2. Academic Validation
  3. Novel metronidazole-chalcone conjugates with potential to counter drug resistance in Trichomonas vaginalis

Novel metronidazole-chalcone conjugates with potential to counter drug resistance in Trichomonas vaginalis

  • Eur J Med Chem. 2014 May 22:79:89-94. doi: 10.1016/j.ejmech.2014.03.076.
Amit Anthwal 1,  U Chinna Rajesh 2,  M S M Rawat 3,  Bhavana Kushwaha 4,  Jagdamba P Maikhuri 4,  Vishnu L Sharma 5,  Gopal Gupta 4,  Diwan S Rawat 6
Affiliations

Affiliations

  • 1 Department of Chemistry, H.N.B. Garhwal University (A Central University), Srinagar (Garhwal), Uttarakhand 246174, India; Department of Chemistry, University of Delhi, Delhi 110007, India.
  • 2 Department of Chemistry, University of Delhi, Delhi 110007, India.
  • 3 Department of Chemistry, H.N.B. Garhwal University (A Central University), Srinagar (Garhwal), Uttarakhand 246174, India. Electronic address: [email protected].
  • 4 Division of Endocrinology, CSIR-Central Drug Research Institute, Lucknow 226031, India.
  • 5 Division of Medicinal & Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226031, India.
  • 6 Department of Chemistry, University of Delhi, Delhi 110007, India. Electronic address: [email protected].
PMID: 24727243 DOI: 10.1016/j.ejmech.2014.03.076
Abstract

Trichomoniasis is the most prevalent, curable sexually transmitted disease (STD), which increases risk of viral STDs and HIV. However, drug resistance has been developed by some strains of Trichomonas vaginalis against Metronidazole (MTZ), the FDA approved drug against trichomoniasis. In the present study twenty two chalcone hybrids of metronidazole have been synthesized in a quest to get new molecules with higher potential against metronidazole-resistant T. vaginalis. All new hybrid molecules were found active against T. vaginalis with varying levels of activity against MTZ-susceptible and resistant strains. Eight compounds (4a, 4c, 4d, 4e, 4f, 4h, 4q and 4s) were found as active as the standard drug with an MIC of 1.56 μg/ml against MTZ-susceptible strain. However, compounds 4e, 4h and 4m were 4-times more active than MTZ against drug-resistant T. vaginalis, amongst which 4e and 4h were most promising against both susceptible and resistant strains.

Keywords

Drug resistance; HeLa cell line; Metronidazole; Trichomonas vaginalis.

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