Elumalai Karthikeyan, Ali Mohammed Ashraf, Elumalai Manogaran, Eluri Kalpana, Srinivasan Sivaneswari
New Drug Discovery Research, Department of Medicinal Chemistry, Sunrise University, Alwar, Rajasthan 301030, India.
College of Pharmacy, Sree Vidyanikethan Educational Trust, Tirupati 517102, India.
Biotechnol Rep (Amst). 2014 Oct 29;5:1-6. doi: 10.1016/j.btre.2014.10.007. eCollection 2015 Mar.
A new series of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines was prepared by reacting of -(3-oxobutanoyl)pyrazine-2-carboxamide with urea/thiourea and appropriate aldehyde in the presence of catalytic amount of laboratory made -toluenesulfonic acid as an efficient catalyst. Confirmation of the chemical structure of the synthesized compounds (4a-l) was substantiated by TLC, different spectral data IR, H NMR, mass spectra and elemental analysis. The synthesized compounds were evaluated for acetyl and butyl cholinesterase (AChE and BuChE) inhibitor activity. The titled compounds exhibited weak, moderate or high AChE and BuChE inhibitor activity. Especially, compound (4l) showed the best AChE and BuChE inhibitory activity of all the 1,2,3,4-tetrahydropyrimidine derivatives, with an IC value of 0.11 μM and 3.4 μM.
通过使-(3-氧代丁酰基)吡嗪-2-甲酰胺与尿素/硫脲以及合适的醛在催化量的自制对甲苯磺酸作为有效催化剂存在下反应，制备了一系列新型的吡嗪酰胺稠合的1,2,3,4-四氢嘧啶。通过薄层色谱法（TLC）、不同的光谱数据（红外光谱（IR）、核磁共振氢谱（H NMR）、质谱）和元素分析证实了合成化合物（4a - l）的化学结构。对合成的化合物进行了乙酰胆碱酯酶和丁酰胆碱酯酶（AChE和BuChE）抑制活性评估。标题化合物表现出弱、中等或高的AChE和BuChE抑制活性。特别是，化合物（4l）在所有1,2,3,4-四氢嘧啶衍生物中表现出最佳的AChE和BuChE抑制活性，IC值分别为0.11 μM和3.4 μM。
