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2 edition of Heterocyclic pyrophosphate analogues as potential antiviral agents found in the catalog.

Heterocyclic pyrophosphate analogues as potential antiviral agents

Matthew Alexander Naylor

Heterocyclic pyrophosphate analogues as potential antiviral agents

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Published by typescript in [s.l.] .
Written in English


Edition Notes

Thesis (Ph.D.) - University of Warwick, 1985.

Statementby Matthew Alexander Naylor.
ID Numbers
Open LibraryOL13863404M

NAD analogues designed as potential anticancer agents. Quest for selective inhibition of inosine monophosphate dehydrogenase (IMPDH). NAD analogues Pharmacol. Ther. , 76, Luyten I, Pankiewicz KW, Watanabe KA, Chattopadhyaya J. The determination of the tautomeric equlibrium of pseudouridine in the basic solution. J. Org.


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Heterocyclic pyrophosphate analogues as potential antiviral agents by Matthew Alexander Naylor Download PDF EPUB FB2

HETEROCYCLIC PYROPHOSPHATE ANALOGUES AS POTENTIAL ANTIVIRAL AGENTS by Matthew Alexander Naylor, (Warwick) A thesis submitted in partial fulfilment of the requirements for the degree of Doctor of Philosophy at the University of Warwick Department of.

A series of novel and known heterocyclic pyrophosphate analogues have been synthesised and screened for activity against herpesvirus DNA polymerases, influenza A RNA transcriptase and calf thymus DNA polymerase a. A direct correlation between the compounds1 abilities to form complexes with zinc ions, as determined by a gel filtration method, and their effectiveness as inhibitors of the RNA Author: Matthew Alexander Naylor.

Heterocyclic pyrophosphate analogues as potential antiviral agents Author: Naylor, M. ISNI: Awarding Body: University of Warwick Current Institution: University of Warwick Date of Award: Availability of Full Text.

nucleotide analogues as antiviral agents acs symposium series By Andrew Neiderman phosphonylmethoxypropyl hpmp and n 2 phosphonylmethoxyethyl pme derivatives of heterocyclic pyrophosphate analogues charles e mckenna jeffrey n levy leslie a khawli vahak harutunian ting gao.

Nucleotide Analogues as Antiviral Agents by John C. Martin,available at Book Depository with free delivery : John C. Martin. Design, synthesis, DNA binding, and biological evaluation of water-soluble hybrid molecule containing two pyrazole analogues of the alkylating cyclopropyl-pyrroloindole (CPI) subunit of the antitumor agent CC and polypyrrol minor groove binders.

Rapid synthesis of carbonucleoside phophonate analogues as potential antiviral agents via a hydrophosphonylation reaction of ethynyl carbocyclic precursors B. Sidi Mohamed, C. Périgaud, S. Peyrottes, J. Uttaro and C. Mathé, New J. Chem.,42,   The discovery that some nucleoside analogues endowed with the unnatural l-configuration can possess biological activities has been a significant breakthrough in antiviral this regard, lamivudine (3TC) was the first l-nucleoside enantiomer approved against HIV and HBV, and several other l-nucleosides are currently under clinical development as antiviral agents.

By Horatio Alger, Jr. - # Read Nucleotide Analogues As Antiviral Agents Acs Symposium Series #, antiviral activity of the nucleotide analogue ribavirin 5 sulfamate donald f smee chapter 9 doi bk ch publication date print august 22 this was a.

Antiviral Research, 5 () Elsevier AVR Review article Metal chelators as potential antiviral agents D.W. Hutchinson Department of Chemistry, University of Warwick, Coventry, W.

Midlands, CV4 7AL, U.K. (Received 9 May ; accepted 28 May ) Summary Metal-chelating compounds can inhibit virus-induced enzymes in infected cells by. Abstract: Background: Nucleoside analogues are well-known antitumor, antiviral, and chemotherapeutic agents.

Alterations on both their sugar and the heterocyclic parts may lead to significant changes in the spectrum of their biological activity and the degree of selective toxicity, as well as in. Oligonucleotide Analogues as Potential Chemotherapeutic Agents G. Zon Chap DOI: /bkch Publication Date (Print): Aug Largely in response to the AIDS epidemic, the amount of research directed toward the discovery of antiviral agents has greatly expanded.

This new volume focuses on the potential of nucleotides to exert potent in vivo antiviral effects. It presents the findings of an international group of scientists who are carrying out research at the forefront of the nucleotide drug design.

