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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共23条记录   Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS A beta Reduction [作者：STAMFORD ANDREW W; SCOTT JACK D; LI SARAH W; BABU SURESH; TADESSE DAWIT; HUNTER RACHAEL; WU YUSHENG; MISIASZEK JEFFREY; CUMMING JARED N; GILBERT ERIC J; HUANG CHUNLI; MCKITTRICK BRIAN A; HONG LIWU; GUO TAO; ZHU ZHAONING; STRICKLAND COREY; ORTH PETER; VOIGT JOHANNES H; KENNEDY MATTHEW E; CHEN XIA; KUVELKAR RESHMA; HODGSON ROBERT; HYDE LYNN A; COX KATHLEEN; FAVREAU LEONARD; PARKER ERIC M; GREENLEE WILLIAM J,期刊：ACS Medicinal Chemistry Letters, 页码：897-902 , 文章类型： Article，,卷期：2012年3-11] Inhibition of BACE1 to prevent brain A beta peptide formation is a potential disease modifying approach to the treatment of Alzheimer's disease. Despite over a decade of drug discovery efforts, the identification of brai... Identification of Aminopyridazine-Derived Antineuroinflammatory Agents Effective in an Alzheimer's Mouse Model [作者：ZHOU WEI; ZHONG GUIFA; RAO XIURONG; XIE HUI; ZENG SHAOGAO; CHI TIANYAN; ZOU LIBO; WU DONGHAI; HU WENHUI,期刊：ACS Medicinal Chemistry Letters, 页码：903-907 , 文章类型： Article，,卷期：2012年3-11] Targeting neuroinflammation may be a new strategy to combat Alzheimer's disease. An aminopyridazine 1b previously reported as a novel antineuroinflammatory agent was considered to have a potential therapeutic effect for ... Initial Optimization of a New Series of gamma-Secretase Modulators Derived from a Triterpene Glycoside [作者：FULLER NATHAN O; HUBBS JED L; AUSTIN WESLEY F; CREASER STEFFEN P; MCKEE TIMOTHY D; LOUREIRO ROBYN M B; TATE BARBARA; XIA WEIMING; IVES JEFFREY L; FINDEIS MARK A; BRONK BRIAN S,期刊：ACS Medicinal Chemistry Letters, 页码：908-913 , 文章类型： Article，,卷期：2012年3-11] The discovery of a new series of gamma-secretase modulators is disclosed Starting from a triterpene glycoside gamma-secretase modulator that gave a very low brain-to-plasma ratio, initial SAR and optimization involved re... Neuroprotective Tri- and Tetracyclic BChE Inhibitors Releasing Reversible Inhibitors upon Carbamate Transfer [作者：DARRAS FOUAD H; KLING BEATA; HEILMANN JOERG; DECKER MICHAEL,期刊：ACS Medicinal Chemistry Letters, 页码：914-919 , 文章类型： Article，,卷期：2012年3-11] Tri- and tetracyclic nitrogen-bridgehead compounds were designed and synthesized to yield micromolar cholinesterase (chE), inhibitors. Structure-activity relationships identified potent compounds with butyrylcholinestera... Nonpeptidic Lysosomal Modulators Derived from Z-Phe-Ala-Diazomethylketone for Treating Protein Accumulation Diseases [作者：VISWANATHAN KISHORE; HOOVER DENNIS J; HWANG JEANNIE; WISNIEWSKI MEAGAN L; IKONNE UZOMA S; BAHR BEN A; WRIGHT DENNIS L,期刊：ACS Medicinal Chemistry Letters, 页码：920-924 , 文章类型： Article，,卷期：2012年3-11] Lysosomes are involved in protein turnover and removing misfolded species, and their enzymes have the potential to offset the defect in proteolytic clearance that contributes to the age-related dementia Alzheimer's disea... Synthesis of Lithocholic Acid Derivatives as Proteasome Regulators [作者：DANG ZHAO; JUNG KATHY; QIAN KEDUO; LEE KUOHSIUNG; HUANG LI; CHEN CHINHO,期刊：ACS Medicinal Chemistry Letters, 页码：925-930 , 文章类型： Article，,卷期：2012年3-11] Accumulation of aberrant protein aggregates, such as amyloid beta peptide (A beta), due to decreased proteasome activities, might contribute to the neurodegeneration in Alzheimer's disease. In this study, lithocholic aci... Synthesis and SAR Studies of Fused Oxadiazines as gamma-Secretase Modulators for Treatment of Alzheimer's Disease [作者：HUANG XIANHAI; ZHOU WEI; LIU XIAOXIANG; LI HONGMEI; SUN GEORGE; MANDAL MIHIRBARAN; VICAREL MONICA; ZHU XIAOHONG; BENNETT CHAD; MCCRAKEN TROY; PISSARNITSKI DMITRI; ZHAO ZHIQIANG; COLE DAVID; GALLO GIOCONDA; ZHU ZHAONING; PALANI ANANDAN; ASLANIAN ROBERT; CLADER JOHN; CZARNIECKI MICHAEL; GREENLEE WILLIAM; BURNETT DUANE; COHENWILLIAMS MARY; HYDE LYNN; SONG LIXIN; ZHANG LILI; CHU INHOU; BUEVICH ALEXEI,期刊：ACS Medicinal Chemistry Letters, 页码：931-935 , 文章类型： Article，,卷期：2012年3-11] Fused oxadiazines (3) were discovered as selective and orally bioavailable gamma-secretase modulators (GSMs) based on the structural framework of oxadiazoline GSMs. Although structurally related, initial modifications sh...