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; Arien, Kevin K.; Botta, Maurizio published the artcile< 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>, Synthetic Route of 197638-83-8, the main research area is HIV1 antiviral gel dihydroalkyloxybenzyl oxopyrimidine.
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, mols. 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 mol. modeling. At the same time, a vaginal microbicide gel formulation was developed and tested for one of the most promising candidates.
Journal of Medicinal Chemistry published new progress about Anti-HIV agents. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Synthetic Route of 197638-83-8.
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics