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Niclosamide, ニクロサミド , никлосамид , نيكلوساميد , 氯硝柳胺 , 

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Niclosamide.svg

Niclosamide

ChemSpider 2D Image | Niclosamide | C13H8Cl2N2O4

Niclosamide

ニクロサミド;

Formula
C13H8Cl2N2O4
cas
50-65-7
Mol weight
327.1196
никлосамид [Russian] [INN]
نيكلوساميد [Arabic] [INN]
氯硝柳胺 [Chinese] [INN]
Niclosamide [BSI] [INN] [ISO] [USAN] [Wiki]
1532
2′,5-Dichlor-4′-nitro-salizylsaeureanilid [German]
2′,5-Dichloro-4′-nitrosalicylanilide
200-056-8 [EINECS]
2820605
50-65-7 [RN]
]
5-Chlor-N-(2-chlor-4-nitrophenyl)-2-hydroxybenzolcarboxamid
5-Chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide

CAS Registry Number: 50-65-7

CAS Name: 5-Chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide
Additional Names: 2¢,5-dichloro-4¢-nitrosalicylanilide; 5-chloro-N-(2¢-chloro-4¢-nitrophenyl)salicylamide; 5-chlorosalicyloyl-(o-chloro-p-nitranilide); N-(2¢-chloro-4¢-nitrophenyl)-5-chlorosalicylamide
Manufacturers’ Codes: Bayer 2353
Trademarks: Cestocide (Bayer); Niclocide (Miles); Ruby (Spencer); Trédémine (RPR); Yomesan (Bayer)
Molecular Formula: C13H8Cl2N2O4
Molecular Weight: 327.12
Percent Composition: C 47.73%, H 2.47%, Cl 21.68%, N 8.56%, O 19.56%
Literature References: Prepn: GB 824345 (1959 to Bayer), C.A. 54, 15822b (1960). See also: E. Schraufstätter, R. Gönnert, US 3079297; R. Strufe et al., US 3113067 (both 1963 to Bayer); Bekhli et al., Med. Prom. SSSR 1965, 25.
Properties: Pale yellow crystals, mp 225-230°. Practically insol in water. Sparingly sol in ethanol, chloroform, ether.
Melting point: mp 225-230°
Derivative Type: Ethanolamine salt
CAS Registry Number: 1420-04-8
Additional Names: Clonitrilide
Trademarks: Bayluscid (Bayer)
Molecular Formula: C13H8Cl2N2O4.C2H7NO
Molecular Weight: 388.20
Percent Composition: C 46.41%, H 3.89%, Cl 18.27%, N 10.82%, O 20.61%
Properties: Yellow-brown solid, mp 204°.
Melting point: mp 204°
Use: The ethanolamine salt as a molluscicide.
Therap-Cat: Anthelmintic (Cestodes).
Therap-Cat-Vet: Anthelmintic (Cestodes).
Keywords: Anthelmintic (Cestodes).

Niclosamide, sold under the brand name Niclocide among others, is a medication used to treat tapeworm infestations.[2] This includes diphyllobothriasishymenolepiasis, and taeniasis.[2] It is not effective against other worms such as pinworms or roundworms.[3] It is taken by mouth.[2]

Side effects include nausea, vomiting, abdominal pain, and itchiness.[2] It may be used during pregnancy and appears to be safe for the baby.[2] Niclosamide is in the anthelmintic family of medications.[3] It works by blocking the uptake of sugar by the worm.[4]

Niclosamide was discovered in 1958.[5] It is on the World Health Organization’s List of Essential Medicines, the safest and most effective medicines needed in a health system.[6] The wholesale cost in the developing world is about 0.24 USD for a course of treatment.[7] It is not commercially available in the United States.[3] It is effective in a number of other animals.[4]

Side effects

Side effects include nausea, vomiting, abdominal pain, constipation, and itchiness.[2] Rarely, dizziness, skin rash, drowsiness, perianal itching, or an unpleasant taste occur. For some of these reasons, praziquantel is a preferable and equally effective treatment for tapeworm infestation.[citation needed]

Mechanism of action

Niclosamide inhibits glucose uptake, oxidative phosphorylation, and anaerobic metabolism in the tapeworm.[8]

