Sulphonamides synthesis and antibacterial activity


Sulfonamides and trimethoprim

The 25 december 1932, the German chemical company I.G. Farbenindustrie filed a patent application on a red dye that showed a remarkable ability to cure certain kinds of bacterial infections in mice. By the time the patent was awarded just over two years later, the dye, called Prontosil, had been found to have the same therapeutic effect in humans. The discovery was published in a brief publication in a German medical journal in 1935 by Gerhard Domagk, went on the market and became available to doctors in April 1935.

In retrospect, it is clear that the introduction of Prontosil marked a turning point in the history of medicine. As the first of the compounds called sulfonamides or, more familiarly, sulfa drugs, Prontosil initiated a revolution in the therapeutics and management of bacterial infections. Within a few years, feared diseases such as streptococcal infections (including childbed fever and septicemia), pneumonia, meningitis, dysentery, gonorrhea, and urinary tract infections, were brought under a substantial measure of control by chemotherapy. The medical success of the sulfa drugs gave a powerful impetus to the expansion of the international pharmaceutical industry and of the research and development enterprise within it. The same success contributed heavily to the opening of what was widely referred to as an era of miracle drugs, with its attendant optimism and raised expectations of medicine, accelerated appearance of new medicines as a result of increased levels of research, regulatory dilemmas, and unanticipated therapeutic problems. Finally, the sulfa drugs proved extraordinarily fruitful as starting points for molecular modifications that led to new drugs or classes of drugs not only for bacterial infections (eventually including tuberculosis) but also for leprosy (Hansenís disease), diabetes, hyperthyroidism, gout, heart disease, and hypertension. The reach of research based on the sulfa drugs extended beyond human into veterinary medicine and even to the discovery of new herbicides.

The sulphonamides represent a pivotal moment in the history of medicine. They are a result of the first major phase of the industrialization of pharmaceutical innovation, and the event that started the second great phase of that process and that is continuing in our time. Those who witnessed the introduction of the sulphonamides into medicine recognized that a major revolution was under way. F. Sherwood Taylor, in 1942 wrote a book entitled "The Conquest of Bacteria: From Salvarsan to Sulphapyridine" describing the sulphonamides as the successful result of the research carried out by Ehrlich and ultimately of the bacteriology and
synthetic organic chemistry of the late nineteenth century.


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