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.jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117 Bioorg+Med+Chem+Lett
2016 ; 26
(22
): 5573-5579
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Synthesis and biological evaluation of ranitidine analogs as
multiple-target-directed cognitive enhancers for the treatment of Alzheimer s
disease
#MMPMID27769620
Gao J
; Midde N
; Zhu J
; Terry AV
; McInnes C
; Chapman JM
Bioorg Med Chem Lett
2016[Nov]; 26
(22
): 5573-5579
PMID27769620
show ga
Using molecular modeling and rationally designed structural modifications, the
multi-target structure-activity relationship for a series of ranitidine analogs
has been investigated. Incorporation of a variety of isosteric groups indicated
that appropriate aromatic moieties provide optimal interactions with the
hydrophobic and ?-? interactions with the peripheral anionic site of the AChE
active site. The SAR of a series of cyclic imides demonstrated that AChE
inhibition is increased by additional aromatic rings, where 1,8-naphthalimide
derivatives were the most potent analogs and other key determinants were
revealed. In addition to improving AChE activity and chemical stability,
structural modifications allowed determination of binding affinities and
selectivities for M1-M4 receptors and butyrylcholinesterase (BuChE). These
results as a whole indicate that the 4-nitropyridazine moiety of the JWS-USC-75IX
parent ranitidine compound (JWS) can be replaced with other chemotypes while
retaining effective AChE inhibition. These studies allowed investigation into
multitargeted binding to key receptors and warrant further investigation into
1,8-naphthalimide ranitidine derivatives for the treatment of Alzheimer's
disease.
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