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Guanidinyl benzothiazole derivatives: Synthesis and structure activity relationship studies of a novel series of potential antimicrobial and antioxidants

机译:胍基苯并噻唑衍生物:一系列潜在的抗菌剂和抗氧化剂的合成与结构活性关系的研究

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摘要

A series of N-phenyl-substituted and disubstituted guanidinyl benzothiazole derivatives 4a-4m were synthesized and characterized as novel antimicrobial and antioxidant agents. The in-vitro antioxidant activities of these compounds were evaluated and compared with commercial antioxidants, using ascorbic acid (AA) and employing 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay and 2,2'-azino-bis (3-ethylbenzthiazoline- 6-sulphonic acid (ABTS) assay. The results showed that IC50 values of compounds 4a and 4m were similar to the IC50 values of the standard. This assay indicates the good activities of these compounds. In addition, the in-vitro antimicrobial activities of these compounds were evaluated and the results demonstrated that the compounds 4i and 4l exhibited excellent antimicrobial activities. Compounds 4c and 4i having electron withdrawing groups at p-position and compound 4l and 4m having electron donating groups at o-position showed better antimicrobial activities compared to the standard.
机译:合成了一系列的N-苯基取代和二取代的胍基苯并噻唑衍生物4a-4m,并将其表征为新型的抗菌剂和抗氧化剂。对这些化合物的体外抗氧化活性进行了评估,并与商业抗氧化剂进行了比较,使用抗坏血酸(AA)并使用1,1-二苯基-2-吡啶并肼基(DPPH)测定和2,2'-叠氮基双(3-乙基苯并噻唑啉-6-磺酸(ABTS)测定结果表明,化合物4a和4m的IC50值与标准品的IC50值相似,此测定表明这些化合物具有良好的活性,此外,还存在体外抗菌剂对这些化合物的活性进行了评估,结果表明化合物4i和4l具有优异的抗菌活性,在p位具有吸电子基团的化合物4c和4i以及在o位具有给电子基团的化合物4l和4m具有更好的抗菌活性。与标准相比。

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