Biopolym. Cell. 2020; 36(5):371-380.
http://dx.doi.org/10.7124/bc.000A3B
Bioorganic Chemistry
4-Alkyl-1-(2-fluorobenzoyl)thiosemicarbazides and products of their de-hydrocyclization as compounds with potential anticonvulsant activity
1Czyżewska I., 1Kuśmierz E., 1Wujec M.
  1. Medical University
    4a, Chodźki Str., Lublin, Poland, 20-093

Abstract

Aim. To accomplish the synthesis of new thiosemicarbazides and their cyclic analogues derived from 2-fluorobenzoic acid hydrazide and to evaluate further their anticonvulsant activity. Methods. Organic synthesis, NMR spectroscopy, molecular docking. Results. A number of thiosemicarbazide derivatives have been synthesized by the reaction of 2-fluorobenzoic acid hydrazide with the corresponding isothiocyanates in [the] ethanol medium. The subsequent alkaline dehydrocyclization of thiosemicarbazides led to some new 1,2,4-triazole derivatives. Docking studies were performed to predict [the] anticonvulsant activity for the synthesized compounds on GABA-A receptors and pentameric ion channels of Erwinia chrysanthemi (ELIC). Conclusions. The synthesized thiosemicarbazides and their cyclic analogues [are] characterized as a prospective molecular platform for the creation of new highly active compounds as potential anticonvulsant drugs.
Keywords: thiosemicarbazides, 1,2,4-triazoles, anticonvulsant activity
Full text: (PDF, in English)

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