Desai Nisheeth C, Trivedi Amit R, Somani Hardik C, Bhatt Kandarp A
Division of Medicinal Chemistry, Department of Chemistry, (UGC NON-SAP & DST-FIST Sponsored), Maharaja Krishnakumarsinhji Bhavnagar University, Mahatma Gandhi Campus, Bhavnagar, Gujarat, 364 002, India.
Chem Biol Drug Des. 2015 Sep;86(3):370-7. doi: 10.1111/cbdd.12502. Epub 2015 Jan 9.
A series of novel 1,4-dihydropyridine-3,5-dicarbamoyl derivatives bearing an imidazole nucleus at C-4 position were synthesized in excellent yields via multicomponent Hantzsch reaction. The newly synthesized compounds were characterized by IR, (1) H NMR, (13) C NMR, and mass spectroscopy. The synthesized compounds 3a-p were screened for antitubercular activity. Among all the screened compounds, compounds 3j and 3m showed most prominent activity against Mycobacterium tuberculosis with minimum inhibitory concentration of 0.02 μg/mL and SI > 500, making it more potent than first-line antitubercular drug isoniazid. In addition, these compounds displayed relatively low cytotoxicity.
通过多组分汉茨希反应，以优异的产率合成了一系列在C-4位带有咪唑核的新型1,4-二氢吡啶-3,5-二氨基甲酰基衍生物。通过红外光谱、¹H核磁共振、¹³C核磁共振和质谱对新合成的化合物进行了表征。对合成的化合物3a-p进行了抗结核活性筛选。在所有筛选的化合物中，化合物3j和3m对结核分枝杆菌表现出最显著的活性，最低抑菌浓度为0.02μg/mL，选择性指数>500，使其比一线抗结核药物异烟肼更有效。此外，这些化合物表现出相对较低的细胞毒性。
