Pontiki E, Hadjipavlou-Litina D, Chaviara A T
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki, Greece.
J Enzyme Inhib Med Chem. 2008 Dec;23(6):1011-7. doi: 10.1080/14756360701841251.
Highly reactive radicals are implicated in many pathological conditions. The quest for radical scavengers or antioxidants, spans the previous decades. A new series of complexes of the type [Cu (dien) (2a-2tzn) Y(2)] and [Cu (dienXXY(2)) (2a-5mt)] and of the type [Cu (dptaS) Cl(2)] and [Cu (dptaS) Br(2)] (dptaS = 1, 3-propanediamine) or Schiff mono-base of dipropylenetriamine with 2-thiophene-carboxaldehyde, has been tested for anti-inflammatory and antioxidant activity. The tested compounds inhibit the carrageenin-induced rat paw edema (52.0-82.6%) and present important scavenging activity. Compound 6 is the most potent (82.6%) in the in vivo experiment. Lipophilicity-as R(M) values - has been determined. The results support that in general, adducts of the type [Cu (dienXXY(2)) (2a-5mt)] exhibit increased activity compared to the starting material of type [Cu (dienXXY(2))]. An attempt to correlate the biological results with their structural characteristics and physicochemical parameters has been made.
高反应性自由基与许多病理状况有关。在过去几十年里,人们一直在寻找自由基清除剂或抗氧化剂。已经测试了一系列新型配合物,如[Cu (dien) (2a - 2tzn) Y(2)]、[Cu (dienXXY(2)) (2a - 5mt)]以及[Cu (dptaS) Cl(2)]和[Cu (dptaS) Br(2)](dptaS = 1, 3 - 丙二胺),还有二亚丙基三胺与2 - 噻吩甲醛形成的席夫单碱,以检测它们的抗炎和抗氧化活性。所测试的化合物能抑制角叉菜胶诱导的大鼠足爪肿胀(抑制率为52.0 - 82.6%),并具有重要的清除活性。化合物6在体内实验中活性最强(抑制率为82.6%)。已测定了亲脂性——以R(M)值表示。结果表明,一般来说,[Cu (dienXXY(2)) (2a - 5mt)]类型的加合物相比[Cu (dienXXY(2))]类型的起始原料表现出更高的活性。已尝试将生物学结果与其结构特征和物理化学参数相关联。