
4- DESIGN, SYNTHESIS, AND BIOLOGICAL EVALUATION OF NOVEL CIPROFLOXACIN-SULFONAMIDE CONJUGATES INVOLVING UREA LINKERS
ByDoha Ali Ibrahim Al-Omari SupervisorDr. Ghadeer Abdul Rahman Suaifan, Prof Co-SupervisorDr. Mayaddah Bashir Shehadeh, Prof
ABSTRACT
Antimicrobial resistance poses a significant challenge to global health and economy, adding complexity to the management of infections. Accordingly, there is a rising interest in the creation of conjugates that combine diverse pharmacological characteristics to tackle antibacterial resistance. In this study, we outline the design, synthesis, and biological evaluation of ciprofloxacin-sulfonamide conjugates, incorporating a urea linker, possessing dual functionality as urease inhibitor and potential antibacterial agents. A set of novel substituted arylsulfonylurea-ciprofloxacin conjugates were synthesized.
The reaction of arylsulfonamides with diphenyl carbonate and 4-dimethylaminopyridine resulted in the formation of either phenyl N-(2,4-arylsulfonyl)carbamate 4-dimethylaminopyridinium salts or N-(4-arylsulfonyl)-4-dimethylaminopyridinium-1-carboxamide salts, based on the substitution on the arylsulfonamide. Both categories of intermediates led to the formation of aryl sulfonylurea-ciprofloxacin conjugate (5a-h) when reacted with ciprofloxacin.
The antimicrobial activity of the novel compounds was evaluated in vitro against various gram positive pathogens as staphylococcus aureus (S. aureus) and gram negative pathogens as Helicobacter pylori (H. Pylori) and Escherichia coli (E. coli). Results highlighted conjugate's growth inhibitory activity with minimum inhibitory concentration (MIC) values ranging from 0.625-5 µM against S. aureus ATCC 25923; 1.25-5 µM against methicillin-resistant S. aureus ATCC 3359; 2.5-6.25 µM against H. Pylori NCTC 11638; 0.025-0.05 µM against E. coli NCTC 11954; 0.05 µM against the food poisoning E.coli O157: H7, compared to ciprofloxacin (MIC = 0.05-0.625 µM) against all tested bacteria. Additionally, the arylsulfonylurea conjugates exhibited inhibitory characteristics against jack-bean urease, with half maximal inhibitory concentration (IC50) values varying from 31 to 72 µM, compared to the positive control thiourea (IC50 = 180 µM). Accordingly, it could be proposed that the attachment of sulfonamide via a urea linkage on the 7-position of ciprofloxacin provided analogues with antibacterial and urease inhibitory activity.