中国神经再生研究(英文版) ›› 2017, Vol. 12 ›› Issue (8): 1256-1261.doi: 10.4103/1673-5374.213541

• 综述:退行性病与再生 • 上一篇    下一篇

阿尔茨海默病治疗中新旧靶点相互作用的关键结构:杂环化合物

  

  • 收稿日期:2017-07-14 出版日期:2017-08-15 发布日期:2017-08-15
  • 基金资助:

    本研究得到了2007-2013年发展与凝聚力基金-APQ Apulia区域研究“支持智能专业化和社会与环境可持续性-未来研究的区域计划”、伊拉斯姆斯·纳马斯特联盟的共同资助与支持(I2PCTF6)(NAMASTE_20140147)。

Heterocyclic compounds as key structures for the interaction with old and new targets in Alzheimer’s disease therapy

Asha Hiremathad1, Luca Piemontese2   

  1. 1 Centre for Nano and Material Sciences, Jain University, Jain Global Campus, Kanakapura, Ramanagaram, Bangalore, India; 2 Dipartimento di Farmacia–Scienze del Farmaco, Università degli Studi di Bari “Aldo Moro”, Bari, Italy
  • Received:2017-07-14 Online:2017-08-15 Published:2017-08-15
  • Contact: Luca Piemontese, Ph.D.,luca.piemontese@uniba.it.
  • Supported by:

    This study was supported by Intervento cofinanziato dal Fondo di Sviluppo e Coesione 2007-2013 –APQ Ricerca Regione Puglia “Programma regionale a sostegno della specializzazione intelligente e della sostenibilità sociale ed ambientale - Future In Research”. Project ID: I2PCTF6 (to LP). Erasmus NAMASTE consortium (unique grant number: NAMASTE_20140147) (to AH).

摘要:

 

 
本研究得到了2007-2013年发展与凝聚力基金-APQ Apulia区域研究“支持智能专业化和社会与环境可持续性-未来研究的区域计划”、伊拉斯姆斯·纳马斯特联盟的共同资助与支持(I2PCTF6)(NAMASTE_20140147)。
 
随着人口的老龄化进程的不断加剧,阿尔茨海默病(AD)正成为日益突出的社会问题。事实上,只有5种药物被FDA批准用于治疗这种神经退行性疾病,但效果均不理想。其中,Rivastigmine、多奈哌齐、加兰他敏是乙酰胆碱酯酶抑制剂,美金刚是NMDA受体拮抗剂,而第5种制剂是多奈哌齐与美金刚的组合。
 

AD的预防和治疗是制药行业的新挑战,也是公共机构、医生、患者及其家属所面临的新挑战:迫切需要找到治疗神经退行性疾病的新方法。鉴于该病的病理学多重起源,本研究强烈推荐多靶点干预策略。文中讨论了一种新化学结构--杂环化合物增强AD靶向治疗的效果。

orcid:0000-0002-7980-5818(Luca Piemontese)
0000-0001-7170-2614(Asha Hiremathad)

Abstract:

Nowadays, Alzheimer’s disease (AD) is widely recognized as a real social problem. In fact, only five drugs are FDA approved for the therapy of this widespread neurodegenerative disease, but with low results so far. Three of them (rivastigmine, donepezil and galantamine) are acetylcholinesterase inhibitors, memantine is a N-methyl-D-aspartate receptor antagonist, whereas the fifth formulation is a combination of donepezil with memantine. The prevention and treatment of AD is the new challenge for pharmaceutical industry, as well as for public institutions, physicians, patients, and their families. The discovery of a new and safe way to cure this neurodegenerative disease is urgent and should not be delayed further. Because of the multiple origin of this pathology, a multi-target strategy is currently strongly pursued by researchers. In this review, we have discussed new structures designed to better the activity on the classical AD targets. We have also examined old and new potential drugs that could prove useful future for the therapy of the pathology by acting on innovative, not usual, and not yet fully explored targets like peroxisome proliferator-activated receptor (PPARs).

Key words: Alzheimer’s disease, multi-target strategy, peroxisome proliferator-activated receptors, heterocyclic
compounds,
neurodegenerative diseases