磺胺嘧啶

磺胺嘧啶用途

【用途一】
磺胺类药，用于治疗由溶血性链球菌、肺炎球菌、脑膜炎球菌、淋病双球菌、大肠杆菌所致的感染
【用途二】
磺胺类药，有抑菌与收剑作用
【用途三】
为磺胺类药的优良品种，抗菌作用较强，疗效较好，吸收较快，排泄较慢，在血中有效浓度较高。临床用于治疗上呼吸道感染。流行性脑膜炎、中耳炎、疖痈、产褥热、尿道感染及急性菌痢等。
【用途四】
磺胺类抗生素，依靠抑制二氢蝶酸合成酶（dihydropteroate synthase）阻止合成二氢蝶酸。作用模式: 抑制原核生物叶酸合成。

磺胺嘧啶作用

磺胺嘧啶属中效磺胺，对非产酶金葡菌、化脓性链球菌、肺炎链球菌、大肠埃希菌、克雷伯菌属、沙门菌属、志贺菌属等肠杆菌科细菌、淋球菌、脑膜炎球菌、流感嗜血杆菌具有抗菌作用，此外在体外对沙眼衣原体、星形奴卡菌、疟原虫和弓形虫也有抗微生物活性。本品抗菌活性同磺胺甲唑。但近年来细菌对本品的耐药性增高，尤其是链球菌属、奈瑟菌属以及肠杆菌科细菌。磺胺类为广谱抑菌剂。本品在结构上类似对氨基苯甲酸(PABA)，可与PABA竞争性作用于细菌体内的二氢叶酸合成酶，从而阻止PABA作为原料合成细菌所需的叶酸，减少了具有代谢活性的四氢叶酸的量，而后者则是细菌合成嘌呤、胸腺嘧啶核苷和脱氧核糖核酸(DNA)的必需物质，因此抑制了细菌的生长繁殖。

磺胺嘧啶名称

[ CAS 号 ]:
68-35-9

[ 中文名 ]:
磺胺嘧啶

[ 英文名 ]:
Sulfadiazine

[中文别名 ]:

[英文别名 ]:

Sulfadiazine
A-306
2-sulfanilylaminopyrimidine
2-sulfanilamidopyrimidine
PYRIMAL
FLAMAZINE
sulfapyrimidine
MFCD00006065
Silvadene
sulphadiazine

磺胺嘧啶生物活性

[ 描述 ]:

Sulfadiazine是磺胺类抗生素。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

研究领域 >> 感染

[参考文献]

[1]. Kucan, J.O., et al., Comparison of silver sulfadiazine, povidone-iodine and physiologic saline in the treatment of chronic pressure ulcers. J Am Geriatr Soc, 1981. 29(5): p. 232-5.

[相关活性小分子]

磺胺嘧啶物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
512.6±52.0 °C at 760 mmHg

[ 熔点 ]:
253 °C (dec.)(lit.)

[ 分子式 ]:
C₁₀H₁₀N₄O₂S

[ 分子量 ]:
250.277

[ 闪点 ]:
263.8±30.7 °C

[ 精确质量 ]:
250.052444

[ PSA ]:
106.35000

[ LogP ]:
-0.12

[ 外观性状 ]:
白色至略黄色结晶粉末

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.679

[ 储存条件 ]:
0-6°C

[ 水溶解性 ]:
水溶性：不溶；可溶于：二甲基甲酰胺；微溶：丙酮；不溶：乙醇,乙醚

磺胺嘧啶MSDS

详细MSDS(安全技术说明书)

磺胺嘧啶毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WP1925000

CHEMICAL NAME :: Sulfanilamide, N(sup 1)-2-pyrimidinyl-

CAS REGISTRY NUMBER :: 68-35-9

BEILSTEIN REFERENCE NO. :: 0235192

LAST UPDATED :: 199707

DATA ITEMS CITED :: 20

MOLECULAR FORMULA :: C10-H10-N4-O2-S

MOLECULAR WEIGHT :: 250.30

WISWESSER LINE NOTATION :: T6N CNJ BMSWR DZ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 229 mg/kg/8D-I

TOXIC EFFECTS :: Gastrointestinal - other changes Kidney, Ureter, Bladder - urine volume decreased

REFERENCE :: IJMDAI Israel Journal of Medical Sciences. (POB 1435, Jerusalem 91013, Israel) V.1- 1965- Volume(issue)/page/year: 6,561,1970

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 138 mg/kg

TOXIC EFFECTS :: Behavioral - general anesthetic Kidney, Ureter, Bladder - urine volume decreased Kidney, Ureter, Bladder - hematuria

