3684-46-6|溴沙定|Broxaldine|-范德生物科技公司

溴沙定

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names：
Broxaldine
CAS号：
3684-46-6
MDL Number：
MF(分子式)： C17H11Br2NO2 MW(分子量)： 421.08
EINECS:222-971-1 Reaxys Number:
Pubchem ID:77262 Brand:BIOFOUNT

溴沙定(3684-46-6,Broxaldine,Brobenzoxaldine)是一种抗原虫药。Broxaldine抑制艰难梭菌的MIC值为4 µM，并具有抗真菌作用。

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中文别名	溴沙定(3684-46-6);溴索丁;二溴甲喹苯酯;5,7-二溴-2-甲基-8-喹啉基苯甲酸酯;5,7-二溴-8-羟基喹那啶;5,7-二溴-8-苯甲酰氧基奎尼丁; 5,7-二溴-2-甲基-8-酚基苯甲酸酯；
英文别名	Broxaldine(3684-46-6);5,7-dibromo-2-methyl-8-quinolylbenzoate;Broxaldine;Brobenzoxaldine; 5,7-Dibromo-8-benzoyloxyquinaldine; 5,7-Dibrom-2-methyl-8-chinolyl benzoat;
CAS号	3684-46-6
SMILES	CC1=NC2=C(OC(C3=CC=CC=C3)=O)C(Br)=CC(Br)=C2C=C1
Inchi	InChI=1S/C17H11Br2NO2/c1-10-7-8-12-13(18)9-14(19)16(15(12)20-10)22-17(21)11-5-3-2-4-6-11/h2-9H,1H3
InchiKey	IJTPLVAAROHGGB-UHFFFAOYSA-N
分子式 Formula	C17H11Br2NO2
分子量 Molecular Weight	421.08
闪点 FP	279.2±30.1 °C
熔点 Melting point	No data available
沸点 Boiling point	538.1±50.0 °C at 760 mmHg
Polarizability极化度	37.3±0.5 10-24cm3
密度 Density	1.7±0.1 g/cm3
蒸汽压 Vapor Pressure	0.0±1.4 mmHg at 25°C
溶解度Solubility	生物体外In Vitro:DMSO溶解度≥ 42.86 mg/mL(101.79 mM)*"≥" means soluble可溶, but saturation unknown溶解度未知.
性状	固体粉末,Power
储藏条件 Storage conditions	-20°C 3 years年 4°C 2 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月

溴沙定(3684-46-6,Broxaldine,Brobenzoxaldine)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

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产品说明	溴沙定(3684-46-6,Broxaldine,Brobenzoxaldine)是一种抗原生动物药物。
Introduction	溴沙定(3684-46-6,Broxaldine,Brobenzoxaldine)is an antiprotozoal drug.
Application1
Application2
Application3

溴沙定(3684-46-6,Broxaldine,Brobenzoxaldine)药理学：

溴沙定(3684-46-6,Broxaldine,Brobenzoxaldine)是一种抗原虫药。Broxaldine抑制艰难梭菌的MIC值为4 µM，并具有抗真菌作用。

警示图
危险性	warning
危险性警示	Not available
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理
备注	实验过程中防止吸入、食入，做好安全防护

Hazra SK, et al. Therapeutic trial of a combination of broxyquinoline and brobenzoxaldine in the treatment of leprosy. Lepr India. 1979 Oct;51(4):505-10.

AbdelKhalek A, et al. Screening for potent and selective anticlostridial leads among FDA-approved drugs. J Antibiot (Tokyo). 2020 Mar 4.

A study on the neurotoxicity of broxyquinoline and brobenzoxaldine combination in therapeutic doses PMID 3081428; Human toxicology 1986 Jan; 5(1):35-41 Name matches: broxyquinoline brobenzoxaldine

Impairment of exercise tolerance due to broxyquinoline-brobenzoxaldine combination PMID 3081430; Human toxicology 1986 Jan; 5(1):63-4 Name matches: broxyquinoline brobenzoxaldine

Broxyquinoline and brobenzoxalidine suspension (Intestopan-AI 307) in childhood diarrhoea. A clinical trial on 533 children PMID 4933138; Indian journal of pediatrics 1970 May; 37(268):177-84 Name mat

溴沙定(3684-46-6,Broxaldine,Brobenzoxaldine)参考文献：

1.[Toxicity of hydroxyquinoline derivatives].
Pashov D, Simeonov SP, Drumev D, Pe?nikova Ts, Dzhurov A. Vet Med Nauki. 1980;17(3):118-23.

We studied a 90 day toxicity in dogs of the compound broxyquinoline + broxaldine--5:1 (enteroquin), applied orally and daily in doses of 0.1 and 0.2/kg t/24 h. We established the toxic manifestations during the period after the 15th day of the treatment: leukopenia, neutropenia and lymphocytosis (by 0.2 kg t/24 h). After the second and fifth day we observed a decrease of appetite, depression of the CNS, paralyses, arrhythmia, progressing loss in weight, proteinorrhea (more pronounced with those receiving 0.2/kg t (24 h); lethal consequence with some part of the animals 25% (ba 0.1/kg t) and 50% (by 0.2 kg t). We found out pathohistologically necrobiotic changes in the medulla oblongata and the kidneys, toxic distrophy of the liver, blood-vessel injuries. The toxic changes observed can be interpreted in connection with the presence of a species specific reaction.

2.Letter: Effect of broxyquinoline and broxaldine in leprosy.
Sharma CS. Lancet. 1975 Feb 15;1(7903):405.

3、A study on the neurotoxicity of broxyquinoline and brobenzoxaldine combination in therapeutic doses
R Swain, J S Bapna, A K Das, S Chandrasekar, R P Swaminathan, B Bosco, S Veliath, D P Thombre

Abstract The neurotoxicity of a combination of broxyquinoline and brobenzoxaldine (Intestopan Forte, containing 500 mg and 100 mg of the drugs respectively per capsule) was investigated by prospective clinical and electrophysiological studies in patients and volunteer subjects given the drugs in therapeutic doses (two capsules three times a day for 5 days). Of 16 patients with intestinal amoebiasis given the drugs (study A), 13 (81.25%) were cured. Adverse effects were mild and did not affect treatment. No neurological adverse effect was reported. Neurological examinations revealed no abnormality in any patient after treatment. Seven volunteer subjects underwent medical, neurological and ophthalmological examinations, and electrophysiological studies of ulnar and peroneal nerve conduction before and after treatment with the drugs in therapeutic doses (study B). Transient paresthesias were reported by one subject on the fourth day of treatment. No medical, neurological or ophthalmological abnormality was detected in any subject after treatment. There was no significant change in motor nerve conduction velocities. There was a significant (P less than 0.001) increase in the stimulus strength for distal ulnar stimulation and a significant (P less than 0.01) decrease in stimulus duration for proximal and distal ulnar stimulation. No significant changes were seen in the peroneal nerves in these parameters. No qualitative abnormality was seen in the oscilloscopic patterns of nerve conduction after treatment. Literature on the neurotoxicity of the halogenated hydroxyquinolines is reviewed. It is concluded that broxyquinoline and brobenzoxaldine (and probably other halogenated hydroxyquinolines as well) are safe and effective in therapeutic doses; neurotoxicity is unlikely to occur when these drugs are used according to therapeutic recommendations.

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