Preliminary Anti-Coxsackie Activity of Novel 1-[4-(5,6-dimethyl(H)- 1H(2H)-benzotriazol-1(2)-yl)phenyl]-3-alkyl(aryl)ureas

2020 ◽  
Vol 16 (5) ◽  
pp. 677-688 ◽  
Author(s):  
Sandra Piras ◽  
Paola Corona ◽  
Roberta Ibba ◽  
Federico Riu ◽  
Gabriele Murineddu ◽  
...  
Keyword(s):  
Chronic Disease ◽  
Antiviral Activity ◽  
Wide Spectrum ◽  
Immunocompromised Patients ◽  
Human Pathogen ◽  
Alkyl Aryl ◽  
Dna Viruses ◽  
Coxsackievirus B ◽  
Selective Activity

Background: Coxsackievirus infections are associated with cases of aseptic meningitis, encephalitis, myocarditis, and some chronic disease. Methods: A series of benzo[d][1,2,3]triazol-1(2)-yl derivatives (here named benzotriazol-1(2)-yl) (4a-i, 5a-h, 6a-e, g, i, j and 7a-f, h-j) were designed, synthesized and in vitro evaluated for cytotoxicity and antiviral activity against two important human enteroviruses (HEVs) members of the Picornaviridae family [Coxsackievirus B 5 (CVB-5) and Poliovirus 1 (Sb-1)]. Results: Compounds 4c (CC50 >100 μM; EC50 = 9 μM), 5g (CC50 >100 μM; EC50 = 8 μM), and 6a (CC50 >100 μM; EC50 = 10 μM) were found active against CVB-5. With the aim of evaluating the selectivity of action of this class of compounds, a wide spectrum of RNA (positive- and negativesense), double-stranded (dsRNA) or DNA viruses were also assayed. For none of them, significant antiviral activity was determined. Conclusion: These results point towards a selective activity against CVB-5, an important human pathogen that causes both acute and chronic diseases in infants, young children, and immunocompromised patients.

ChemInform Abstract: ANTIVIRAL ACTIVITY OF SOME β-DIKETONES. 1. ARYL ALKYL DIKETONES. IN VITRO ACTIVITY AGAINST BOTH RNA AND DNA VIRUSES

1977 ◽  
Vol 8 (42) ◽  
pp. no-no
Author(s):  
G. D. DIANA ◽  
U. J. SALVADOR ◽  
E. S. ZALAY ◽  
R. E. JOHNSON ◽  
J. C. COLLINS ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Dna Viruses ◽  
Rna And Dna

scholarly journals 4′-Ethynyl Nucleoside Analogs: Potent Inhibitors of Multidrug-Resistant Human Immunodeficiency Virus Variants In Vitro

2001 ◽  
Vol 45 (5) ◽  
pp. 1539-1546 ◽  
Author(s):  
Ei-Ichi Kodama ◽  
Satoru Kohgo ◽  
Kenji Kitano ◽  
Haruhiko Machida ◽  
Hiroyuki Gatanaga ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Reverse Transcriptase ◽  
Wide Spectrum ◽  
Nucleoside Analogs ◽  
Transcriptase Inhibitor ◽  
Multidrug Resistant ◽  
Human Immunodeficiency Viruses ◽  
Reverse Transcriptase Inhibitor ◽  
Hiv 1

