Citation: Ming Sheng Feng, Ping Guo, Li Xun Jiang, Jing Bo Shi, Yu Ping Cao, Qi Zheng Yao. Synthesis of novel methotrexate derivatives with inhibition activity of nitric oxide synthase[J]. Chinese Chemical Letters, ;2009, 20(2): 178-180. doi: 10.1016/j.cclet.2008.10.027 shu

Synthesis of novel methotrexate derivatives with inhibition activity of nitric oxide synthase

a Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China;
b Nanjing Hicin Pharmaceutical Co., Ltd., Nanjing 210046, China

Received Date: 28 August 2008

Fund Project: We are grateful to the National Natural Science Foundation of China (No. 39870882).

Seventeen 4-alkylamino/arylamino-substituted methotrexate (MTX) derivatives 6a-14a were designed and synthesized. Their inhibition activities against inducible nitric oxide synthase (iNOS) were evaluated in vitro. The pharmacological results showed that most of the prepared compounds displayed the potent inhibitory effects on iNOS.
- Tetrahydrobiopterin,
- Inhibitor of nitric oxide synthase,
- Synthesis,
- Methotrexate
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