- Discovery and Characterization of an Inhibitor of Glucosylceramide Synthase
[作者:RICHARDS STEVEN; LARSON CHRISTOPHER J; KOLTUN ELENA S; HANEL ART; CHAN VICKY; NACHTIGALL JASON; HARRISON AMANDA; AAY NAING; DU HONGWANG; ARCALAS ARLYN; GALAN ADAM; ZHANG JEFF; ZHANG WENTAO; WON KWANGAI; TAM DANNY; QIAN FAWN; WANG TAO; FINN PATRICIA; OGILVIE KATHY; ROSEN JON; AOYAMA RON; PLONOWSKI ARTUR; CANCILLA BELINDA; BENTZIEN FRAUKE; YAKES MICHAEL; MOHAN RAJU; LAMB PETER; NUSS JOHN; KEARNEY PATRICK,期刊:Journal of Medicinal Chemistry, 页码:4322-4335 , 文章类型: Article,,卷期:2012年55-9]
- Targeting glycosphingolipid synthesis has emerged as a novel approach for treating metabolic diseases. 32 (EXEL-0346) represents a new class of glucosylceramide synthase (GCS) inhibitors. This report details the elaborat...
- Novel 1,2,4-Triazolo[1,5-a]pyridines and Their Fused Ring Systems Attenuate Oxidative Stress and Prolong Lifespan of Caenorhabiditis elegans
[作者:MEKHEIMER RAMADAN AHMED; SAYED AHMED AMIR RADWAN; AHMED ELTAIB ALI,期刊:Journal of Medicinal Chemistry, 页码:4169-4177 , 文章类型: Article,,卷期:2012年55-9]
- In this paper we report the synthesis of some novel 1,2,4-triazolo [1,5-a]pyridine and azolotriazolopyridine ring systems. The products were screened for various types of activity like antibacterial, antifungal, and anti...
- Synthesis, Structure-Activity Relationship, and Pharmacological Studies of Novel Melanin-Concentrating Hormone Receptor 1 Antagonists 3-Aminomethylquinolines: Reducing Human Ether-a-go-go-Related Gene (hERG) Associated Liabilities
[作者:KASAI SHIZUO; KAMATA MAKOTO; MASADA SHINICHI; KUNITOMO JUN; KAMAURA MASAHIRO; OKAWA TOMOHIRO; TAKAMI KAZUAKI; OGINO HITOMI; NAKANO YOSHIHIDE; ASHINA SHUNTAROU; WATANABE KAORU; KAISHO TOMOKO; IMAI YUMI N; RYU SUNGHI; NAKAYAMA MASAHARU; NAGISA YASUTAKA; TAKEKAWA SHIRO; KATO KOKI; MURATA TOSHIKI; SUZUKI NOBUHIRO; ISHIHARA YUJI,期刊:Journal of Medicinal Chemistry, 页码:4336-4351 , 文章类型: Article,,卷期:2012年55-9]
- Recently, we discovered 3-aminomethylquinoline derivative 1, a selective, highly potent, centrally acting, and orally bioavailable human MCH receptor 1 (hMCHR1) antagonist, that inhibited food intake in F344 rats with di...
- Discovery of a Potent and Selective GPR120 Agonist
[作者:SHIMPUKADE BHARAT; HUDSON BRIAN D; HOVGAARD CHRISTINE KIEL; MILLIGAN GRAEME; ULVEN TROND,期刊:Journal of Medicinal Chemistry, 页码:4511-4515 , 文章类型: Article,,卷期:2012年55-9]
- GPR120 is a receptor of unsaturated long-chain fatty acids reported to mediate GLP-1 secretion, insulin sensitization, anti-inflammatory, and anti-obesity effects and is therefore emerging as a new potential target for t...
- Fluorocyclopentenyl-cytosine with Broad Spectrum and Potent Antitumor Activity
[作者:CHOI WON JUN; CHUNG HWAJIN; CHANDRA GIRISH; ALEXANDER VARUGHESE; ZHAO LONG XUAN; LEE HYUK WOO; NAYAK AKSHATA; MAJIK MAHESH S; KIM HEA OK; KIM JINHEE; LEE YOUNG B; AHN CHANG H; LEE SANG KOOK; JEONG LAK SHIN,期刊:Journal of Medicinal Chemistry, 页码:4521-4525 , 文章类型: Article,,卷期:2012年55-9]
- On the basis of the potent biological activity of cyclopentenyl-pyrimidines, fluorocyclopentenyl-pyrimidines were designed and synthesized from D-ribose. Among these, the cytosine derivative 5a showed highly potent antig...
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