The increased antiviral potency could be related to an improved conversion of the prodrug to the biologically active form; however, the reported SI values (–) indicate a low therapeutic potential for this nucleoside to treat flaviviral infections.

45 Further substitutions of GS molecule at the C1′ position with methyl, vinyl. More than half of the book is concerned about acyclic nucleosides analogues.

Also covered are pyrophosphate analogues and oligonucleotide analogues as chemotherapeutic agents. Timely as it was init is a book you should not miss if you work in the field of nucleosides / nucleotides / oligonucleotides / nucleic s: 1.

A series of purine and pyrimidine N-(2-(phosphonomethoxy)ethyl) derivatives bearing aminomethyl, (dimethylamino)methyl, morpholinomethyl, and (trimethylammonio)methyl groups at the 2‘-position were synthesized.

The compounds were prepared by alkylation of the heterocyclic bases with appropriately substituted (aminoalkyl)oxiranes followed by condensation of the resulting intermediates with. In an organic chemistry, largest families of organic compounds are belongs in the heterocyclic compounds.

In our daily life important of heterocyclic compounds are of very essential. It has broad range of application in medicinal chemistry and in agrochemicals products. Applications are also found in as developers, as corrosion inhibitors, sanitizers, as copolymers, antioxidants, dye stuff.

Phosphonated Nucleoside Analogues as Antiviral Agents. January ; DOI: /__ In book: Therapy of Viral Infections (pp) Authors: endowed with an antiviral potential.

T1 - From ribavirin to NAD analogues and back to ribavirin in search for anticancer agents. AU - Pankiewicz, Krzysztof W. AU - Felczak, Krzysztof.

PY - /10/1. Y1 - /10/1. N2 - Ribavirin, a broad-spectrum antiviral agent is used in the clinic alone or. We report the synthesis and antiviral activity of a new family of non-nucleoside antivirals, derived from the 4-keto-1,2-oxathiole-2,2-dioxide (beta-keto-gamma-sultone) heterocyclic system.

analogues as tubulin polymerization inhibitors with antiproliferative activities against tumor cell lines THP1 and MCF7 [29]. Another indole compound, 1,4-bis(di(5-hydroxy-1H-indolyl)methyl)-benzene (SK) (8) (Figure 4), was evaluated for its potential as a pharmaceutical compound for cancer treatment through a well-designed.

Current available drugs for antiviral therapy of CMV infections include the inhibitors of viral DNA polymerase, such as the nucleoside analog ganciclovir, the nucleotide analog cidofovir, and the pyrophosphate analogue foscarnet.

All these drugs have low oral bioavailability and dose-related toxicities, and therefore new antiviral agents with. Antiviral agents are effective inhibitors of these virus specific enzymes. As viruses direct the cell machinery for effective viral replication, an effective antiviral agent must prevent completion of the viral growth cycle in the infected cell without being toxic to the surrounding normal cells (Desselberger, ).

Ganciclovir [10] is a structurally related antiviral agent that has been used for the treatment of cytomegalovirus infections in AIDS patient and in recipients of organ transplants.

Cladribine (Leustatin) 32 [11] and Pentostatin 33 [12] are drugs, used to treat hairy cel leukaemia (leukemic reticuloendotheliosis) and multiple sclerosis. Current Fields of Interest: Medicinal/Synthetic Bioorganic/Organic Chemistry and Drug Design: Discovery, design and synthesis of nucleoside/nucleotide and heterocyclic enzyme inhibitors with chemotherapeutic emphasis in the areas of antiviral, anticancer, antibiotic, and antiparasitic y goals include development of potent inhibitors to shut down disease replication pathways.

Purine analogues and their oral prodrugs have also been described as well as other antiviral drugs, such as foscarnet that inhibits pyrophosphate binding site on viral DNA polymerases, while numerous novel compounds have been investigated against FHV-1 including siRNAs which target the FHV-1 glycoprotein D (gD) alone or jointly with DNA.

Acyclic nucleoside diphosphonate derivatives of purines and pyrimidines were prepared by Mitsunobu reaction of suitably protected heterocyclic bases with alcohols containing the (phosphonomethyl)phosphanyl moiety. Furthermore, nonhydrolyzable acyclic analogues of dUDP were prepared as potential inhibitors of dUTPase.

