293300-23-9

Upstream product

• 654-01-3 (2,6-difluorophenyl)acetonitrile 
• 533-68-6 2-bromobutyric acid ethyl ester 
• 85068-28-6 2,6-difluorophenylacetic acid 
• 221121-33-1 2-(2,6-difluoro-phenyl)-1-imidazol-1-yl-ethanone 

Downstream Products

• 293300-24-0 6-(2,6-difluorophenylmethyl)-3,4-dihydro-5-ethyl-2-thioxopyrimidin-4(3H)-one 
• 1307311-14-3 2-[(4-cyanophenylamino)carbonylmethylthio]-6-(2,6-difluorobenzyl)-5-ethylpyrimidin-4(3H)-one 
• 1304538-62-2 2-[(4-methoxyphenylamino)carbonylmethylthio]-6-(2,6-difluorobenzyl)-5-ethylpyrimidin-4(3H)-one 
• 1304538-61-1 2-[(4-bromophenylamino)carbonylmethylthio]-6-(2,6-difluorobenzyl)-5-ethylpyrimidin-4(3H)-one 
• 1304538-60-0 2-[(4-chlorophenylamino)carbonylmethylthio]-6-(2,6-difluorobenzyl)-5-ethylpyrimidin-4(3H)-one 
• 1307311-12-1 2-[(4-fluorophenylamino)carbonylmethylthio]-6-(2,6-difluorobenzyl)-5-ethylpyrimidin-4(3H)-one 

Relevant academic research and scientific papers

Synthesis and biological evaluation of 6-substituted 5-Alkyl-2-(phenylaminocarbonylmethylthio)pyrimidin-4(3H)-ones as potent HIV-1 NNRTIs

A series of new 5-alkyl-2-phenylaminocarbonylmethylthiopyrimidin-4(3H)-ones bearing variously substituted arylmethyl moieties at the C6 position of the pyrimidine ring were synthesized and evaluated for anti-HIV activity in MT-4 cells. Most of these new c

Discovery of Dihydro-Alkyloxy-Benzyl-Oxopyrimidines as Promising Anti-Influenza Virus Agents

A series of novel dihydro-alkyloxy-benzyl-oxopyrimidine derivatives were synthesized and evaluated for their activity against influenza virus in Madin-Darby canine kidney cells. Four dihydro-alkyloxy-benzyl-oxopyrimidine derivatives (4a1, 4a2, 4a3, and 4d1) showed potent activity against influenza virus. Among them, compound 4a3 was the most promising lead with broad activity against influenza A (antiviral EC50 values of 9 and 18μm for the A/H1N1 and A/H3N2 subtype, respectively) and influenza B viruses (EC50: 33μm). The antiviral mechanism of action of these dihydro-alkyloxy-benzyl-oxopyrimidine derivatives must be quite different from that of the currently approved anti-influenza virus drugs that target the viral M2 or neuraminidase proteins. The dihydro-alkyloxy-benzyl-oxopyrimidine derivatives represent a new avenue for further optimization and development of novel anti-influenza virus agents. Dihydro-alkyloxy-benzyl-oxopyrimidine (DABO) derivatives were discoveried as new anti-influenza agents. Among them, compound 4a3 was the most promising with broad activity against influenza A (A/H1N1 and A/H3N2 subtype) and influenza B virus.

5-alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure - Activity relationship profile

A series of dihydro-alkylthio-benzyl-oxopyrimidines (S-DABOs) bearing a 2-aryl-2-oxoethylsulfanyl chain at pyrimidine C2, an alkyl group at C5, and a 2,6-dichloro-, 2-chloro-6-fluoro-, and 2,6-difluoro-benzyl substitution at C6 (oxophenethyl-S-DABOs, 6-8)

Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: Synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants

A series of novel S-DABO analogues, characterized by different substitution patterns at positions 2, 5, and 6 of the heterocyclic ring, were synthesized in a straightforward fashion by means of parallel synthesis and evaluated as inhibitors of human immun

Does the 2-methylthiomethyl substituent really confer high anti-HIV-1 activity to S-DABOs?

S-DABO derivatives containing the methylthiomethyl (MTM) group have been synthesized and tested for anti-HIV-1 activity in cell-based assay (MTT and p24 assays) and for their capability to target the HIV-1 reverse transcriptase in enzyme assays. Data of experiments lead to the conclusion that the introduction of a 2-MTM-thio side chain is not sufficient per se to significantly increase S-DABO's potency. Nevertheless, potent MTM-S-DABOs can be obtained by introducing a 2,6-difluorophenylmethyl moiety as a C-6 substituent.