Synthesis, characterization, and biological activities of new benzofuran derivatives

Kifah S.M. Salih, Mikdad T. Ayoub, Haythem A. Saadeh, Najim A. Al-Masoudi, Mohammad S. Mubarak

Research output: Contribution to journalArticlepeer-review

14 Citations (Scopus)


A number of new benzofuran derivatives, ethyl 3-[(alkylamino)methyl]-6-methoxy-1-benzofuran-2-carboxylates (5a-i), were obtained via the reaction between ethyl 3-(bromomethyl)-6-methoxy-1-benzofuran-2-carboxylate (3) and amines or amino acid ethyl esters. In addition, 1,4-bis[(ethyl 6-methoxy-1-benzofuran-3-yl-2-carboxylate)methyl]piperazine (9), N,N′-diethyl-N,N′-bis[(6-methoxy-1-benzofuran-3-yl-2-carboxy late)methyl]but-2-ene-1,4-diamine (10) and 1,2-bis[(ethyl 6-methoxy-1-benzofuran-3-yl-2-carboxylate)methyl]- 1,2-dimethyl-hydrazine (11) were also obtained from the reaction of 3 with diamines. Their in vitro anti-HIV-1 (strain IIIB) and HIV-2 (strain ROD) activities of the synthesized compounds in human T-lymphocyte were tested; ethyl 3-bromomethyl-6-methoxycoumarlate displayed an ability to inhibit HIV-1 and HIV-2 replication in cell culture at non-toxic concentrations.

Original languageEnglish
Pages (from-to)1577-1587
Number of pages11
Issue number7
Publication statusPublished - Jul 1 2007
Externally publishedYes


  • 3-Bromomethyl-2-carbethoxy-6-methoxybenzofuran
  • Amino Acid Ethyl Ester
  • Benzofuran
  • Cyclization
  • HIV

ASJC Scopus subject areas

  • Analytical Chemistry
  • Pharmacology
  • Organic Chemistry


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