𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Synthesis and Biological Evaluation of Tacrine-Thiadiazolidinone Hybrids as Dual Acetylcholinesterase Inhibitors

✍ Scribed by Isabel Dorronsoro; Diana Alonso; Ana Castro; Maria del Monte; Esther García-Palomero; Ana Martínez

Publisher
John Wiley and Sons
Year
2005
Tongue
English
Weight
125 KB
Volume
338
Category
Article
ISSN
0365-6233

No coin nor oath required. For personal study only.

✦ Synopsis

Abstract

The synthesis of tacrine‐thiadiazolidinone hybrids is described. These compounds are designed as dual acetylcholinesterase inhibitors binding simultaneously to the peripheral and catalytic sites of the enzyme. All tested compounds exhibit significant AChE inhibitory activity. Competition assays using propidium as reference of selective ligand for the peripheral anionic site on acetylcholinesterase indicates the influence of the designed compounds over the peripheral site. They can be considered as new leads in the optimization of Alzheimer's disease modifying agents.

📜 SIMILAR VOLUMES

ChemInform Abstract: Synthesis and Biolo
ChemInform Abstract: Synthesis and Biological Evaluation of Clitocine Analogues as Adenosine Kinase Inhibitors.
✍ Chih-Hung Lee; Jerome F. Daanen; Meiqun Jiang; Haixia Yu; Kathy L. Kohlhaas; Kar 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 30 KB

## Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable v

Synthesis and Biological Evaluation of N
Synthesis and Biological Evaluation of Novel Homocamptothecins Conjugating with Dihydropyrimidine Derivatives as Potent Topoisomerase I Inhibitors
✍ Lingjian Zhu; Pengfei Cheng; Ning Lei; Jianzhong Yao; Chunquan Sheng; Chunlin Zh 📂 Article 📅 2011 🏛 John Wiley and Sons 🌐 English ⚖ 334 KB 👁 1 views

## Abstract Homocamptothecin (hCPT) is a camptothecin (CPT) homologue with the insertion of a methylene (CH~2~) spacer between the alcohol moiety and carbonyl group of the classical six‐membered α‐hydroxylactone ring. This modification provides higher lactone stability and did not impair its acti