221121-33-1Relevant articles and documents
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity
Manetti, Fabrizio,Esté, José A.,Clotet-Codina, Imma,Armand-Ugón, Mercedes,Maga, Giovanni,Crespan, Emmanuele,Cancio, Reynel,Mugnaini, Claudia,Bernardini, Cesare,Togninelli, Andrea,Carmi, Caterina,Alongi, Maddalena,Petricci, Elena,Massa, Silvio,Corelli, Federico,Botta, Maurizio
, p. 8000 - 8008 (2005)
A simple and efficient methodology for the parallel solution-phase synthesis has been set up to obtain a series of thiouracils, in turn selectively S-benzylated under microwave irradiation to give new S-DABOs. Biological screening led to the identificatio
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains
Mai, Antonello,Artico, Marino,Rotili, Dante,Tarantino, Domenico,Clotet-Codina, Imma,Armand-Ugón, Mercedes,Ragno, Rino,Simeoni, Silvia,Sbardella, Gianluca,Nawrozkij, Maxim B.,Samuele, Alberta,Maga, Giovanni,Esté, José A.
, p. 5412 - 5424 (2008/03/13)
Following the disclosure of dihydro-alkoxy-, dihydro-alkylthio-, and dihydro-alkylamino-benzyl-oxopyrimidines (DABOs, S-DABOs, and NH-DABOs) as potent and selective anti-HIV-1 agents belonging to the non-nucleoside reverse transcriptase inhibitor (NNRTI)
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
Mugnaini, Claudia,Alongi, Maddalena,Togninelli, Andrea,Gevariya, Harsukh,Brizzi, Antonella,Manetti, Fabrizio,Bernardini, Cesare,Angeli, Lucilla,Tafi, Andrea,Bellucci, Luca,Corelli, Federico,Massa, Silvio,Maga, Giovanni,Samuele, Alberta,Facchini, Marcella,Clotet-Codina, Imma,Armand-Ugón, Mercedes,Esté, José A.,Botta, Maurizio
, p. 6580 - 6595 (2008/04/12)
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?
Sbardella, Gianluca,Mai, Antonello,Artico, Marino,Massa, Silvio,Marceddu, Tiziana,Vargiu, Laura,Marongiu, Maria Elena,La Colla, Paolo
, p. 30 - 39 (2007/10/03)
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.
5-alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3,4-dihydropyrimidin- 4(3H)-ones: Novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives
Mai, Antonello,Artico, Marino,Sbardella, Gianluca,Massa, Silvio,Novellino, Ettore,Greco, Giovanni,Loi, Anna Giulia,Tramontano, Enzo,Marongiu, Maria Elena,La Colla, Paolo
, p. 619 - 627 (2007/10/03)
Molecular modeling analysis of compounds belonging to the recently published series of dihydro-alkoxy-benzyl-oxopyrimidines (DABOs), such as S- DABOs and DATNOs, gave support to the design of new 2,6-disubstituted benzyl- DABO derivatives as highly potent