Antiradical and Antimicrobial Activity of Thiosemicarbaside and 1,2,4-Triazole Derivatives of Hydroxybenzoic Acid
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radical and Antimicrobial Activity of Thiosemicarbaside and 1,2,4-Triazole Derivatives of Hydroxybenzoic Acid Zh. B. Satpaevaa, b, 1, Z. T. Shulgauc, S. B. Akhmetovad, O. A. Nurkenovb, S. D. Fazylova, b, and M. Zh. Burkeeva aBuketov
State University, Karaganda, 100028 Kazakhstan Institute of Organic Synthesis and Coal Chemistry, Karaganda, 100008 Kazakhstan c RSE National Center for Biotechnology, Ministry of Education and Science, Nur-Sultan, 010000 Kazakhstan d Karaganda State Medical University, Karaganda, 100000 Kazakhstan b
Received February 10, 2020; revised February 20, 2020; accepted February 22, 2020
Abstract—The antimicrobial and antioxidant activity of synthesized biologically active compounds have been evaluated in comparison with the standard antioxidant, ascorbic acid. The antioxidant activity of the compounds has been studied by their ability to interact with the 2,2-diphenyl-1-picrylhydrazyl radical (DPPH ). The proposed test system has revealed the pronounced antiradical activity of 2-(2-hydroxybenzoyl)-Nphenylhydrazinecarbothioamide (1) (IC50(DPPH) = 15.5 μM) and 2-(4-hydroxybenzoyl)N-phenylhydrazinecarbothiamide (2) (IC50(DPPH) = 31.7 μM). A weak antibacterial activity of these compounds has been shown against gram-positive and gram-negative test strains. Keywords: antioxidant, antiradical, antimicrobial activity, strain, free radical, thiosemicarbazide, 1,2,4-triazole, DPPH DOI: 10.1134/S1068162020040172
INTRODUCTION Salicylic acid derivatives (salicylates) entered clinical practice at the end of the 19th century and are widely used to date. Salicylates, such as acetylsalicylic acid (aspirin), sodium salicylate, salicylanilide, salicylamide (SAM), methyl salicylate are used in medicine as analgesic, antipyretic, antiplatelet, antioxidant, antiproliferative, and cytotoxic agents [1–3]. These compounds also showed antitumor activity [4– 6]. According to recent data, the salicylic acid derivatives can be considered as bioregulators, which are synthesized in the body and perform protective functions. These properties of salicylates allow for rethinking their role in the pathophysiology of humans and animals. The presence of the OH and COOH groups in the neighboring positions of the benzene ring provides great opportunities for chemical transformations of salicylic acid. Salicylic acid is a natural phenolic hormone, which plays an important role in protecting plants from various types of fungi and pathogens. According to the literature data on various derivatives of salicylic acid [7, 8], the following relationships in their structure–biological activity can be noted. (a) All substitutions in the acidic groups (sites I and II) provided the preservation of antipyretic, analgesic, 1 Corresponding author: e-mail: [email protected].
and anti-inflammatory properties and the appearance of new types of activity (R' = OCH3, OC3H7-i, NH2, NHCH2CH2, COOR, etc. [9–11]. (b) Substitutions in the phenyl ring (site III) led to the appearance of antituberculosis, fungicidal, antifungal, antidepressant, and oth
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