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Iran J Basic Med Sci. 2017 Sep;20(9):975-989. doi: 10.22038/IJBMS.2017.9260.

Synthesis, characterization, molecular docking studies and biological evaluation of some novel hybrids based on quinazolinone, benzofuran and imidazolium moieties as potential cytotoxic and antimicrobial agents.

Iranian journal of basic medical sciences

Parvin Asadi, Ghadamali Khodarahmi, Ali Jahanian-Najafabadi, Lotfollah Saghaie, Farshid Hassanzadeh

Affiliations

  1. Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran.
  2. Department of Pharmaceutical Biotechnology, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran.

PMID: 29085591 PMCID: PMC5651464 DOI: 10.22038/IJBMS.2017.9260

Abstract

OBJECTIVES: Hybridization of bioactive natural and synthetic compounds is one of the most promising novel approaches for the design of hit and lead compounds with new molecular structures. In this investigation, a series of novel hybrid structures bearing quinazolinone, benzofuran and imidazolium moieties were designed and synthesized.

MATERIALS AND METHODS: Novel hybrid compounds were prepared and their structures were characterized by spectral and analytical data. In order to evaluate the biological activities, the synthesized hybrid compounds were studied for

RESULTS: The results of antimicrobial activity showed that compound 14e, with two halogen atoms on quinazolinone and benzofuran was the most active against all the tested strains of microorganisms with the MIC value 16-128 µg/ml. Some of the tested compounds showed good cytotoxicity on MCF-7, and compound 14c with IC

CONCLUSION: Based on the obtained results, the hybrid derivatives of quinazolinone, benzofuran and imidazolium could be regarded as efficient candidates for further molecular developments of anticancer and antimicrobial agents.

Keywords: Antibacterial; Benzofuran; Cytotoxic; Imidazolium salt; QM/MM Docking; Quinazolinone

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