Design, synthesis, and biological activity of a novel series of 2, 5-disubstituted furans/pyrroles as HIV-1 fusion inhibitors targeting gp41

…, NE Abo-Dya, A Abdelmajeid, AK Debnath…

Index: Jiang, Shibo; Tala, Srinivasa R.; Lu, Hong; Zou, Peng; Avan, Ilker; Ibrahim, Tarek S.; Abo-Dya, Nader E.; Abdelmajeid, Abdelmotaal; Debnath, Asim K.; Katritzky, Alan R. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 22 p. 6895 - 6898

Full Text: HTML

Citation Number: 16

Abstract

Based on molecular docking analysis of earlier results, we designed a series of 2, 5- disubstituted furans/pyrroles (5a–h) as HIV-1 entry inhibitors. Compounds were synthesized by Suzuki–Miyaura cross coupling, followed by a Knoevenagel condensation or Wittig reaction. Four of these compounds were found to be effective in inhibiting HIV-1 infection, with the best compounds being 5f and 5h, which exhibited significant inhibition on HIV- ...