3485. Ebrotidine

Nomenclature

CAS number: 100981-43-9
[N(E)]-N-[[[2-[[[2-[(Aminoiminomethyl)amino]-4-thiazolyl]methyl]thio]ethyl]amino]methylene]-4-bromobenzenesulfonamide; (E)-N-p-bromobenzenesulfonyl-N′-[2-[[[2-[(aminoiminomethyl)amino]-4-thiazolyl]methyl]thio]ethyl]formamidine; p-bromo-N-[(E)-[[2-[[[2-[(diaminomethylene)amino]-4-thiazolyl]methyl]thio]ethyl]amino]methylene]benzenesulfonamide; FI-3542; Ebrocit (Ferrer); Ebrodin (Ferrer); Ulsanic (Ferrer).
C14H17BrN6O2S3; mol wt 477.42.
C 35.22%, H 3.59%, Br 16.74%, N 17.60%, O 6.70%, S 20.15%.

Description and references

Histamine H2-receptor antagonist. Prepn: R. Foguet et al., EP 159012; eidem, US 4728655 (1985, 1988 both to Ferrer); L. Anglada et al., Eur. J. Med. Chem. 23, 97 (1988). Clinical pharmacology: S. J. Konturek et al., Scand. J. Gastroenterol. 27, 438 (1992); M. Maczka et al., J. Physiol. Pharmacol. 43, 139 (1992). Clinical evaluation in gastroesophageal reflux disease: E. Sito et al., ibid. 44, 259 (1993). HPLC determn in urine and metabolism study: E. Rozman et al., J. Pharm. Sci. 83, 252 (1994).

Chemical structure

Properties

Crystals from ethyl acetate. mp 142.5-146°.

Therapeutic Category

Antiulcerative.

Keywords

Antiulcerative; Histamine H2-Receptor Antagonist