スルフイソキサゾール 化学特性,用途語,生産方法
外観
白色, 結晶性粉末～粉末
溶解性
メタノールにやや溶けやすく、エタノール(95)にやや溶けにくく、水に極めて溶けにくい。
解説
4-amino-N-(3,4-dimethyl-5-isoxazolyl)-benzenesulfonamide．C11H13N3O3S(267.30)．スルフイソキサゾール，スルファフラゾールともいう．サルファ剤の一種．5-アミノ-3,4-ジメチルイソオキサゾールとアセチルスルファニルクロリドから合成される．白色の結晶．分解点194 ℃．アセトン，酸性およびアルカリ性水溶液に易溶，水，クロロホルムに難溶．短時間作用型の抗菌薬で，すみやかに排泄されて尿路結石を生じにくいので，泌尿器疾患薬に適する．森北出版「化学辞典（第2版）
効能
抗菌薬, 葉酸合成阻害薬
使用上の注意
アルゴン封入
化学的特性
white to cream powder
使用
Sulfisoxazole is a sulfonamide based antibacterial that exhibits activity against wide spectrum of gram-negative and gram-positive bacterium.
定義
ChEBI: A sulfonamide antibacterial with an oxazole substituent. It has antibiotic activity against a wide range of gram-negative and gram-positive organisms.
抗菌性
Like all examined sulfanilamides, this drug is effective in treating infections caused by
streptococci, gonococci, pneumococci, staphylococci, and also colon bacillus. However,
about 90% of it binds with proteins in the plasma after oral administration, and it diffuses mostly to tissues and tissue fluids, which makes it the drug of choice for many systemic infections. Synonyms of this drug are gantrisin, fultrxin, sulfazin, sulfolar, and
others.
一般的な説明
Sulfisoxazole’s plasmahalf-life is 6 hours. This compound is a white, odorless,slightly bitter, crystalline powder. Its pKa is 5.0. At pH 6,this sulfonamide has a water solubility of 350 mg in100 mL, and its acetyl derivative has a solubility of 110 mgin 100 mL of water.Sulfisoxazole possesses the action and the uses of othersulfonamides and is used for infections involving sulfonamide-sensitive bacteria. It is claimed to be effective in thetreatment of Gram-negative urinary infections.
空気と水の反応
May be sensitive to prolonged exposure to air and light. Sensitive to heat. Slightly soluble in water.
火災危険
Flash point data for Sulfisoxazole are not available; however, Sulfisoxazole is probably combustible.
応用例（製薬）
3,4-Dimethyl-5-sulfanilamidoisoxazole. It is highly soluble,
even in acid urine. The spectrum and potency are typical of
the group. It is well absorbed, achieving a concentration of
around 20 mg/L 3–4 h after a 2 g oral dose.
Side effects are those common to other sulfonamides. It
is less prone than some other members of the group to cause
renal problems. Its principal use is in urinary tract infection,
and is present in some ophthalmic preparations.
生物活性
A selective ET A endothelin receptor antagonist (IC 50 values are 600 and 2200 nM for ET A and ET B receptors respectively).
安全性プロファイル
Mildly toxic by ingestion. An experimental teratogen. Questionable carcinogen. Mutation data reported. When heated to decomposition it emits very toxic fumes of SOx and NOx.
スルフイソキサゾール 上流と下流の製品情報
原材料
準備製品