含吩噻嗪的4,5-二氢-1H-吡唑并[3,4-d]嘧啶作为抗结核药物。
4,5-Dihydro-1H-pyrazolo[3,4-d]pyrimidine containing phenothiazines as antitubercular agents.
作者信息
Siddiqui Arif B, Trivedi Amit R, Kataria Vipul B, Shah Viresh H
机构信息
Amneal Pharmaceuticals India Pvt Ltd, 882/1-871, Village Rajoda, Tal.: Bavla Dist.: Ahmedabad 382220, Gujarat, India.
Division of Medicinal Chemistry, Department of Chemistry (DST-FIST Sponsored), Mahatma Gandhi Campus, Maharaja Krishnakumarsinhji Bhavnagar University, Bhavnagar 364002, Gujarat, India.
出版信息
Bioorg Med Chem Lett. 2014 Mar 15;24(6):1493-5. doi: 10.1016/j.bmcl.2014.02.012. Epub 2014 Feb 14.
A series of novel dihydropyrazolo[3,4-d]pyrimidine derivatives bearing a phenothiazine nucleus were synthesized in excellent yields via a modified Biginelli multicomponent reaction. The newly synthesized compounds were characterized by IR, (1)H NMR, (13)C NMR, Mass spectra and elemental analysis followed by antimycobacterial screening. Among all the screened compounds, compound 4g showed most pronounced activity against Mycobacterium tuberculosis (Mtb) with minimum inhibitory concentration (MIC) of 0.02μg/mL, making it more potent than first line antitubercular drug isoniazid.
通过改良的Biginelli多组分反应，以优异的产率合成了一系列带有吩噻嗪核的新型二氢吡唑并[3,4-d]嘧啶衍生物。通过红外光谱、氢核磁共振谱、碳核磁共振谱、质谱和元素分析对新合成的化合物进行了表征，随后进行了抗分枝杆菌筛选。在所有筛选的化合物中，化合物4g对结核分枝杆菌（Mtb）表现出最显著的活性，最低抑菌浓度（MIC）为0.02μg/mL，使其比一线抗结核药物异烟肼更有效。
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