R. R. Roepke, T. Maren, E. Mayer
Oct 1, 1957
Citations
0
Influential Citations
30
Citations
Journal
Annals of the New York Academy of Sciences
Abstract
Of a series of sulfanilamidopyridazines synthesized by Clark et al.,I Kynext sulfamethoxypyridazine (3-sulfanilamido-6-methoxypyridazine) appeared to be of particular interest because of a combination of adequate solubility and antibacterial activity combined with a low rate of urinary excretion. The structure of sulfamethoxypyridazine (SPIIP) is shown in FIGURE 1. The solubilities of the compound and its N4-acetyl derivative are listed in TABLE 1, with similar data for sulfadiazine and sulfisoxazole. Standardized bacterial infections in mice, as described by White et ~ l . , ~ were used by Kuck4 to compare the antibacterial potency of SAIP with that of sulfadiazine. In the treatment of pneumococcal, streptococcal, and Pasleurella infections, Kuck found no significant difference in the potency of these two drugs on a basis of either blood level or oral dosage. In the Klebsiella infection, ShIP was about half as potent as sulfadiazine. This report is concerned primarily with studies on ShIP with respect to its absorption, distribution, and excretion in dogs; conjugation in rats; acute toxicity in mice and dogs; and chronic toxicity in rats and dogs.