Marc Gabriel, Stana Anca, Franchini Ana Horiana, Vodnar Dan Cristian, Barta Gabriel, Tertiş Mihaela, Şanta Iulia, Cristea Cecilia, Pîrnău Adrian, Ciorîţă Alexandra, Dume Bogdan, Toma Vlad-Alexandru, Vlase Laurian, Oniga Ilioara, Oniga Ovidiu
Department of Pharmaceutical Chemistry, "Iuliu Hațieganu" University of Medicine and Pharmacy, 41 Victor Babeș Street, RO-400012 Cluj-Napoca, Romania.
Department of Food Science and Technology, University of Agricultural Sciences and Veterinary Medicine, 3-5 Manăştur Street, RO-400372 Cluj-Napoca, Romania.
Antioxidants (Basel). 2021 Oct 27;10(11):1707. doi: 10.3390/antiox10111707.
Oxidative stress represents the underlying cause of many chronic diseases in human; therefore, the development of potent antioxidant compounds for preventing or treating such conditions is useful. Starting from the good antioxidant and antiradical properties identified for the previously reported Dihydroxy-Phenyl-Thiazol-Hydrazinium chloride (DPTH), we synthesized a congeneric series of phenolic thiazoles. The radical scavenging activity, and the antioxidant and chelation potential were assessed in vitro, a series of quantum descriptors were calculated, and the electrochemical behavior of the synthesized compounds was studied to evaluate the impact on the antioxidant and antiradical activities. In addition, their antibacterial and antifungal properties were evaluated against seven aerobic bacterial strains and a strain of , and their cytotoxicity was assessed in vitro. Compounds , and presented remarkable antioxidant and antiradical properties, and compounds , and displayed good Cu chelating activity. Compounds and were very active against ATCC 27853 compared to norfloxacin, and proved less cytotoxic than ascorbic acid against the human keratinocyte cell line (HaCaT cells, CLS-300493). Several phenolic compounds from the synthesized series presented excellent antioxidant activity and notable anti- potential.
氧化应激是人类许多慢性疾病的根本原因；因此，开发有效的抗氧化化合物用于预防或治疗此类疾病是有益的。基于先前报道的二羟基-苯基-噻唑-肼氯化物（DPTH）所具有的良好抗氧化和抗自由基特性，我们合成了一系列同类的酚噻唑。在体外评估了其自由基清除活性、抗氧化和螯合潜力，计算了一系列量子描述符，并研究了合成化合物的电化学行为以评估其对抗氧化和抗自由基活性的影响。此外，评估了它们对七种需氧细菌菌株和一种真菌菌株的抗菌和抗真菌特性，并在体外评估了它们的细胞毒性。化合物 、 和 具有显著的抗氧化和抗自由基特性，化合物 、 和 表现出良好的铜螯合活性。与诺氟沙星相比，化合物 和 对 ATCC 27853具有很强的活性，并且在人角质形成细胞系（HaCaT细胞，CLS-300493）中证明其细胞毒性比抗坏血酸小。合成系列中的几种酚类化合物具有出色的抗氧化活性和显著的抗……潜力。 （注：原文中“a strain of ”后面缺少具体内容）