ABSTRACT A series of 4′-ethynyl (4′-E) nucleoside analogs were designed, synthesized, and identified as being active against a wide spectrum of human immunodeficiency viruses (HIV), including a variety of laboratory strains of HIV-1, HIV-2, and primary clinical HIV-1 isolates. Among such analogs examined, 4′-E-2′-deoxycytidine (4′-E-dC), 4′-E-2′-deoxyadenosine (4′-E-dA), 4′-E-2′-deoxyribofuranosyl-2,6-diaminopurine, and 4′-E-2′-deoxyguanosine were the most potent and blocked HIV-1 replication with 50% effective concentrations ranging from 0.0003 to 0.01 μM in vitro with favorable cellular toxicity profiles (selectivity indices ranging 458 to 2,600). These 4′-E analogs also suppressed replication of various drug-resistant HIV-1 clones, including HIV-1M41L/T215Y, HIV-1K65R, HIV-1L74V, HIV-1M41L/T69S-S-G/T215Y, and HIV-1A62V/V75I/F77L/F116Y/Q151M. Moreover, these analogs inhibited the replication of multidrug-resistant clinical HIV-1 strains carrying a variety of drug resistance-related amino acid substitutions isolated from HIV-1-infected individuals for whom 10 or 11 different anti-HIV-1 agents had failed. The 4′-E analogs also blocked the replication of a non-nucleoside reverse transcriptase inhibitor-resistant clone, HIV-1Y181C, and showed an HIV-1 inhibition profile similar to that of zidovudine in time-of-drug-addition assays. The antiviral activity of 4′-E-thymidine and 4′-E-dC was blocked by the addition of thymidine and 2′-deoxycytidine, respectively, while that of 4′-E-dA was not affected by 2′-deoxyadenosine, similar to the antiviral activity reversion feature of 2′,3′-dideoxynucleosides, strongly suggesting that 4′-Eanalogs belong to the family of nucleoside reverse transcriptase inhibitors. Further development of 4′-E analogs as potential therapeutics for infection with multidrug-resistant HIV-1 is warranted.

Antiviral activity of some .beta.-diketones. 1. Aryl alkyl diketones. In vitro activity against both RNA and DNA viruses

1977 ◽  
Vol 20 (6) ◽  
pp. 750-756 ◽  
Author(s):  
Guy D. Diana ◽  
U. Joseph Salvador ◽  
Ethel S. Zalay ◽  
Robert E. Johnson ◽  
Joseph C. Collins ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Dna Viruses ◽  
Rna And Dna

ChemInform Abstract: ANTIVIRAL ACTIVITY OF SOME β-DIKETONES. 2. ARYLOXY ALKYL DIKETONES. IN VITRO ACTIVITY AGAINST BOTH RNA AND DNA VIRUSES

1977 ◽  
Vol 8 (42) ◽  
pp. no-no
Author(s):  
G. D. DIANA ◽  
U. J. SALVADOR ◽  
E. S. ZALAY ◽  
P. M. CARABATEAS ◽  
G. L. WILLIAMS ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Dna Viruses ◽  
Rna And Dna

Mx1, Mx2 and Mx3 proteins from the gilthead seabream (Sparus aurata) show in vitro antiviral activity against RNA and DNA viruses

2013 ◽  
Vol 56 (4) ◽  
pp. 630-636 ◽  
Author(s):  
M.A. Fernández-Trujillo ◽  
E. García-Rosado ◽  
M.C. Alonso ◽  
D. Castro ◽  
M.C. Álvarez ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Sparus Aurata ◽  
Gilthead Seabream ◽  
Dna Viruses ◽  
Rna And Dna

scholarly journals Antivirals Against Chikungunya Virus: Is the Solution in Nature?

Viruses ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 272 ◽  
Author(s):  
Daniel Oliveira Silva Martins ◽  
Igor de Andrade Santos ◽  
Débora Moraes de Oliveira ◽  
Victória Riquena Grosche ◽  
Ana Carolina Gomes Jardim
Keyword(s):  
Chronic Disease ◽  
Hepatitis C ◽  
Antiviral Activity ◽  
Yellow Fever ◽  
Chikungunya Virus ◽  
Natural Compounds ◽  
Southwest Asia ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

The worldwide outbreaks of the chikungunya virus (CHIKV) in the last years demonstrated the need for studies to screen antivirals against CHIKV. The virus was first isolated in Tanzania in 1952 and was responsible for outbreaks in Africa and Southwest Asia in subsequent years. Between 2007 and 2014, some cases were documented in Europe and America. The infection is associated with low rates of death; however, it can progress to a chronic disease characterized by severe arthralgias in infected patients. This infection is also associated with Guillain–Barré syndrome. There is no specific antivirus against CHIKV. Treatment of infected patients is palliative and based on analgesics and non-steroidal anti-inflammatory drugs to reduce arthralgias. Several natural molecules have been described as antiviruses against viruses such as dengue, yellow fever, hepatitis C, and influenza. This review aims to summarize the natural compounds that have demonstrated antiviral activity against chikungunya virus in vitro.

