Synthesis, antimicrobial and antioxidant activities of pyridyl substituted thiazolyl triazole derivatives

Abstract In this present study, 63 different 5-[4-methyl-2-(pyridin-3/4-yl)thiazole-5-yl]-4-substituted-3-substituted benzylthio-4H-1,2,4-triazole derivatives were synthesized, and evaluated for their in vitro antimicrobial activity against various human pathogenic microorganisms and antioxidant activity. The derivatives were synthesized in a multi-step synthesis procedure including triazole and thiazole ring closure reactions, respectively. The synthesized derivatives (A1-24; B1-39) were screened for their antibacterial, antifungal, and antioxidant activities compared to standard agents. The derivatives possessing 3-pyridyl moiety particularly exhibited relatively high antibacterial activity (MIC= < 3.09-500 µg/mL) against Gram-positive bacteria, and compounds possessing 4-pyridyl moiety showed remarkable antioxidant activity.

摘要 本研究共合成63种不同的5-[4-甲基-2-(吡啶-3/4-基)噻唑-5-基]-4-取代-3-取代苄硫基-4H-1,2,4-三唑（4H-1,2,4-triazole）衍生物，并对其针对多种人类致病微生物的体外抗菌活性与抗氧化活性开展了评价。该类衍生物通过多步合成工艺制备，合成过程依次涉及三唑环与噻唑环的关环反应。本研究以标准药物为参照，对合成得到的衍生物（A1-24；B1-39）的抗菌、抗真菌及抗氧化活性进行了筛选。结果显示，带有3-吡啶基（3-pyridyl）基团的衍生物对革兰氏阳性菌（Gram-positive bacteria）展现出相对较高的抗菌活性，最低抑菌浓度（Minimum Inhibitory Concentration，MIC）为<3.09~500 μg/mL；而带有4-吡啶基的化合物则表现出显著的抗氧化活性。