基于小分子的生物活性杂环脒衍生物的常规和微波辅助合成。
Conventional and microwave assisted synthesis of small molecule based biologically active heterocyclic amidine derivatives.
机构信息
Department of Chemistry, Indian Institute of Technology-Roorkee, Roorkee 247667 Uttaranchal, India.
出版信息
Eur J Med Chem. 2010 Mar;45(3):902-8. doi: 10.1016/j.ejmech.2009.11.030. Epub 2009 Nov 18.
Heterocyclic amidine derivatives have been synthesized by condensation of 2-cyanopyrazine, 4-cyanopyridine and 2-cyanopyridine with furfurylamine, histamine, 1-(3-aminopropyl)imidazole, 4-picolylamine, 2-picolylamine, and tryptamine respectively, in the presence of sodium methoxide as well as via microwave irradiation in good yields. All these compounds were screened for anti-inflammatory and anticancer activities. At a dose of 50mg/kg p.o. compounds 3a (36.6%), 3d (32%), 4d (31.0%) and 4e (33.8%) exhibited good anti-inflammatory activity, comparable to standard drug ibuprofen which showed 39% activity at 50mg/kg p.o.
杂环脒衍生物已经通过缩合 2-氰基吡嗪、4-氰基吡啶和 2-氰基吡啶与糠基胺、组氨酸、1-(3-氨基丙基)咪唑、4-吡啶甲胺、2-吡啶甲胺和色胺分别在甲醇钠的存在下以及通过微波辐射合成，以良好的产率得到。所有这些化合物都被筛选出具有抗炎和抗癌活性。在 50mg/kg p.o.的剂量下，化合物 3a(36.6%)、3d(32%)、4d(31.0%)和 4e(33.8%)表现出良好的抗炎活性，与标准药物布洛芬相当，布洛芬在 50mg/kg p.o.时表现出 39%的活性。
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