Carbocyclic nucleoside analogues are an essential class of antiviral agents and are commonly used in the treatment of viral diseases (hepatitis B, AIDS). Recently, we reported the racemic synthesis and the anti-human immunodeficiency virus activities (HIV) of 3′-fluoro-5′-norcarbocyclic nucleoside phosphonates bearing purines as heterocyclic base.

Thus, there appears to be a real need for a review article summarising the benzothiazolyl antiviral agents.

This mini‐review makes no attempt to be comprehensive but highlights the potential of benzothiazole analogues against various viral diseases with a focus on structure–activity relationships (SAR), as well as their molecular targets. Get this from a library. Nucleotide analogues as antiviral agents: developed from a symposium sponsored by the Division of Carbohydrate Chemistry and the Division of Medicinal Chemistry at the th National Meeting of the American Chemical Society, Los Angeles, California, September[John C Martin; American Chemical Society.

Cosalane and related compounds are a peculiar group of anti-HIV agents with activities against a broad range of viral targets, such as viral entry and reverse transcriptase (RT). Cosalane and its analogues having anionic pharmacophore inhibit the binding of gp to CD4 as well as the fusion of the viral envelope with the cell membrane.

Compounds 7, 16 and 26 containing a morpholine fragment exhibited the highest efficiency as agents inhibiting the replication of the influenza virus A(H1N1) with selectivity indices of 82, 45 correspondingly. Derivatives 9 (SI = 23) and 18 (SI = 25) containing a 1-methylpiperazine motif showed moderate antiviral activity.

Structure. A broad-spectrum antiviral small molecule is reported to act as an inhibitor of viral polymerase activity and is shown to be effective in protecting non-human primates from lethal filovirus.

A practical and convenient methodology for the synthesis of chiral cyclopentenol derivative (+)a has been developed as the key intermediate that was utilized for the synthesis of biologically active carbocyclic nucleosides. The selective protection of allylic hydroxyl group followed by the ring-closing metathesis (RCM) reaction with Grubbs catalysts provided (+)a on a 10 g scale with 52%.

Holy, A. et al. Acyclic nucleotide analogues: synthesis, antiviral activity and inhibitory effects on some cellular and virus-encoded enzymes in vitro. Antiviral Res. 13, – (). CAS. INTRODUCTION. Over the course of human civilization, viral infections have caused millions of human casualties worldwide, driving the development of antiviral drugs in a pressing need (1, 2).A new era of antiviral drug development has begun since the first antiviral drug, idoxuridine, was approved in June ().Since then, many antiviral drugs have been developed for clinical use to treat.

• Describes the design, synthesis and antiviral evaluation of new conjugated compounds of ef, Medline, CAS, Google Scholar; 4 Bandarage UK, Clark MP, Perola E et al. Novel 2-substituted 7-azaindole and 7-azaindazole analogues as potential antiviral agents for the treatment of influenza.

Antiviral Phytochemicals Several hundred plant and herb species that have potential as novel antiviral agents have been studied. A wide variety of active phytochemicals Flavonoids, terpenoids, lignans, sulphides, polyphenolics, coumarins, saponins, furyl compounds, alkaloids, polyines, thiophenes, proteins and peptides have been identified.

Two main ways: 1. Viral thymidine kinase preferentially kicks off first phosphorylation of prodrug. Acycloguanosine triphosphate (ACG-PPP) is ten times more effective against herpesvirus DNA polymerase than against cellular DNA polymerase alpha, because the viral enzyme has a much higher affinity for ACG-PPP than does the cellular enzyme.

Pyrophosphate analogues. The antiviral drug foscarnet is used to treat CMV retinitis in the patient with AIDS. It’s also used to treat acyclovir-resistant HSV infections in the immunocompromised patient.

Pharmacokinetics. Foscarnet is poorly bound to plasma proteins. In patients with normal kidney function, the majority of foscarnet is.

2-Heterocyclic indolesulfones as inhibitors of HIV-1 reverse transcriptase. Novel isomeric dideoxynucleosides as potential antiviral agents. Tetrahedron, Vol. 50, No. 26 Synthesis of Some New Nucleoside Analogues as Potential Antiviral Agents. Nucleosides and .Heterocyclic antidepressants inhibit the nerve cells' ability to reuptake norepinephrine and group of drugs, once the mainstay of treatment, include: .Pyrophosphate is the first member of an entire series of polyphosphates.

The term pyrophosphate is also the name of esters formed by the condensation of a phosphorylated biological compound with inorganic phosphate, as for dimethylallyl pyrophosphate.

This bond is also referred to as a high-energy phosphate bond.