Antiviral activity of some .beta.-diketones. 2. Aryloxy alkyl diketones. In vitro activity against both RNA and DNA viruses

1977 ◽  
Vol 20 (6) ◽  
pp. 757-761 ◽  
Author(s):  
Guy D. Diana ◽  
U. Joseph Salvador ◽  
Ethel S. Zalay ◽  
Philip M. Carabateas ◽  
Gordon L. Williams ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Dna Viruses ◽  
Rna And Dna

scholarly journals Antiviral Activities of Novel 5-Phosphono-Pent-2-en-1-yl Nucleosides and Their Alkoxyalkyl Phosphonoesters

2006 ◽  
Vol 51 (2) ◽  
pp. 611-615 ◽  
Author(s):  
Hyunah Choo ◽  
James R. Beadle ◽  
Earl R. Kern ◽  
Mark N. Prichard ◽  
Kathy A. Keith ◽  
...  
Keyword(s):  
Hepatitis B Virus ◽  
Hepatitis B ◽  
Antiviral Activity ◽  
Oral Bioavailability ◽  
Dna Viruses ◽  
B Virus ◽  
Acyclic Nucleoside Phosphonates ◽  
Antiviral Activities ◽  
Acyclic Nucleoside

ABSTRACT Three acyclic nucleoside phosphonates are currently approved for clinical use against infections caused by cytomegalovirus (Vistide), hepatitis B virus (Hepsera), and human immunodeficiency virus type 1 (Viread). This important antiviral class inhibits viral polymerases after cellular uptake and conversion to their diphosphates, bypassing the first phosphorylation, which is required for conventional nucleoside antivirals. Small chemical alterations in the acyclic side chain lead to marked differences in antiviral activity and the spectrum of activity of acyclic nucleoside phosphonates against various classes of viral agents. We synthesized a new class of acyclic nucleoside phosphonates based on a 5-phosphono-pent-2-en-1-yl base motif in which the oxygen heteroatom usually present in acyclic nucleoside phosphonates has been replaced with a double bond. Since the intrinsic phosphonate moiety leads to low oral bioavailability and impaired cellular penetration, we also prepared the hexadecyloxypropyl esters of the 5-phosphono-pent-2-en-1-yl nucleosides. Our earlier work showed that this markedly increases antiviral activity and oral bioavailability. Although the 5-phosphono-pent-2-en-1-yl nucleosides themselves were not active, the hexadecyloxypropyl esters were active against DNA viruses and hepatitis B virus, in vitro. Notably, the hexadecyloxypropyl ester of 9-(5-phosphono-pent-2-en-1-yl)-adenine was active against hepatitis B virus mutants resistant to lamivudine, emtricitabine, and adefovir.

Antiviral activity of some .beta.-diketones. 4. Benzyl diketones. In vitro activity against both RNA and DNA viruses

1978 ◽  
Vol 21 (9) ◽  
pp. 889-894 ◽  
Author(s):  
G. D. Diana ◽  
Philip M. Carabateas ◽  
Robert E. Johnson ◽  
Gordon L. Williams ◽  
Francis Pancic ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Dna Viruses ◽  
Rna And Dna

Antiviral Activity ofFolium IsatidisDerived ExtractsIn VitroandIn Vivo

2013 ◽  
Vol 41 (04) ◽  
pp. 957-969 ◽  
Author(s):  
You-Ping Deng ◽  
Yuan-Yuan Liu ◽  
Zhao Liu ◽  
Jin Li ◽  
Ling-Min Zhao ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Influenza A ◽  
Viral Infections ◽  
Antiviral Agent ◽  
Adenovirus Type ◽  
Coxsackie Virus ◽  
Herbaceous Plant ◽  
Dna Viruses ◽  
Syncytial Virus

Folium isatidis is a native Chinese herbaceous plant widely used for medicinal purposes for thousands of years. However, few studies have focused on the leaves of Isatis indigotica. In this report, we isolated a series of four fractions (I–IV) from Folium isatidis and explored the antiviral activity of each tested extract. The extracts were active against a panel of RNA and DNA viruses in vitro, namely influenza A virus (IAV), coxsackie virus B3 (CVB3), respiratory syncytial virus (RSV), and adenovirus type 7 (Ad-7). Oral administration of 200 mg/kg/d of fraction III in mice exerted strong antiviral effects in viral replication, accompanied by prolonged survival rate, attenuated lung tissue damage as well as significant reductions in pulmonary virus titers and lung index. Our results provide the first biochemical evidence that Folium isatidis and its extracts could be used as potential antiviral agent in the postexposure prophylaxis for multiple viral infections.

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