BIOMAT Database Logo BIOMAT Database Logo

New 2-Oxoimidazolidine Derivatives: Design, Synthesis and Evaluation of Anti-BK Virus Activities in Vitro. 2019

Yurii Kornii, and Svitlana Chumachenko, and Oleg Shablykin, and Mark N Prichard, and Scott H James, and Caroll Hartline, and Victor Zhirnov, and Volodymyr Brovarets
Department of Chemistry of Bioactive Nitrogen-Containing Heterocyclic Bases, V. P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry, NAS of Ukraine, 1, Murmanska Str., Kyiv, 02094, Ukraine.

A series of novel 2-oxoimidazolidine derivatives were synthesized and their antiviral activities against BK human polyomavirus type 1 (BKPyV) were evaluated in vitro. Bioassays showed that the synthesized compounds 1-{[(4E)-5-(dichloromethylidene)-2-oxoimidazolidin-4-ylidene]sulfamoyl}piperidine-4-carboxylic acid (5) and N-Cyclobutyl-N'-[(4E)-5-(dichloromethylidene)-2-oxoimidazolidin-4-ylidene]sulfuric diamide (4) exhibited moderate activities against BKPyV (EC50 =5.4 and 5.5 μm, respectively) that are comparable to the standard drug Cidofovir. Compound 5 exhibited the same cytotoxicity in HFF cells and selectivity index (SI50 ) as Cidofovir. The selectivity index of compound 4 is three times less than that of Cidofovir due to the higher toxicity of this compound. Hence, these compounds may be taken as lead compound for further development of novel ant-BKPyV agents.

UI MeSH Term Description Entries
D008826 Microbial Sensitivity Tests Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses). Bacterial Sensitivity Tests,Drug Sensitivity Assay, Microbial,Minimum Inhibitory Concentration,Antibacterial Susceptibility Breakpoint Determination,Antibiogram,Antimicrobial Susceptibility Breakpoint Determination,Bacterial Sensitivity Test,Breakpoint Determination, Antibacterial Susceptibility,Breakpoint Determination, Antimicrobial Susceptibility,Fungal Drug Sensitivity Tests,Fungus Drug Sensitivity Tests,Sensitivity Test, Bacterial,Sensitivity Tests, Bacterial,Test, Bacterial Sensitivity,Tests, Bacterial Sensitivity,Viral Drug Sensitivity Tests,Virus Drug Sensitivity Tests,Antibiograms,Concentration, Minimum Inhibitory,Concentrations, Minimum Inhibitory,Inhibitory Concentration, Minimum,Inhibitory Concentrations, Minimum,Microbial Sensitivity Test,Minimum Inhibitory Concentrations,Sensitivity Test, Microbial,Sensitivity Tests, Microbial,Test, Microbial Sensitivity,Tests, Microbial Sensitivity
D001739 BK Virus A species of POLYOMAVIRUS apparently infecting over 90% of children but not clearly associated with any clinical illness in childhood. The virus remains latent in the body throughout life and can be reactivated under certain circumstances. BK polyomavirus,Human Polyomavirus BK,Polyomavirus, BK,Polyomavirus hominis 1,Polyomavirus BK, Human
D002470 Cell Survival The span of viability of a cell characterized by the capacity to perform certain functions such as metabolism, growth, reproduction, some form of responsiveness, and adaptability. Cell Viability,Cell Viabilities,Survival, Cell,Viabilities, Cell,Viability, Cell
D002478 Cells, Cultured Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others. Cultured Cells,Cell, Cultured,Cultured Cell
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000077404 Cidofovir An acyclic nucleoside phosphonate that acts as a competitive inhibitor of viral DNA polymerases. It is used in the treatment of RETINITIS caused by CYTOMEGALOVIRUS INFECTIONS and may also be useful for treating HERPESVIRUS INFECTIONS. 1-((3-Hydroxy-2-phosphonylmethoxy)propyl)cytosine,1-(3-Hydroxy-2-phosphonylmethoxypropyl)cytosine,Cidofovir Anhydrous,Cidofovir Sodium,Cidofovir, (+-)-isomer,Cidofovir, (R)-isomer,Cidofovir, Sodium Salt,GS 504,GS-504,HPMPC,Vistide,GS504
D000998 Antiviral Agents Agents used in the prophylaxis or therapy of VIRUS DISEASES. Some of the ways they may act include preventing viral replication by inhibiting viral DNA polymerase; binding to specific cell-surface receptors and inhibiting viral penetration or uncoating; inhibiting viral protein synthesis; or blocking late stages of virus assembly. Antiviral,Antiviral Agent,Antiviral Drug,Antivirals,Antiviral Drugs,Agent, Antiviral,Agents, Antiviral,Drug, Antiviral,Drugs, Antiviral
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D014779 Virus Replication The process of intracellular viral multiplication, consisting of the synthesis of PROTEINS; NUCLEIC ACIDS; and sometimes LIPIDS, and their assembly into a new infectious particle. Viral Replication,Replication, Viral,Replication, Virus,Replications, Viral,Replications, Virus,Viral Replications,Virus Replications

