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Galidesivir

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BCX4430.svg

ChemSpider 2D Image | Galidesivir | C11H15N5O3

Galidesivir

  • Molecular FormulaC11H15N5O3
  • Average mass265.268 Da
Immucillin-A
OLF97F86A7
UNII:OLF97F86A7
галидесивир [Russian] [INN]
غاليديسيفير [Arabic] [INN]
加利司韦 [Chinese] [INN]
Galidesivir [INN]
(2S,3S,4R,5R)-2-(4-amino- 5H-pyrrolo[3,2-d]pyrimidin- 7-yl)-5-(hydroxymethyl) pyrrolidine-3,4-diol
(2S,3S,4R,5R)-2-(4-Amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl)-5-(hydroxymethyl)-3,4-pyrrolidinediol [ACD/IUPAC Name]
10284
222631-44-9 [RN]
249503-25-1 [RN]
3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)- [ACD/Index Name]
BCX4430 [Wiki]

Galidesivir

249503-25-1

222631-44-9, BCX-4430 (HCL salt form of galidesivir)

2-(4-Amino-5H-pyrrolo(3,2-d)pyrimidin-7-yl)-5-(hydroxymethyl)pyrrolidine-3,4-diol.png

Galidesivir (BCX4430Immucillin-A) is an antiviral drug, an adenosine analog[1] (a type of nucleoside analog).[2] It is developed by BioCryst Pharmaceuticals with funding from NIAID, originally intended as a treatment for hepatitis C, but subsequently developed as a potential treatment for deadly filovirus infections such as Ebola virus disease and Marburg virus disease.

It also shows broad-spectrum antiviral effectiveness against a range of other RNA virus families, including bunyavirusesarenavirusesparamyxovirusescoronavirusesflaviviruses and phleboviruses.[3] BCX4430 has been demonstrated to protect against both Ebola and Marburg viruses in both rodents and monkeys, even when administered up to 48 hours after infection,[1] and development for use in humans was then being fast-tracked due to concerns about the lack of treatment options for the 2013-2016 Ebola virus epidemic in West Africa.[4]

BCX4430 later showed efficacy against Zika virus in a mouse model, though there are no plans for human trials at this stage.[5]

Galidesivir is one of several antiviral drugs being tested for coronavirus disease 2019.[6]

Image result for Galidesivir SYNTHESIS

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https://www.sciencedirect.com/science/article/pii/S0040402017305926

Image result for Galidesivir SYNTHESIS

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https://cen.acs.org/sections/coronavirus/biological-chemistry/infectious-disease/coronavirus-drug-repurposing.html

coronavirus-scheme.jpg

When any new virus emerges, drug and vaccine developers spring into action, searching for products to stop it in its tracks. Drug discovery campaigns launch, vaccine development efforts ramp up, and everyone mobilizes to get it all into the clinic as quickly as possible.

The current pandemic, driven by a coronavirus known as SARS-CoV-2, is no different. Already, a Phase I study of an mRNA-based vaccine developed by Moderna has begun, and major pharma companies and small biotechs are working on other types of vaccines. But even if they work, the most optimistic timelines put a vaccine a year to 18 months away.

The more immediate approach to an outbreak is to scour the medicine cabinet for existing molecules that could be repurposed against a new virus. The most advanced potential treatment is Gilead Sciences’ remdesivir, an antiviral discovered during the 2014 Ebola epidemic. The compound is already being tested in four, Phase III trials—two in China and two in the US—against the respiratory disease COVID-19. Gilead expects the first dataset from those studies to come out in April.

A new paper from CAS explored remdesivir and other possible options the cabinet might contain (ACS Cent. Sci. 2020, DOI: 10.1021/acscentsci.0c00272). CAS, a division of the American Chemical Society, which publishes C&EN, looked at the landscape of patent and journal articles covering small molecules, antibodies, and other therapeutic classes to identify therapies with potential activity against COVID-19.

SARS-CoV-2, belongs to the same family as two coronaviruses responsible for earlier outbreaks, Severe Acute Respiratory Syndrome (SARS) and Middle East Respiratory Syndrome (MERS). Because all three feature structurally similar proteins that allow entry into and replication inside host cells, CAS searched for patent data related to those more well-studied coronaviruses.

C&EN has assembled the relevant small molecules identified by CAS, which can be explored by the stage in the viral life cycle they aim to disrupt.

Patents

Patent ID Title Submitted Date Granted Date
US7390890 Inhibitors of nucleoside metabolism 2007-08-23 2008-06-24
US7211653 Inhibitors of nucleoside metabolism 2005-02-03 2007-05-01
US6803455 Inhibitors of nucleoside metabolism 2003-05-22 2004-10-12
US6492347 Inhibitors of nucleoside metabolism 2002-05-23 2002-12-10
US6228847 Inhibitors of nucleoside metabolism 2001-05-08
Patent ID Title Submitted Date Granted Date
EP1023308 INHIBITORS OF NUCLEOSIDE METABOLISM 2000-08-02 2005-09-07
US6066722 Inhibitors of nucleoside metabolism 2000-05-23

References

  1. Jump up to:a b Warren TK, Wells J, Panchal RG, Stuthman KS, Garza NL, Van Tongeren SA, et al. (April 2014). “Protection against filovirus diseases by a novel broad-spectrum nucleoside analogue BCX4430” (PDF)Nature508 (7496): 402–5. Bibcode:2014Natur.508..402Wdoi:10.1038/nature13027PMID 24590073.
  2. ^ Kamat SS, Burgos ES, Raushel FM (October 2013). “Potent inhibition of the C-P lyase nucleosidase PhnI by Immucillin-A triphosphate”Biochemistry52 (42): 7366–8. doi:10.1021/bi4013287PMC 3838859PMID 24111876.
  3. ^ Westover JB, et al. Galidesivir limits Rift Valley fever virus infection and disease in Syrian golden hamsters. Antiviral Res. 2018 Aug;156:38-45. Westover, J. B.; Mathis, A.; Taylor, R.; Wandersee, L.; Bailey, K. W.; Sefing, E. J.; Hickerson, B. T.; Jung, K. H.; Sheridan, W. P.; Gowen, B. B. (2018). “Galidesivir limits Rift Valley fever virus infection and disease in Syrian golden hamsters”Antiviral Research156: 38–45. doi:10.1016/j.antiviral.2018.05.013PMC 6035881PMID 29864447.
  4. ^ Rodgers P (8 April 2014). “BioWar Lab Helping To Develop Treatment For Ebola”Forbes Magazine.
  5. ^ Julander JG, Siddharthan V, Evans J, Taylor R, Tolbert K, Apuli C, et al. (January 2017). “Efficacy of the broad-spectrum antiviral compound BCX4430 against Zika virus in cell culture and in a mouse model”Antiviral Research137: 14–22. doi:10.1016/j.antiviral.2016.11.003PMC 5215849PMID 27838352.
  6. ^ Praveen Duddu. Coronavirus outbreak: Vaccines/drugs in the pipeline for Covid-19. clinicaltrialsarena.com 19 February 2020.

 

Galidesivir
BCX4430.svg
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
Formula C11H15N5O3
Molar mass 265.268 g·mol−1
3D model (JSmol)

//////////////Galidesivir, Immucillin-A, OLF97F86A7, UNII:OLF97F86A7, галидесивирغاليديسيفير加利司韦 , BCX4430, BCX 4430, CORONAVIRUS, COVID 19

 

nitazoxanide


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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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