Offiong O E, Martelli S
Department of Chemistry, University of Calabar, Nigeria.
Farmaco. 1995 Sep;50(9):625-32.
2-Acetylpyridine-(2-methylthiosemicarbazone), 2-acetylpyridine-(4-methylthiosemicarbazone), 2-acetylpyridine-(4-phenylthiosemicarbazone) and some of their metal complexes of the platinum group have been synthesized, characterized by chemical and spectral methods and studied for their antibacterial, antifungal and amoebicidal activity in vitro. They were studied also for their antimalarial activity and for toxicity in vivo. The platinum metal chelates exhibited significant activity against a wide spectrum of microorganisms at different concentrations. The Ru (III) chelates derived from 2-acetylpyridine-(4-methylthiosemicarbazone) seem to be the most efficient inhibitors. Evaluation of the antimalarial activity of the complexes in mice infected with Plasmodium berghei indicated that cures were attainable at dose levels of 20-160 mg/kg.
已合成了2-乙酰吡啶-(2-甲基硫代半卡巴腙)、2-乙酰吡啶-(4-甲基硫代半卡巴腙)、2-乙酰吡啶-(4-苯基硫代半卡巴腙)及其一些铂族金属配合物,通过化学和光谱方法对其进行了表征,并研究了它们在体外的抗菌、抗真菌和杀阿米巴活性。还研究了它们的抗疟活性和体内毒性。铂金属螯合物在不同浓度下对多种微生物表现出显著活性。源自2-乙酰吡啶-(4-甲基硫代半卡巴腙)的钌(III)螯合物似乎是最有效的抑制剂。对感染伯氏疟原虫的小鼠体内配合物的抗疟活性评估表明,在20-160mg/kg的剂量水平下可实现治愈。