Recent advances in chemotherapy have been of great benefit in the treatment of infections of the urinary tract. Research in chemotherapeutic agents, especially the sulfonamide compounds, is progressing rapidly. It has been our privilege to have under clinical investigation one of these drugs—sulfacetimide-Schering1 (p-amino- benzene - sulfonyl- acetyl -imide)—which we have used with good results in the treatment of more than 200 cases of infections of the urinary tract due to the colon-aerogenes group of organisms.
In the vast amount of experimental work on sulfanilamide, it was found that it was acetylated in its passage through the body. This acetylation occurs at the amino group in the para position. Vonkennel and Korth2 found that sulfanilamide when acetylated at this particular position became nontoxic but completely lost its therapeutic value.
In an effort to develop a compound which would still be relatively nontoxic yet hold its therapeutic effectiveness in the body, Dohrn and Diedrich3 succeeded in removing one of the hydrogen atoms of the sulfonamide group and placing the acetyl group in this position. The structural formula is:
WELEBIR F, BARNES RW. THE USE OF SULFACETIMIDE IN BACILLARY INFECTIONS OF THE URINARY TRACT. JAMA. 1941;117(25):2132-2135. doi:10.1001/jama.1941.02820510020005