Other applications

Niclosamide’s metabolic effects are relevant to wide ranges of organisms, and accordingly it has been applied as a control measure to organisms other than tapeworms. For example, it is an active ingredient in some formulations such as Bayluscide for killing lamprey larvae,[9][10] as a molluscide,[11] and as a general purpose piscicide in aquaculture. Niclosamide has a short half-life in water in field conditions; this makes it valuable in ridding commercial fish ponds of unwanted fish; it loses its activity soon enough to permit re-stocking within a few days of eradicating the previous population.[11] Researchers have found that niclosamide is effective in killing invasive zebra mussels in cool waters.[12]

Research

Niclosamide is being studied in a number of types of cancer.[13] Niclosamide along with oxyclozanide, another anti-tapeworm drug, was found in a 2015 study to display “strong in vivo and in vitro activity against methicillin-resistant Staphylococcus aureus (MRSA)”.[14]

syn

https://www.sciencedirect.com/science/article/pii/S0099542805320028

Image result for niclosamide

References

  1. Jump up to:a b c d e f World Health Organization (2009). Stuart MC, Kouimtzi M, Hill SR (eds.). WHO Model Formulary 2008. World Health Organization. pp. 81, 87, 591. hdl:10665/44053ISBN 9789241547659.
  2. Jump up to:a b c “Niclosamide Advanced Patient Information – Drugs.com”http://www.drugs.comArchived from the original on 20 December 2016. Retrieved 8 December 2016.
  3. Jump up to:a b Jim E. Riviere; Mark G. Papich (13 May 2013). Veterinary Pharmacology and Therapeutics. John Wiley & Sons. p. 1096. ISBN 978-1-118-68590-7Archived from the original on 10 September 2017.
  4. ^ Mehlhorn, Heinz (2008). Encyclopedia of Parasitology: A-M. Springer Science & Business Media. p. 483. ISBN 9783540489948Archived from the original on 2016-12-20.
  5. ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  6. ^ “Niclosamide”International Drug Price Indicator GuideArchived from the original on 10 May 2017. Retrieved 1 December 2016.
  7. ^ Weinbach EC, Garbus J (1969). “Mechanism of action of reagents that uncouple oxidative phosphorylation”. Nature221 (5185): 1016–8. doi:10.1038/2211016a0PMID 4180173.
  8. ^ Boogaard, Michael A. Delivery Systems of Piscicides “Request Rejected”(PDF)Archived (PDF) from the original on 2017-06-01. Retrieved 2017-05-30.
  9. ^ Verdel K.Dawson (2003). “Environmental Fate and Effects of the Lampricide Bayluscide: a Review”. Journal of Great Lakes Research29 (Supplement 1): 475–492. doi:10.1016/S0380-1330(03)70509-7.
  10. Jump up to:a b “WHO Specifications And Evaluations. For Public Health Pesticides. Niclosamide” (PDF).[dead link]
  11. ^ “Researchers find new methods to combat invasive zebra mussels”The Minnesota Daily. Retrieved 2018-11-19.
  12. ^ “Clinical Trials Using Niclosamide”NCI. Retrieved 20 March 2019.
  13. ^ Rajamuthiah R, Fuchs BB, Conery AL, Kim W, Jayamani E, Kwon B, Ausubel FM, Mylonakis E (April 2015). Planet PJ (ed.). “Repurposing Salicylanilide Anthelmintic Drugs to Combat Drug Resistant Staphylococcus aureus”PLoS ONE10 (4): e0124595. doi:10.1371/journal.pone.0124595ISSN 1932-6203PMC 4405337PMID 25897961.

External links

 

Niclosamide

Niclosamide
Niclosamide.svg
Clinical data
Trade names Niclocide, Fenasal, Phenasal, others[1]
AHFS/Drugs.com Micromedex Detailed Consumer Information
Routes of
administration
By mouth
ATC code
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.000.052 Edit this at Wikidata
Chemical and physical data
Formula C13H8Cl2N2O4
Molar mass 327.119 g/mol g·mol−1
3D model (JSmol)
Melting point 225 to 230 °C (437 to 446 °F)

//////////Niclosamide ニクロサミド , никлосамидنيكلوساميد氯硝柳胺 , covid 19, corona virus


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DR ANTHONY CRASTO

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK PHARMACEUTICALS LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 30 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, Dr T.V. Radhakrishnan and Dr B. K. Kulkarni, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 30 year tenure till date Dec 2017, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 9 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 50 Lakh plus views on dozen plus blogs, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 19 lakh plus views on New Drug Approvals Blog in 216 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc

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