Good news for humans – bad news for pathogens. From the first therapeutic use of penicillin in 1941 to the advent of antibacterial drugs, each newly marketed antibiotic has invariably resulted in the emergence of resistant bacterial pathogens. The emergence and spread of these unwanted life forms that have evolved mechanisms of resistance to multiple antibiotics is becoming a major threat to public health in the 21st century. The seriousness of antibiotic resistance lies in the fact that today bacterial strains are not only resistant to commonly available antibacterial medication but also may have acquired greater virulence, meaning they may have become more sinister and deadly. Therefore, the discovery and development of new antibiotics is of crucial importance to counter the explosive growth of multidrug resistant pathogens; the threat to our society is simply too big to ignore the rise of multi-drug resistance.
Worry not! One of the tributaries to the river of healthcare solutions may sprout from within SBASSE. Here’s the big idea – empowering drugs with Fluorine. One way to improve the efficiency of drugs is to introduce fluorine (or fluorinated groups) in the drug molecule. The incorporation of fluorine into a drug molecule can lead to improved metabolic stability, bioavailability, as well as more efficient binding when compared to the non-fluorinated counterparts. Consequently, about a quarter of all pharmaceuticals on the market contain fluorine, and almost all new drug candidates have fluorine in them in one form or the other. Commonly used fluorinated drugs include ciprofloxacin (antibiotic) and fluconazole (antifungal), the former selling like hot cakes in the months leading to winter.
In Pakistan, bacterial infection is very common and mortality rate is increasing. Unfortunately, we are totally dependent on other countries for the solution of our health-related problems. There is dire need to develop international quality synthetic medicinal chemistry research infrastructure in Pakistan to come up with indigenous solutions to our health problems, and to remove our dependence on foreign countries.
Sulfonamides (-SO2NH-) containing compounds such as cyanobenzenesulphonamide, and methylbenzene sulphonamide are synthetic antibacterial compounds that are generally wide-spectrum drugs active against a range of Gram-positive and Gram-negative bacteria. In this proposal, Dr. Ghayoor Abbas and Dr. Shaper Mirza, a research team from LUMS; and Dr. Tariq, from Shalimar Institute of Health Sciences will investigate the use of novel fluorinated sulphonamides as potential antibiotics for killing resistant strains of uropathogenic Escherichia coli (UPEC) and Staphylococcus aureus. A series of novel sulfonamides will be synthesized via SuFEx chemistry route from sulfonyl fluorides and will be evaluated for their antimicrobial activity using in vitro antibacterial assays. Minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) will also be determined.
This was certainly a million-rupee idea – quite literally. The Shahid Hussain Foundation has very generously awarded a fund of PKR 1.2 million for the development of this study. We congratulate all the researchers involved and wish them best of luck for their work. May the force of progress be with them.
