Furonazide Explained

Furonazide is a crystalline tuberculostatic drug substance with a reported melting point of 199-201.5 °C.^[1] __TOC__

Synthesis

Furonazide was first prepared in 1955 by Miyatake from isoniazid and 2-Acetylfuran by refluxing in ethanol, followed by filtration of the crystalline product.^{[1] [2]}

Applications

Furonazide has shown bacteriostatic action and is tuberculostatic at levels of 10⁻⁸ molar.^[1] The in vitro antibacterial activity of furonazide against Bacillus Calmette-Guerin was found to be essentially equal to that of isoniazid on an equimolar basis.^[3] In vivo studies in the guinea pig showed furonazide slightly more active than isoniazid as a tuberculostatic agent.^[4] The drug has relatively low toxicity. The median lethal dose (LD₅₀, rat oral) was reported as 2,600 mg/kg.^[5]

Notes and References

1. Kazuo Miyatake, “Derivatives of isonicotinic acid hydrazide”, Japanese Patent 32,002,484 B4 (1957)
2. Kazuo Miyatake . Syntheses of compounds related to isonicotinic acid hydrazide. III. Antitubercular compounds . Yakugaku Zasshi. 75 . 1066–9. 1955. Ichimura . Shozo . Nagasaki . Senkichi . Hoji . Kazuhiko. 10.1248/yakushi1947.75.9_1066. free .
3. Kiichiro Kakemi . Stability of drugs in biological media. II. Relations between the stability in culture media and antibacterial activity of some isoniazid derivatives. Chemical & Pharmaceutical Bulletin. 17. 1623–8. 1969. Sezaki. Hitoshi. Iwamoto. Kikuo. Sano. Yukito . 10.1248/cpb.17.1623 . 8. 4981613. free.
4. Giovanni Pacilio. Tuberculostatic activity of some isoniazid derivatives administered to guinea pigs at different time intervals. Atti della Societa Italiana delle Scienze Veterinarie. 18 . 631–6. 1964. Pagnini. Pietro. Genazzani. Enrico.
5. "Drugs - Synonyms and Properties" data were obtained from Ashgate Publishing Co. (US)