Related Publications

Yurii Kornii, and Svitlana Chumachenko, and Oleg Shablykin, and Mark N Prichard, and Scott H James, and Caroll Hartline, and Victor Zhirnov, and Volodymyr Brovarets
Design, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives.
September 2018, European journal of medicinal chemistry,
Yurii Kornii, and Svitlana Chumachenko, and Oleg Shablykin, and Mark N Prichard, and Scott H James, and Caroll Hartline, and Victor Zhirnov, and Volodymyr Brovarets
2-Azetidinone derivatives: design, synthesis, in vitro anti-microbial, cytotoxic activities and DNA cleavage study.
December 2009, European journal of medicinal chemistry,
Yurii Kornii, and Svitlana Chumachenko, and Oleg Shablykin, and Mark N Prichard, and Scott H James, and Caroll Hartline, and Victor Zhirnov, and Volodymyr Brovarets
Design, synthesis and anti-plasmodial evaluation in vitro of new 4-aminoquinoline isatin derivatives.
May 2005, Bioorganic & medicinal chemistry,
Yurii Kornii, and Svitlana Chumachenko, and Oleg Shablykin, and Mark N Prichard, and Scott H James, and Caroll Hartline, and Victor Zhirnov, and Volodymyr Brovarets
Design, Synthesis, and Evaluation of Anticonvulsant Activities of New Triazolopyrimidine Derivatives.
January 2022, Frontiers in chemistry,
Yurii Kornii, and Svitlana Chumachenko, and Oleg Shablykin, and Mark N Prichard, and Scott H James, and Caroll Hartline, and Victor Zhirnov, and Volodymyr Brovarets
Anti-HBV agents. Part 2: synthesis and in vitro anti-hepatitis B virus activities of alisol A derivatives.
April 2009, Bioorganic & medicinal chemistry letters,
Yurii Kornii, and Svitlana Chumachenko, and Oleg Shablykin, and Mark N Prichard, and Scott H James, and Caroll Hartline, and Victor Zhirnov, and Volodymyr Brovarets
Design, synthesis, and antihepatitis B virus activities of novel 2-pyridone derivatives.
January 2010, Journal of medicinal chemistry,
Yurii Kornii, and Svitlana Chumachenko, and Oleg Shablykin, and Mark N Prichard, and Scott H James, and Caroll Hartline, and Victor Zhirnov, and Volodymyr Brovarets
Design, synthesis and evaluation of cytotoxic, antimicrobial, and anti-HIV-1 activities of new 1,2,3,4-tetrahydropyrimidine derivatives.
April 2019, Research in pharmaceutical sciences,
Yurii Kornii, and Svitlana Chumachenko, and Oleg Shablykin, and Mark N Prichard, and Scott H James, and Caroll Hartline, and Victor Zhirnov, and Volodymyr Brovarets
New 2-alkylthio-1-benzylimidazole-5-carboxylic acid derivatives targeting gp41: design, synthesis and in vitro anti-HIV activity evaluation.
June 2022, Current HIV research,
Yurii Kornii, and Svitlana Chumachenko, and Oleg Shablykin, and Mark N Prichard, and Scott H James, and Caroll Hartline, and Victor Zhirnov, and Volodymyr Brovarets
Design, synthesis, and in vitro evaluation of thiosemicarbazone derivatives as anti-filarial agents.
October 2022, Experimental parasitology,
Yurii Kornii, and Svitlana Chumachenko, and Oleg Shablykin, and Mark N Prichard, and Scott H James, and Caroll Hartline, and Victor Zhirnov, and Volodymyr Brovarets
Design, synthesis and in vitro anti-mycobacterial activities of homonuclear and heteronuclear bis-isatin derivatives.
June 2018, Fitoterapia,
Copied contents to your clipboard!