Synthesis, characterization and pharmacokinetic studies of 4-(3-aryl-1, 6-dihydro-6-iminopyridazin-1-yl)butanoic acid hydrochlorides

Din Islam, Samiron Kumar, T. A. Chowdhury, Mahe Zame Sarker, H. Nishino, Aminul Haque, M. M. Rahman
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引用次数: 1

Abstract

A series of six title compounds have been prepared using 3-amino- 6-chloropyridazine as starting material collected from commercial sources and were characterized by IR, 1H NMR, and high-resolution mass spectral (HRMS) data. The method involves three steps: Suzuki-Miyaura cross-coupling reaction, N(2)-alkylation, and acid hydrolysis, respectively, to obtain final products with good yields. According to Lipinski's rule of five and Veber's rule, pharmacokinetics studies of the synthesized compounds showed that all the parameters were in between the permissible limits. The toxicity parameters were low for the compounds to act as drugs. J. Bangladesh Acad. Sci. 45(1); 37-47: June 2021
4-(3-芳基- 1,6 -二氢-6-亚氨基吡啶嗪-1-基)丁酸盐酸的合成、表征及药代动力学研究
以3-氨基- 6-氯吡嗪为原料,制备了一系列6个标题化合物,并用IR、1H NMR和高分辨率质谱(HRMS)对其进行了表征。该方法分为Suzuki-Miyaura交叉偶联反应、N(2)-烷基化反应和酸水解三步,得到收率较高的终产物。根据利平斯基五定律和韦伯定律,合成化合物的药代动力学研究表明,所有参数都在允许范围内。这些化合物的毒性参数较低,可作为药物使用。[j] .科学通报,2004 (1);37-47: 2021年6月
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