2''-디옥시-5-요오드유리딘

2''-디옥시-5-요오드유리딘 속성

2''-디옥시-5-요오드유리딘 MSDS

2'-Deoxy-5-iodouridine

2''-디옥시-5-요오드유리딘 C화학적 특성, 용도, 생산

화학적 성질

Crystalline Solid

용도

Idoxuridine is an antiviral agent effective against herpes-simplex infections; in ophthalmie eyedrops, ointments, and solutions.

Indications

Idoxuridine (Herplex) is a water-soluble iodinated derivative of deoxyuridine that inhibits several DNA viruses including HSV, VZV, vaccinia, and polyoma virus. The triphosphorylated metabolite of idoxuridine inhibits both viral and cellular DNA synthesis and is also incorporated into DNA. Such modified DNA is susceptible to strand breakage and causes aberrant viral protein synthesis. Because of its significant host cytotoxicity, idoxuridine cannot be used to treat systemic viral infections. The development of resistance to this drug is common.

정의

ChEBI: A pyrimidine 2'-deoxyribonucleoside compound having 5-iodouracil as the nucleobase; used as an antiviral agent.

Pharmaceutical Applications

A halogenated pyrimidine analog originally synthesized as an anticancer agent. Formulated in dimethylsulfoxide for topical application and as a solution for ophthalmic use.
Activity is largely limited to DNA viruses, primarily HSV-1, HSV-2 and VZV. HSV-1 plaque formation in BHK 21 cells is sensitive to 6.25–25 mg/L; type 2 microplaques required 62.5–125 mg/L. RNA viruses are not affected, with the exception of oncogenic RNA viruses such as Rous sarcoma virus. Drug resistance is easily generated in vitro, and may be an obstacle to treatment. However, there is little or no crossresistance with newer nucleoside analogs.
It is poorly soluble in water, and aqueous solutions are ineffective against infections other than those localized to the eye. In animals, therapeutic levels are achieved in the cornea within 30 min of ophthalmic application and persist for 4 h. Penetration is otherwise poor, with only the biologically inactive dehalogenated metabolite uracil entering the eye.
The drug is too toxic for systemic administration. Contact dermatitis, punctate epithelial keratopathy, follicular conjunctivitis, ptosis, stenosis and occlusion of the puncta and keratinization of the lid margins occur in up to 14% of those receiving ophthalmic preparations.
It is used in herpes keratitis, but has largely been superseded by trifluridine or aciclovir.

Mechanism of action

Idoxuridine is a nucleoside containing a halogenated pyrimidine and is an analogue of thymidine. It acts as an antiviral agent against DNA viruses by interfering with their replication based on the similarity of structure between thymidine and idoxuridine. Idoxuridine is first phosphorylated by the host cell virusencoded enzyme thymidine kinase to an active triphosphate form. The phosphorylated drug inhibits cellular DNA polymerase to a lesser extent than HSV DNA polymerase, which is necessary for the synthesis of viral DNA. The triphosphate form of the drug is then incorporated during viral nucleic acid synthesis by a false pairing system that replaces thymidine. When transcription occurs, faulty viral proteins are formed, resulting in defective viral particles.

Clinical Use

The only FDA-approved use of idoxuridine is in the treatment of herpes simplex infections of the eyelid, conjunctiva conjunctiva, and cornea. It is most effective against surface infections because it has little ability to penetrate the tissues of the eye. intravenous idoxuridine was designated an orphan drug for the treatment of soft tissue sarcoma.

부작용

Idoxuridine may cause local irritation, mild edema, itching, and photophobia. Corneal clouding and small punctate defects in the corneal epithelium have been reported. Allergic reactions are rare.

Safety Profile

Moderately toxic by intraperitoneal route. Experimental teratogenic and reproductive effects. Questionable carcinogen with experimental carcinogenic data. Human mutation data reported. When heated to decomposition it emits very toxic fumes of Iand NOx.

신진 대사

Idoxuridine is metabolized rapidly in the body to iodouracil, uracil, and iodide. Metabolites are excreted in the urine.

2''-디옥시-5-요오드유리딘 준비 용품 및 원자재

원자재

준비 용품

2''-디옥시-5-요오드유리딘 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Shenzhen Nexconn Pharmatechs Ltd	+86-755-89396905 +86-15013857715	admin@nexconn.com	China	10248	58
Beijing Ribio Biotech Co.,Ltd	010-62664360 +8613328773880	wucy@ribio.com.cn	China	117	58
NewCan Biotech Limited	+86-0571-86912261 +8613735419629	sales@newcanbio.com	China	10026	58
Wuhu Nuowei chemistry Co., Ltd.	+86-0553-2911116-802 +undefined17756524438	sales1@nuowei-chem.com	China	1642	58
Hebei Yanxi Chemical Co., Ltd.	+8617531190177	peter@yan-xi.com	China	5993	58
airuikechemical co., ltd.	+undefined86-15315557071	sales02@airuikechemical.com	China	994	58
Capot Chemical Co.,Ltd.	571-85586718 +8613336195806	sales@capotchem.com	China	29797	60
Shanghai Daken Advanced Materials Co.,Ltd	+86-371-66670886	info@dakenam.com	China	15928	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21691	55
Hangzhou FandaChem Co.,Ltd.	008657128800458; +8615858145714	fandachem@gmail.com	China	9348	55

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