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基于吡唑的吡啶并[2,3-d]嘧啶-2,4(1H,3H)-二酮的催化区域选择性合成及其生物评价。

Catalytic regioselective synthesis of pyrazole based pyrido[2,3-d]pyrimidine-diones and their biological evaluation.

机构信息

Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar-388 120, Gujarat, India.

出版信息

Org Biomol Chem. 2014 Mar 21;12(11):1751-8. doi: 10.1039/c3ob42132e.

DOI:10.1039/c3ob42132e
PMID:24496121
Abstract

A new type of biopolymer-based heterogeneous catalyst, cellulose supported acidic ionic liquid (Cell-IL), which was developed earlier in our lab, has been found to be very effective for the regioselective synthesis of pyrazole based pyrido[2,3-d]pyrimidine-diones. Its regioselectivity was confirmed by (1)H NMR spectroscopy. All the newly synthesized compounds were characterized by LC-MS, (1)H NMR, (13)C NMR, IR spectroscopy and elemental analysis. The newly synthesized compounds were evaluated for their in vitro antimalarial activity against Plasmodium falciparum, in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv strain and also for their antibacterial activity against a panel of pathogenic strains of bacteria and fungi. Some of them exhibited excellent activity when compared with first line drugs.

摘要

一种新型的基于生物聚合物的多相催化剂,即纤维素负载酸性离子液体(Cell-IL),是我们实验室之前开发的,已被发现非常有效地用于区域选择性合成基于吡唑的吡啶并[2,3-d]嘧啶-二酮。其区域选择性通过(1)H NMR 光谱得到证实。所有新合成的化合物都通过 LC-MS、(1)H NMR、(13)C NMR、IR 光谱和元素分析进行了表征。新合成的化合物进行了体外抗疟活性评价,针对恶性疟原虫,体外抗结核活性评价针对结核分枝杆菌 H37Rv 株,以及针对一组致病细菌和真菌的抗菌活性评价。与一线药物相比,其中一些化合物表现出优异的活性。

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