- Thiophene Bioisosteres of Spirocyclic sigma Receptor Ligands: Relationships between Substitution Pattern and sigma Receptor Affinity
[作者:OBERDORF CHRISTOPH; SCHEPMANN DIRK; MIGUEL VELA JOSE; BUSCHMANN HELMUT; HOLENZ JOERG; WUENSCH BERNHARD,期刊:Journal of Medicinal Chemistry, 页码:5350-5360 , 文章类型: Article,,卷期:2012年55-11]
- On the basis of the 6',7'-dihydrospiro-[piperidine-4,4'-thieno[3,2-c]pyran] framework, a series of more than 30 sigma ligands with versatile substituents in 1-, 2'-, and 6'-position has been synthesized and pharmacologic...
- Water-Soluble Pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines as Human A(3) Adenosine Receptor Antagonists
[作者:BARALDI PIER GIOVANNI; SAPONARO GIULIA; ROMAGNOLI ROMEO; TABRIZI MOJGAN AGHAZADEH; BARALDI STEFANIA; MOORMAN ALLAN R; COSCONATI SANDRO; DI MARO SALVATORE; MARINELLI LUCIANA; GESSI STEFANIA; MERIGHI STEFANIA; VARANI KATIA; BOREA PIER ANDREA; PRETI DELIA,期刊:Journal of Medicinal Chemistry, 页码:5380-5390 , 文章类型: Article,,卷期:2012年55-11]
- A relevant problem of the pyrazolo[4,3-e]-[1,2,4]triazolo[1,5-c]pyrimidine nucleus, an attractive scaffold for the preparation of adenosine receptor antagonists, is the low water solubility. We originally functionalized ...
- Design, Synthesis, and Pharmacological Characterization of Indol-3-ylacetamides, Indol-3-yloxoacetamides, and Indol-3-ylcarboxamides: Potent and Selective CB2 Cannabinoid Receptor Inverse Agonists
[作者:PASQUINI SERENA; MUGNAINI CLAUDIA; LIGRESTI ALESSIA; TAFI ANDREA; BROGI SIMONE; FALCIANI CHIARA; PEDANI VALENTINA; PESCO NICOLO; GUIDA FRANCESCA; LUONGO LIVIO; VARANI KATIA; BOREA PIER ANDREA; MAIONE SABATINO; DI MARZO VINCENZO; CORELLI FEDERICO,期刊:Journal of Medicinal Chemistry, 页码:5391-5402 , 文章类型: Article,,卷期:2012年55-11]
- In our search for new cannabinoid receptor modulators, we describe herein the design and synthesis of three sets of indole-based ligands characterized by an acetamide, oxalylamide, or carboxamide chain, respectively. Mos...
- Antitumor Agents. 293. Nontoxic Dimethyl-4,4 '-dimethoxy-5,6,5 ',6 '-dimethylenedioxybiphenyl-2,2 '-dicarboxylate (DDB) Analogues Chennosensitlize Multidrug-Resistant Cancer Cells to Clinical Anticancer Drugs
[作者:HUNG HSINYI; OHKOSHI EMIKA; GOTO MASUO; BASTOW KENNETH F; NAKAGAWAGOTO KYOKO; LEE KUOHSIUNG,期刊:Journal of Medicinal Chemistry, 页码:5413-5424 , 文章类型: Article,,卷期:2012年55-11]
- Novel dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethylenedioxybipheny1-2,2'-dicarboxylate (DDB) analogues were designed and synthesized to improve their chemo-sensitizing action on KBvin (vincristine-resistant nasopharyngeal c...
- Discovery of a Novel Series of Potent and Orally Bioavailable Phosphoinositide 3-Kinase gamma Inhibitors
[作者:LEAHY JAMES W; BUHR CHRIS A; JOHNSON HENRY W B; KIM BYUNG GYU; BAIK TAEGON; CANNOY JONAH; FORSYTH TIMOTHY P; JEONG JOON WON; LEE MATTHEW S; MA SUNGHOON; NOSON KEVIN; WANG LONGCHENG; WILLIAMS MATTHEW; NUSS JOHN M; BROOKS ERIC; FOSTER PAUL; GOON LEANNE; HEALD NATHAN; HOLST CHARLES; JAEGER CHRISTOPHER; LAM SCOTT; LOUGHEED JULIE; LAM NGUYEN; PLONOWSKI ARTHUR; SONG JOANNE; STOUT THOMAS; WU XIANG; YAKES MICHAEL F; YU PEIWEN; ZHANG WENTAO; LAMB PETER; RAEBER OLIVIA,期刊:Journal of Medicinal Chemistry, 页码:5467-5482 , 文章类型: Article,,卷期:2012年55-11]
- The phosphoinositide 3-kinases (PI3Ks) have been linked to an extraordinarily diversified group of cellular functions making these enzymes compelling targets for the treatment of disease. A large body of evidence has lin...
- 6-(Methylamino)hexane-1,2,3,4,5-pentanol 4-(((1S,2S)-1-Hydroxy-2,3-dihydro-1H,1 ' H-[2,2-biinden]-2-yl)methyl)benzoate (PH46A): A Novel Small Molecule With Efficacy In Murine Models Of Colitis
[作者:FRANKISH NEIL; SHERIDAN HELEN,期刊:Journal of Medicinal Chemistry, 页码:5497-5505 , 文章类型: Article,,卷期:2012年55-11]
- The indane skeleton is found naturally and in several therapeutic molecules in medicinal chemistry. During our work on the anti-inflammatory activity of naturally occurring and synthetic indanes, we have synthesized a no...
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