2. Academic Validation
  3. 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

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

  • J Med Chem. 2016 Mar 24;59(6):2747-59. doi: 10.1021/acs.jmedchem.5b01979.
Cristina Tintori 1,  Annalaura Brai 1,  Maria Chiara Dasso Lang 1,  Davide Deodato 1,  Antonia Michela Greco 1,  Bruno Mattia Bizzarri 1,  Lorena Cascone 1,  Alexandru Casian 1,  Claudio Zamperini 1,  Elena Dreassi 1,  Emmanuele Crespan 2,  Giovanni Maga 2,  Guido Vanham 3,  Elisa Ceresola 4,  Filippo Canducci 4,  Kevin K Ariën 3,  Maurizio Botta 1 5
Affiliations

Affiliations

  • 1 Dipartimento Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena , Via A. De Gasperi 2, I-53100 Siena, Italy.
  • 2 Istituto di Genetica Molecolare, IGM-CNR, Via Abbiategrasso 207, I-27100 Pavia, Italy.
  • 3 Virology Unit, Institute of Tropical Medicine , Nationalestraat 155, B-2000 Antwerpen, Belgium.
  • 4 Department of Biotechnology and Life Sciences, University of Insubria , Dunant 3, 21100, Varese, Italy.
  • 5 Biotechnology College of Science and Technology, Temple University , Biolife Science Building, Suite 333, 1900 N 12th Street, Philadelphia, Pennsylvania 19122, United States.
PMID: 26898379 DOI: 10.1021/acs.jmedchem.5b01979
Abstract

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.

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