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Tatar E, Yaldız S, Kulabaş N, et al. Synthesis and structure-activity relationship of L-methionine-coupled 1,3,4-thiadiazole derivatives with activity against influenza virus. Chem Biol Drug Des. 2021;doi: 10.1111/cbdd.13995.
Tatar, E., Yaldız, S., Kulabaş, N., Vanderlinden, E., Naesens, L., & Küçükgüzel, �. �. (2021). Synthesis and structure-activity relationship of L-methionine-coupled 1,3,4-thiadiazole derivatives with activity against influenza virus. Chemical biology & drug design, . https://doi.org/10.1111/cbdd.13995
Tatar, Esra, et al. "Synthesis and structure-activity relationship of L-methionine-coupled 1,3,4-thiadiazole derivatives with activity against influenza virus." Chemical biology & drug design vol. (2021). doi: https://doi.org/10.1111/cbdd.13995
Tatar E, Yaldız S, Kulabaş N, Vanderlinden E, Naesens L, Küçükgüzel İ. Synthesis and structure-activity relationship of L-methionine-coupled 1,3,4-thiadiazole derivatives with activity against influenza virus. Chem Biol Drug Des. 2021 Dec 06; doi: 10.1111/cbdd.13995. Epub 2021 Dec 06. PMID: 34873848.
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Chem Biol Drug Des. 2021 Dec 06; doi: 10.1111/cbdd.13995. Epub 2021 Dec 06.

Synthesis and structure-activity relationship of L-methionine-coupled 1,3,4-thiadiazole derivatives with activity against influenza virus.

Chemical biology & drug design

Esra Tatar, Seda Yaldız, Necla Kulabaş, Evelien Vanderlinden, Lieve Naesens, İlkay Küçükgüzel

Affiliations

  1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Marmara University, Haydarpa?a, 34668, ?stanbul, Turkey.
  2. KU Leuven Rega Institute, Laboratory of Virology and Chemotherapy, Herestraat 49, B-3000, Leuven, Belgium.

PMID: 34873848 DOI: 10.1111/cbdd.13995

Abstract

In previous investigations, we identified a class of 1,3,4-thiadiazole derivatives with antiviral activity. N-{3-(Methylsulfanyl)-1-[5-(phenylamino)-1,3,4-thiadiazole-2-yl]propyl}benzamide emerged as a relevant lead compound for designing novel influenza A virus inhibitors. In the present study, we elaborated on this initial lead by performing chemical synthesis and antiviral evaluation of a series of structural analogues. During this research, thirteen novel 1,3,4-thiadiazole derivatives were synthesized by the cyclization of the corresponding thiosemicarbazides as synthetic precursors. The structures and the purities of the synthesized compounds were confirmed through chromatographic and spectral data. Four L-methionine-based 1,3,4-thiadiazole derivatives displayed activity against influenza A virus, the two best compounds being 24 carrying a 5-(4-chlorophenylamino)-1,3,4-thiadiazole moiety and 30 possessing a 5-(benzoylamino)-1,3,4-thiadiazole structure [antiviral EC

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Keywords: 1,3,4-thiadiazoles; ADMET; L-methionine; antiviral activity; influenza virus; virus entry

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