콘텐츠 본문
논문 해외 국제전문학술지(SCI급) SYNTHESIS OF BENZOISOXAZOLE DERIVATIVES AND EVALUATION OF INHIBITORY POTENCY AGAINST CHOLINESTERASE FOR ALZHEIMER'S DISEASE THERAPEUTICS
- 학술지 구분 국제전문학술지(SCI급)
- 게재년월 2016-09
- 저자명 박정호
- 학술지명 BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- 발행처명 KOREAN CHEMICAL SOC
- 발행국가 해외
- 논문언어 외국어
- 전체저자수 5
논문 초록 (Abstract)
To improve Alzheimer's disease (AD) therapeutics, we have designed and synthesized new benzoisoxazole derivatives that are potent inhibitors of cholinesterase (acetylcholinesterase [AChE] and butyrylcholinesterase [BuChE]). Since inhibition o f cholinesterase (ChE) is still considered to be one of the most ef fective ways of treating AD patients, many new classes of ChE inhi bitors have been synthesized. To identify a new type of cholinergic drug, the benzoisoxazole moiety which is the pharmacophore m oiety of Risperidone was coupled with natural antioxidants. Some benzoi soxazole derivatives (26-28 and 30) were found to effectively inhibit B uChE (IC50 < 20 mu M), and some (20 and 26-28) to moderately in hibitAChE (IC50 < 100 mu M). Furthermore, compound 28 showed be tter inhibitory activity against BuChE (IC50 = 0.72 +/- 0.11 mu M) than galantamine (IC50 = 8.4 +/- 0.1 mu M). The new benzoisoxazole derivati ves showing BuChE inhibitory activity represent a new class of ChE inhibitor and can be used to create novel compound derivative drug s for treating AD patients.
