新型 2-(三氟甲基)吩噻嗪-[1,2,3]三唑杂合体的合理设计、合成与抗结核活性评价。
Rational design, synthesis and antitubercular evaluation of novel 2-(trifluoromethyl)phenothiazine-[1,2,3]triazole hybrids.
机构信息
Organic Chemistry Division-II (CPC Division), CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.
Medicinal Chemistry and Antimycobacterial Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500078, India.
出版信息
Bioorg Med Chem Lett. 2014 Jan 1;24(1):233-6. doi: 10.1016/j.bmcl.2013.11.031. Epub 2013 Nov 21.
Molecular hybridization is an emerging structural modification tool to design molecules with better pharmacophoric properties. A series of novel 2-(trifluoromethyl)phenothiazine-1,2,3-triazoles 5a-v designed by hybridizing two antitubercular drugs trifluoperazine and I-A09 in a single molecular architecture, were synthesized in very good yields using click chemistry. Among the all '22' compounds screened for in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv (Mtb), three analogs 5c, 5l and 5o were found to be most potent (MIC: 6.25μg/mL) antitubercular agents with good selectivity index.
分子杂交是一种新兴的结构修饰工具，可用于设计具有更好药效性质的分子。通过将两种抗结核药物三氟拉嗪和 I-A09 杂交到单个分子结构中，设计了一系列新型的 2-(三氟甲基)吩噻嗪-1,2,3-三唑 5a-v，这些化合物使用点击化学以非常高的产率合成。在筛选的所有 22 种化合物中，三种类似物 5c、5l 和 5o 对结核分枝杆菌 H37Rv（Mtb）的体外抗分枝杆菌活性最强（MIC：6.25μg/mL），具有良好的选择性指数。
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