Muzolimine Explained

Muzolimine is a high-ceiling loop diuretic.^[1] It is a pyrazole diuretic which was used for treatment of hypertension but was withdrawn worldwide because of severe neurological side effects.^[2]

Synthesis

Rxn of (1-(3,4-dichlorophenyl)ethyl)hydrazine (1) with ethyl 3-amino-3-ethoxyacrylate (2) leads to a ring-forming two-site reaction and formation of the pyrazoline diuretic agent, muzolimine (3).

Notes and References

1. Wangemann P, Braitsch R, Greger R . The diuretic effect of muzolimine . Pflügers Archiv . 410 . 6 . 674–6 . December 1987 . 3449804 . 10.1007/BF00581331 . 19367481 .
2. Reyes AJ, Leary WP . Clinicopharmacological reappraisal of the potency of diuretics . Cardiovascular Drugs and Therapy . 7 Suppl 1 . 23–8 . January 1993 . 8435374 . 10.1007/BF00877955 . 29589710 .