958237-59-7Relevant academic research and scientific papers
Development and in Vitro Evaluation of a Microbicide Gel Formulation for a Novel Non-Nucleoside Reverse Transcriptase Inhibitor Belonging to the N-Dihydroalkyloxybenzyloxopyrimidines (N-DABOs) Family
Tintori, Cristina,Brai, Annalaura,Dasso Lang, Maria Chiara,Deodato, Davide,Greco, Antonia Michela,Bizzarri, Bruno Mattia,Cascone, Lorena,Casian, Alexandru,Zamperini, Claudio,Dreassi, Elena,Crespan, Emmanuele,Maga, Giovanni,Vanham, Guido,Ceresola, Elisa,Canducci, Filippo,Ari?n, Kevin K.,Botta, Maurizio
, p. 2747 - 2759 (2016/04/10)
Preventing HIV transmission by the use of a vaginal microbicide is a topic of considerable interest in the fight against AIDS. Both a potent anti-HIV agent and an efficient formulation are required to develop a successful microbicide. In this regard, molecules able to inhibit the HIV replication before the integration of the viral DNA into the genetic material of the host cells, such as entry inhibitors or reverse transcriptase inhibitors (RTIs), are ideal candidates for prevention purpose. Among RTIs, S- and N-dihydroalkyloxybenzyloxopyrimidines (S-DABOs and N-DABOs) are interesting compounds active at nanomolar concentration against wild type of RT and with a very interesting activity against RT mutations. Herein, novel N-DABOs were synthesized and tested as anti-HIV agents. Furthermore, their mode of binding was studied by molecular modeling. At the same time, a vaginal microbicide gel formulation was developed and tested for one of the most promising candidates.
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
