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

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]

References

  1. ^ a b c Kazuo Miyatake, “Derivatives of isonicotinic acid hydrazide”, Japanese Patent 32,002,484 B4 (1957)
  2. ^ Kazuo Miyatake; Ichimura, Shozo; Nagasaki, Senkichi; Hoji, Kazuhiko (1955). "Syntheses of compounds related to isonicotinic acid hydrazide. III. Antitubercular compounds". Yakugaku Zasshi. 75: 1066–9. doi:10.1248/yakushi1947.75.9_1066.
  3. ^ Kiichiro Kakemi; Sezaki, Hitoshi; Iwamoto, Kikuo; Sano, Yukito (1969). "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 (8): 1623–8. doi:10.1248/cpb.17.1623. PMID 4981613.
  4. ^ Giovanni Pacilio; Pagnini, Pietro; Genazzani, Enrico (1964). "Tuberculostatic activity of some isoniazid derivatives administered to guinea pigs at different time intervals". Atti della Societa Italiana delle Scienze Veterinarie. 18: 631–6.
  5. ^ "Drugs - Synonyms and Properties" data were obtained from Ashgate Publishing Co. (US)
Allikas: https://en.wikipedia.org/wiki/Furonazide
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