3577. Endralazine

Nomenclature

CAS number: 39715-02-1
6-Benzoyl-5,6,7,8-tetrahydropyrido[4,3-c]pyridazin-3(2H)-one hydrazone; 6-benzoyl-3-hydrazino-5,6,7,8-tetrahydropyrido[4,3-c]pyridazine.
C14H15N5O; mol wt 269.30.
C 62.44%, H 5.61%, N 26.01%, O 5.94%.

Description and references

Prepn: E. Schenker, DE 2221808; idem, US 3838125 (1972, 1974 both to Sandoz); E. Schenker, R. Salzmann, Arzneim.-Forsch. 29, 1835 (1979). Pharmacology: R. Salzmann et al., ibid. 1843. Hemodynamic study: H. U. Lehmann et al., Z. Cardiol. 66, 203 (1977). HPLC determn in human plasma: P. A. Reece et al., J. Chromatogr. 225, 151 (1981). Clinical pharmacology: F. C. Reubi, Eur. J. Clin. Pharmacol. 13, 185 (1978). Clinical study in hypertension: H. U. Lehmann et al., Med. Welt 29, 1007 (1978).

Chemical structure

Properties

Crystals from acetonitrile/water, mp 220-223° (dec).

Derivative

Methanesulfonate.

Nomenclature

CAS number: 65322-72-7
Endralazine mesylate; BQ 22-708; Miretilan (Sandoz).
C14H15N5O.CH3SO3H; mol wt 365.41.
C 49.30%, H 5.24%, N 19.17%, O 17.51%, S 8.78%.

Properties

Cryst, mp 185-188° (dec).

Therapeutic Category

Antihypertensive.

Keywords

Antihypertensive; Hydrazines/Phthalazines