PMID- 20345341
OWN - NLM
STAT- MEDLINE
DCOM- 20100908
LR  - 20190823
IS  - 1875-533X (Electronic)
IS  - 0929-8673 (Linking)
VI  - 17
IP  - 17
DP  - 2010
TI  - Tacrine derivatives and Alzheimer's disease.
PG  - 1825-38
AB  - To date, the pharmacotherapy of Alzheimer's disease (AD) has relied on 
      acetylcholinesterase (AChE) inhibitors (AChEIs) and, more recently, an 
      N-methyl-D-aspartate receptor (NMDAR) antagonist. AD is a multifactorial syndrome 
      with several target proteins contributing to its etiology. "Multi-target-directed 
      ligands" (MTDLs) have great potential for treating complex diseases such as AD 
      because they can interact with multiple targets. The design of compounds that can 
      hit more than one specific AD target thus represents an innovative strategy for 
      AD treatment. Tacrine was the first AChEI introduced in therapy. Recent studies 
      have demonstrated its ability to interact with different AD targets. Furthermore, 
      numerous tacrine homo- and heterodimers have been developed with the aim of 
      improving and enlarging its biological profile beyond its ability to act as an 
      AChEI. Several tacrine hybrid derivatives have been designed and synthesized with 
      the same goal. This review will focus on and summarize the last two years of 
      research into the development of tacrine derivatives able to hit AD targets 
      beyond simple AChE inhibition.
FAU - Tumiatti, V
AU  - Tumiatti V
AD  - Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of 
      Bologna, Via Belmeloro 6, 40126 Bologna, Italy. vincenzo.tumiatti@unibo.it
FAU - Minarini, A
AU  - Minarini A
FAU - Bolognesi, M L
AU  - Bolognesi ML
FAU - Milelli, A
AU  - Milelli A
FAU - Rosini, M
AU  - Rosini M
FAU - Melchiorre, C
AU  - Melchiorre C
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
PL  - United Arab Emirates
TA  - Curr Med Chem
JT  - Current medicinal chemistry
JID - 9440157
RN  - 0 (Amyloid beta-Peptides)
RN  - 0 (Cholinesterase Inhibitors)
RN  - 4VX7YNB537 (Tacrine)
RN  - EC 3.1.1.7 (Acetylcholinesterase)
SB  - IM
MH  - Acetylcholinesterase/*metabolism
MH  - Alzheimer Disease/*drug therapy/metabolism
MH  - Amyloid beta-Peptides/metabolism
MH  - Cholinesterase Inhibitors/*pharmacology/therapeutic use
MH  - Humans
MH  - Models, Molecular
MH  - Structure-Activity Relationship
MH  - Tacrine/*analogs & derivatives/pharmacology/therapeutic use
RF  - 143
EDAT- 2010/03/30 06:00
MHDA- 2010/09/09 06:00
CRDT- 2010/03/30 06:00
PHST- 2009/12/15 00:00 [received]
PHST- 2010/03/19 00:00 [accepted]
PHST- 2010/03/30 06:00 [entrez]
PHST- 2010/03/30 06:00 [pubmed]
PHST- 2010/09/09 06:00 [medline]
AID - BSP/CMC/E-Pub/ 109 [pii]
AID - 10.2174/092986710791111206 [doi]
PST - ppublish
SO  - Curr Med Chem. 2010;17(17):1825-38. doi: 10.2174/092986710791111206.