REFERENCE :: PGMJAO Postgraduate Medical Journal. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1925- Volume(issue)/page/year: 53,103,1977

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 446 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: KLWOAZ Klinische Wochenscrift. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.1- 1922- Volume(issue)/page/year: 27,449,1949

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 880 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 211,367,1950

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,571,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 750 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 29ZVAB "Handbook of Analytical Toxicology," Sunshine, I., ed., Cleveland, OH, Chemical Rubber Co., 1969 Volume(issue)/page/year: -,109,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1600 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,386,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 180 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CSLNX* U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals. (Aberdeen Proving Ground, MD 21010) Volume(issue)/page/year: NX#03347

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 79,354,1943 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 91200 mg/kg/22W-C

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes Endocrine - thyroid weight (goiter) Related to Chronic Data - death

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 79,354,1943

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5250 mg/kg/2W-C

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 81,17,1944

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2640 mg/kg/30D-C

TOXIC EFFECTS :: Endocrine - other changes Blood - changes in spleen Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 14,2856,1980 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 6 gm/kg

SEX/DURATION :: female 9-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: SEIJBO Senten Ijo. Congenital Anomalies. (Nippon Senten Ijo Gakkai, c/o Kinki Daigaku Igakubu Kaibagaku Kyoshitsu, 380 Nishiyama, Sayama-cho, Mirami-Kawachi-gun, Osaka-fu, Japan) V.1-26, 1960-86. For publisher information, see CGANE7. Volume(issue)/page/year: 13,7,1973

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 6 gm/kg

SEX/DURATION :: female 7-12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - eye/ear

REFERENCE :: SEIJBO Senten Ijo. Congenital Anomalies. (Nippon Senten Ijo Gakkai, c/o Kinki Daigaku Igakubu Kaibagaku Kyoshitsu, 380 Nishiyama, Sayama-cho, Mirami-Kawachi-gun, Osaka-fu, Japan) V.1-26, 1960-86. For publisher information, see CGANE7. Volume(issue)/page/year: 13,7,1973

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 6 gm/kg

SEX/DURATION :: female 7-12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: SEIJBO Senten Ijo. Congenital Anomalies. (Nippon Senten Ijo Gakkai, c/o Kinki Daigaku Igakubu Kaibagaku Kyoshitsu, 380 Nishiyama, Sayama-cho, Mirami-Kawachi-gun, Osaka-fu, Japan) V.1-26, 1960-86. For publisher information, see CGANE7. Volume(issue)/page/year: 13,17,1973 *** REVIEWS *** TOXICOLOGY REVIEW JMSHAO Journal of the Mount Sinai Hospital (New York). (New York, NY) V.1-36, 1934-69. For publisher information, see MSJMAZ. Volume(issue)/page/year: 10,343,1943 TOXICOLOGY REVIEW ADVPA3 Advances in Pharmacology. (New York, NY) V.1-6, 1962-68. For publisher information, see AVPCAQ. Volume(issue)/page/year: 4,263,1966 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 80538 No. of Facilities: 1033 (estimated) No. of Industries: 4 No. of Occupations: 9 No. of Employees: 5001 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 80538 No. of Facilities: 95 (estimated) No. of Industries: 2 No. of Occupations: 20 No. of Employees: 2854 (estimated) No. of Female Employees: 849 (estimated)

磺胺嘧啶安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H315-H317-H319-H334-H335

[ 警示性声明 ]:
P261-P280-P284-P304 + P340-P305 + P351 + P338-P342 + P311

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn,Xi

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S26-S36

[ 危险品运输编码 ]:
3249

[ WGK德国 ]:
3

[ RTECS号 ]:
WP1925000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2935009090

磺胺嘧啶合成路线

详细合成路线

磺胺嘧啶上下游产品

磺胺嘧啶上游产品

磺胺嘧啶下游产品

磺胺嘧啶制备

可由糠氯酸与硝基胍合成2-氨基嘧啶后与对乙酰基苯磺酰氯在吡啶中缩合水解而制得。

磺胺嘧啶海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

磺胺嘧啶文献

Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.

Chem. Res. Toxicol. 23 , 171-83, (2010)

Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental...

Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).

J. Sci. Ind. Res. 65(10) , 808, (2006)

Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI typ...

Convenient QSAR model for predicting the complexation of structurally diverse compounds with β-cyclodextrins

Bioorg. Med. Chem. 17 , 896-904, (2009)

This paper reports a QSAR study for predicting the complexation of a large and heterogeneous variety of substances (233 organic compounds) with beta-cyclodextrins (beta-CDs). Several different theoret...

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