Literature DB >> 24900332

Discovery of a Potent Pyrazolopyridine Series of γ-Secretase Modulators.

Jun Qin1, Wei Zhou1, Xianhai Huang1, Pawan Dhondi1, Anandan Palani1, Robert Aslanian1, Zhaoning Zhu1, William Greenlee2, Mary Cohen-Williams1, Nicholas Jones1, Lynn Hyde1, Lili Zhang1.   

Abstract

The synthesis and structure-activity relationship of a novel series of pyrazolopyridines are reported. These compounds represent a new class of γ-secretase modulators that demonstrate good in vitro potency in inhibiting Aβ42 production. Examples with statistically significant in vivo efficacy in reducing the production of rat cerebrospinal fluid Aβ42 were also identified.

Entities:  

Keywords:  Alzheimer's disease; Notch; amyloid-β peptide; γ-secretase modulator

Year:  2011        PMID： 24900332      PMCID： PMC4018171          DOI： 10.1021/ml2000438

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  25 in total

Review 1.  Alzheimer's disease: the amyloid cascade hypothesis.

Authors:  J A Hardy; G A Higgins
Journal:  Science       Date:  1992-04-10       Impact factor: 47.728

2.  Inhibitors of Rho-kinase modulate amyloid-beta (Abeta) secretion but lack selectivity for Abeta42.

Authors:  Stefanie Leuchtenberger; Markus P Kummer; Thomas Kukar; Eva Czirr; Nicole Teusch; Sarah A Sagi; Rebecca Berdeaux; Claus U Pietrzik; Thomas B Ladd; Todd E Golde; Edward H Koo; Sascha Weggen
Journal:  J Neurochem       Date:  2005-11-21       Impact factor: 5.372

Review 3.  Current approaches in the treatment of Alzheimer's disease.

Authors:  Reena S Shah; Hyoung-Gon Lee; Zhu Xiongwei; George Perry; Mark A Smith; Rudy J Castellani
Journal:  Biomed Pharmacother       Date:  2008-03-17       Impact factor: 6.529

4.  What the halted phase III γ-secretase inhibitor trial may (or may not) be telling us.

Authors:  Nina F Schor
Journal:  Ann Neurol       Date:  2011-02       Impact factor: 10.422

5.  Cassette-accelerated rapid rat screen: a systematic procedure for the dosing and liquid chromatography/atmospheric pressure ionization tandem mass spectrometric analysis of new chemical entities as part of new drug discovery.

Authors:  W A Korfmacher; K A Cox; K J Ng; J Veals; Y Hsieh; S Wainhaus; L Broske; D Prelusky; A Nomeir; R E White
Journal:  Rapid Commun Mass Spectrom       Date:  2001       Impact factor: 2.419

6.  The Discovery of Pyridone and Pyridazone Heterocycles as γ-Secretase Modulators.

Authors:  Xianhai Huang; Robert Aslanian; Wei Zhou; Xiaohong Zhu; Jun Qin; William Greenlee; Zhaoning Zhu; Lili Zhang; Lynn Hyde; Inhou Chu; Mary Cohen-Williams; Anandan Palani
Journal:  ACS Med Chem Lett       Date:  2010-05-24       Impact factor: 4.345

Review 7.  The amyloid hypothesis of Alzheimer's disease: progress and problems on the road to therapeutics.

Authors:  John Hardy; Dennis J Selkoe
Journal:  Science       Date:  2002-07-19       Impact factor: 47.728

Review 8.  Advances in gamma-secretase modulation.

Authors:  Dmitri Pissarnitski
Journal:  Curr Opin Drug Discov Devel       Date:  2007-07

9.  Progress in Alzheimer's disease drug discovery: an update.

Authors:  Michael Williams
Journal:  Curr Opin Investig Drugs       Date:  2009-01

Review 10.  Recent advances in the development of gamma-secretase inhibitors.

Authors:  Hubert Josien
Journal:  Curr Opin Drug Discov Devel       Date:  2002-07
View more
  5 in total

1.  Synthesis and SAR Studies of Fused Oxadiazines as γ-Secretase Modulators for Treatment of Alzheimer's Disease.

Authors:  Xianhai Huang; Wei Zhou; Xiaoxiang Liu; Hongmei Li; George Sun; Mihirbaran Mandal; Monica Vicarel; Xiaohong Zhu; Chad Bennett; Troy McCraken; Dmitri Pissarnitski; Zhiqiang Zhao; David Cole; Gioconda Gallo; Zhaoning Zhu; Anandan Palani; Robert Aslanian; John Clader; Michael Czarniecki; William Greenlee; Duane Burnett; Mary Cohen-Williams; Lynn Hyde; Lixin Song; Lili Zhang; Inhou Chu; Alexei Buevich
Journal:  ACS Med Chem Lett       Date:  2012-09-04       Impact factor: 4.345

2.  Discovery of a Tetrahydrobenzisoxazole Series of γ-Secretase Modulators.

Authors:  Zhiqiang Zhao; Dmitri A Pissarnitski; Xianhai Huang; Anandan Palani; Zhaoning Zhu; William J Greenlee; Lynn A Hyde; Lixin Song; Giuseppe Terracina; Lili Zhang; Eric M Parker
Journal:  ACS Med Chem Lett       Date:  2017-09-19       Impact factor: 4.345

3.  γ-Secretase Modulators: Can We Combine Potency with Safety?

Authors:  Harrie J M Gijsen; Marc Mercken
Journal:  Int J Alzheimers Dis       Date:  2012-12-17

4.  Identification and Preclinical Pharmacology of the γ-Secretase Modulator BMS-869780.

Authors:  Jeremy H Toyn; Lorin A Thompson; Kimberley A Lentz; Jere E Meredith; Catherine R Burton; Sethu Sankaranararyanan; Valerie Guss; Tracey Hall; Lawrence G Iben; Carol M Krause; Rudy Krause; Xu-Alan Lin; Maria Pierdomenico; Craig Polson; Alan S Robertson; R Rex Denton; James E Grace; John Morrison; Joseph Raybon; Xiaoliang Zhuo; Kimberly Snow; Ramesh Padmanabha; Michele Agler; Kim Esposito; David Harden; Margaret Prack; Sam Varma; Victoria Wong; Yingjie Zhu; Tatyana Zvyaga; Samuel Gerritz; Lawrence R Marcin; Mendi A Higgins; Jianliang Shi; Cong Wei; Joseph L Cantone; Dieter M Drexler; John E Macor; Richard E Olson; Michael K Ahlijanian; Charles F Albright
Journal:  Int J Alzheimers Dis       Date:  2014-07-08

5.  Discovery of New Pyrazolopyridine, Furopyridine, and Pyridine Derivatives as CDK2 Inhibitors: Design, Synthesis, Docking Studies, and Anti-Proliferative Activity.

Authors:  Adel A-H Abdel-Rahman; Amira K F Shaban; Ibrahim F Nassar; Dina S El-Kady; Nasser S M Ismail; Samy F Mahmoud; Hanem M Awad; Wael A El-Sayed
Journal:  Molecules       Date:  2021-06-26       Impact factor: 4.411
  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.