噻二唑类抗利什曼原虫药物的合成与评价

IF 0.7 Q4 PHARMACOLOGY & PHARMACY Journal of Reports in Pharmaceutical Sciences Pub Date : 2020-07-01 DOI:10.4103/jrptps.JRPTPS_3_20
F. Hassanzadeh, E. Jafari, M. Saeedi, S. Saberi
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引用次数: 1

摘要

背景和目的:1,3,4-噻二唑支架是多种药物类别中的主要结构成分之一,如抗菌剂、抗炎剂、抗肿瘤剂和抗利什曼原虫剂。考虑到噻二唑衍生物的抗利什曼病作用和该疾病的重要性,合成了一些在硫原子或连接在2-位的胺基上进行修饰的噻二唑化合物,并对其抗利什曼活性进行了评估。材料和方法:合成了1,3,4-噻二唑衍生物,包括含2-取代硫代-1,3,4噻二唑的(5-(4-硝基亚苄基氨基)或5-氨基(II,IV,V)和一种含2-取代氨基-1,4噻二唑的衍生物(5-(-4-硝基苯基)(VII),并评价了它们对利什曼原虫前鞭毛体和无鞭毛体形式的体外抗利什曼病活性专业结果:在对前鞭毛体和无鞭毛体孵育24小时后,发现最具活性的化合物是化合物II,半数最大抑制浓度(IC50)值分别为44.4µM和64.7µM。结论:所有合成的化合物在培养48和72小时后对两种主要利什曼原虫都表现出良好的抗利什曼病活性。
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Synthesis and evaluation of thiadiazole-based antileishmanial agents
Background and Objectives: The 1, 3, 4-thiadiazole scaffold is one of the principal structural components, in a variety of drug categories such as antimicrobial, anti-inflammatory, antineoplastic, and antileishmanial agents. Considering the reported antileishmanial effects of thiadiazole derivatives and the importance of this disease, some of the thiadiazole derivatives with modifications at sulfur atom or amine group attached to the 2-position were synthesized and evaluated for antileishmanial activity. Materials and Methods: Derivatives of 1,3,4-thiadiazole including 2-substituted-thio-1,3,4-thiadiazoles bearing (5-(4-nitrobenzylideneamino) or 5-amino (II, IV, V) and one derivative of 2-substituted-amino-1,3,4-thiadiazole bearing (5- (4-nitrophenyl) (VII) were synthesized and evaluated for their in vitro antileishmanial activity against promastigote and amastigote forms of the Leishmania major. Results: The most active compound was found to be compound II after 24-h incubation against promastigotes and amastigotes with the half maximal inhibitory concentration (IC50) values of 44.4 µM and 64.7 µM, respectively. Conclusion: All of the synthesized compounds showed good antileishmanial activity against both forms of L. major after 48 and 72h incubation.
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来源期刊
Journal of Reports in Pharmaceutical Sciences
Journal of Reports in Pharmaceutical Sciences Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
1.40
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期刊介绍: The Journal of Reports in Pharmaceutical Sciences(JRPS) is a biannually peer-reviewed multi-disciplinary pharmaceutical publication to serve as a means for scientific information exchange in the international pharmaceutical forum. It accepts novel findings that contribute to advancement of scientific knowledge in pharmaceutical fields that not published or under consideration for publication anywhere else for publication in JRPS as original research article. all aspects of pharmaceutical sciences consist of medicinal chemistry, molecular modeling, drug design, pharmaceutics, biopharmacy, pharmaceutical nanotechnology, pharmacognosy, natural products, pharmaceutical biotechnology, pharmacology, toxicology and clinical pharmacy.
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