用作生物医药材料的缩氨基硫脲配合物的研究进展

缩氨基硫脲分子具有较高的生物活性,同时该类有机分子易与金属形成配合物,性能得到较大改善,可用作生物医药。所以以缩氨基硫脲分子为配体的配合物材料的研究是生物材料领域的一个热点。本文按照配体分子不同对缩氨基硫脲配合物材料的研究进展进行了分类综述,并对这类材料的发展趋势进行了探讨。     

Formation of first gold(III) complex of an N(4)-disubstituted thiosemicarbazone derived from 2-benzoylpyridine: structural and spectral studies

The reaction between gold(III) chloride(AuCl₃) and 2-benzoylpyridine N(4), N(4)-(butane-1,4-diyl) thiosemicarbazone (HBpypTsc) leads to an unexpected formation of a first gold(III) complex from an N(4)-disubstituted thiosemicarbazone derived from 2-benzoylpyridine. The crystal structure, spectroscopic characterization, and preliminary biological activity of [Au(III)(Cl)(BpypTsc)][Au(I)Cl₂] complex are discussed herein.     

The study of the inhibitory properties of benzoin, benzil, benzoin-(4-phenylthiosemicarbazone) and benzil-(4-phenylthiosemicarbazone) on the corrosion of mild steel in hydrochloric acid

The effects of benzoin (BN), benzil (BL), benzoin-(4-phenylthiosemicarbazone) (BN4PTSC) and benzil-(4-phenylthiosemicarbazone) (BL4PTSC) on the corrosion of mild steel in hydrochloric acid have been studied. Weight loss and hydrogen evolution measurements reveal that BN exhibit a higher maximum inhibition efficiency than BN4PTSC, BL and BL4PTSC. Generally, inhibition was found to increase with increase in inhibitor concentration and temperature. Chemical adsorption mechanism has been proposed for the inhibitors and the difference in the inhibition behaviour of the compounds has been explained in terms of the solubility of the compounds as well as the strength of the inhibitor–metal bond.     

盐酸催化芳醛缩氨基硫脲类化合物的合成反应研究

以一系列芳醛和N4-苯基氨基硫脲为原料,浓盐酸做催化剂,在室温条件下,进行反应合成了5个芳醛缩氨基硫脲类化合物,结果表明,浓盐酸催化下的反应能够在1 h内完成,并且产率在90%左右,是合成该类化合物的高效催化剂。     

Dual Parasiticidal Activities of Phthalimides: Synthesis and Biological Profile against Trypanosoma cruzi and Plasmodium falciparum

Chagas disease and malaria are two neglected tropical diseases (NTDs) that prevail in tropical and subtropical regions in 149 countries. Chagas is also present in Europe, the US and Australia due to immigration of asymptomatic infected individuals. In the absence of an effective vaccine, the control of both diseases relies on chemotherapy. However, the emergence of parasite drug resistance is rendering currently available drugs obsolete. Hence, it is crucial to develop new molecules. Phthalimides, thiosemicarbazones, and 1,3-thiazoles have been used as scaffolds to obtain antiplasmodial and anti-Trypanosoma cruzi agents. Herein we present the synthesis of 24 phthalimido-thiosemicarbazones ( 3 a – x ) and 14 phthalimido-thiazoles ( 4 a – n ) and the corresponding biological activity against T. cruzi, Plasmodium falciparum, and cytotoxicity against mammalian cell lines. Some of these compounds showed potent inhibition of T. cruzi at low cytotoxic concentrations in RAW 264.7 cells. The most active compounds, 3 t (IC₅₀=3.60 μM), 3 h (IC₅₀=3.75 μM), and 4 j (IC₅₀=4.48 μM), were more active than the control drug benznidazole (IC₅₀=14.6 μM). Overall, the phthalimido-thiosemicarbazone derivatives were more potent than phthalimido-thiazole derivatives against T. cruzi. Flow cytometry assay data showed that compound 4 j was able to induce necrosis and apoptosis in trypomastigotes. Analysis by scanning electron microscopy showed that T. cruzi trypomastigote cells treated with compounds 3 h , 3 t , and 4 j at IC₅₀ concentrations promoted changes in the shape, flagella, and surface of the parasite body similar to those observed in benznidazole-treated cells. The compounds with the highest antimalarial activity were the phthalimido-thiazoles 4 l (IC₅₀=1.2 μM), 4 m (IC₅₀=1.7 μM), and 4 n (IC₅₀=2.4 μM). Together, these data revealed that phthalimido derivatives possess a dual antiparasitic profile with potential effects against T. cruzi and lead-like characteristics.