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Synthesis of quinazoline derivatives with acetycholinesterase and butyrylcholinesterase inhibitory activities |
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| รหัสดีโอไอ | |
| Title | Synthesis of quinazoline derivatives with acetycholinesterase and butyrylcholinesterase inhibitory activities |
| Creator | Yuparaid Uetrongchit |
| Contributor | Pattara Sawasdee, Sumrit Wacharasindhu |
| Publisher | Chulalongkorn University |
| Publication Year | 2553 |
| Keyword | Quinazoline, Enzyme inhibitors, สารยับยั้งเอนไซม์, ควินาโซลีน |
| Abstract | Quinazolines were the attractive and useful compounds in medicinal chemistry due to their pharmacology activities such as antibacterial, anticancer, antitumor, antidiabetic, anti-inflammatory, analgesic and antiviral activities. In this study, the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of quinazolines derivatives were evaluated. The 4-substitued aminoquinazolines via amination reaction were first synthesized and found that 4-piperidinoquinazolines (12e) possess the highest activity with the IC₅₀ values toward AChE and BChE of 1.3 µM and 7.5 µM, respectively. Then 4-butylaminoquinazolin (12a), 4-piperidinoquinazolines (12e) and 4-morpholinoquinazoline were chosen for further modified their structures by the electron-withdrawing and electron-releasing groups. From the results, there is no activity trend from these groups as substituents on a benzene ring of the core structures of 12a, 12e and 12f. These might be the cause of the different mode of action in each compound. However, this study 4-piperidinoquinazolines (12e) was a candidate for both AChE and BChE inhibitors. 6-Nitro-4-butylaminoquinazoline (16a) was a potent and selective inhibitor toward AChE over BChE while 6,7-dimethoxy-4-butylaminoquinazoline (16d) was a potent and selective inhibitor toward BChE over AChE. |
| URL Website | cuir.car.chula.ac.th |
