Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Synthesis, Antimicrobial and Pharmacological Evaluation of Thioureaderivatives of 4H-1,2,4-triazole

Author(s): Anna Bielenica, Ewa Kedzierska, Sylwia Fidecka, Hanna Maluszynska, Barbara Miroslaw, Anna E. Koziol, Joanna Stefanska, Silvia Madeddu, Gabriele Giliberti, Giuseppina Sanna, Marta Struga.

Graphical Abstract:


Abstract:

A group of 4H-1,2,4-triazole-derived thioureas was efficiently prepared and evaluated for antibacterial, antifungal and antiviral activities.The chemical identity of all derivatives was established on the basis of spectral methods. The molecular structures of 10 and 21 were determined by an X-ray crystallography. Compounds with phenyl (1), 3,4-dichlorophenyl (2) and p-methoxyphenyl (3) substituents were the most promising against fungi species. The derivative 12 has proved to be significantly active against CVB-5. The CNS-activity of five new 4H-1,2,4-triazolo-thiourea derivatives 2, 10, 12, 18 and 21 was investigated. The results proved that activity of all tested thiourea compounds may be connected with the serotonergic system. Derivatives 2, 10, 12, 18 acted as inhibitors of the head twitch responses (HTR).The biological activity of 21 was also linked with the endogenous opioid system. The derivative 18 diminished the spontaneous mobility and 10 reduced the amphetamineinduced activity of laboratory animals.

Keywords: Antifungal activity, antiviral activity, CNS activity, thiourea, 1, 2, 4-triazole, X-ray crystallography.

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Article Details

VOLUME: 12
ISSUE: 4
Year: 2015
Page: [263 - 276]
Pages: 14
DOI: 10.2174/1570180811666141001010044
Price: $58