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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26条记录   Design, synthesis and inhibition activity of a novel cyclic enediyne amino acid conjugates against MPtpA [作者：CHANDRA KOUSHIK; DUTTA DEBAJYOTI; MITRA ANALAVA; DAS AMIT K; BASAK AMIT,期刊：Bioorganic & Medicinal Chemistry, 页码：3274-3279 , 文章类型： Article，,卷期：2011年19-10] In course of studies towards the discovery of selective inhibitors of MPtpA, a novel cyclic endiyne malonamic acid has been designed and synthesized. The synthesis involves a crucial intramolecular Knoevenagel reaction. ... Inhibitory potential of chemical substitutions at bioinspired sites of beta-D-galactopyranose on neoglycoprotein/cell surface binding of two classes of medically relevant lectins [作者：GIGUERE DENIS; ANDRE SABINE; BONIN MARCANDRE; BELLEFLEUR MARCANDRE; PROVENCAL ALEXANDRE; CLOUTIER PHILIPE; PUCCI BERNARD; ROY RENE; GABIUS HANSJOACHIM,期刊：Bioorganic & Medicinal Chemistry, 页码：3280-3287 , 文章类型： Article，,卷期：2011年19-10] Galactose is the key contact site for plant AB-toxins and the human adhesion/growth-regulatory galectins. Natural anomeric extensions and 3'-substitutions enhance its reactivity, thus prompting us to test the potential o... Design of small molecule inhibitors of acetyl-CoA carboxylase 1 and 2 showing reduction of hepatic malonyl-CoA levels in vivo in obese Zucker rats [作者：BENGTSSON CHRISTOFFER; BLAHO STEFAN; SAITTON DAVID BLOMBERG; BRICKMANN KAY; BRODDEFALK JOHAN; DAVIDSSON OJVIND; DRMOTA TOMAS; FOLMER RUTGER; HALLBERG KENTH; HALLEN STEFAN; HOVLAND RAGNAR; ISIN EMRE; JOHANNESSON PETRA; KULL BENGT; LARSSON LARSOLOF; LOFGREN LARS; NILSSON KRISTINA E; NOESKE TOBIAS; OAKES NICK; PLOWRIGHT ALLEYN T; SCHNECKE VOLKER; STAHLBERG PERNILLA; SORME PERNILLA; WAN HONG; WELLNER ERIC; OSTER LINDA,期刊：Bioorganic & Medicinal Chemistry, 页码：3039-3053 , 文章类型： Article，,卷期：2011年19-10] Inhibition of acetyl-CoA carboxylases has the potential for modulating long chain fatty acid biosynthesis and mitochondrial fatty acid oxidation. Hybridization of weak inhibitors of ACC2 provided a novel, moderately pote... Preparation of allosamidin and demethylallosamidin photoaffinity probes and analysis of allosamidin-binding proteins in asthmatic mice [作者：SATO YOSUKE; SUZUKI SHIGEO; MURAOKA SEIKO; KIKUCHI NAOYA; NODA NAOTAKA; MATSUMOTO TAKAFUMI; INOUE HIROMASA; NAGASAWA HIROMICHI; SAKUDA SHOHEI,期刊：Bioorganic & Medicinal Chemistry, 页码：3054-3059 , 文章类型： Article，,卷期：2011年19-10] Allosamidins, metabolites of Streptomyces with strong inhibitory activities toward family 18 chitinases, show a variety of biological activities in various organisms. We prepared photoaffinity and biotinylated probes of ... Synthesis and antifungal activities of natural and synthetic biflavonoids [作者：SAGRERA GABRIEL; BERTUCCI ANA; VAZQUEZ ALVARO; SEOANE GUSTAVO,期刊：Bioorganic & Medicinal Chemistry, 页码：3060-3073 , 文章类型： Article，,卷期：2011年19-10] The synthesis of some natural and synthetic biflavonoids was performed in good overall yields starting from readily available materials via high yielding aldol and Ullmann condensations. Some of these compounds, especial... New 3-, 8-disubstituted pyrazolo[5,1-c][1,2,4]benzotriazines useful for studying the interaction with the HBp-3 area (hydrogen bond point area) in the benzodiazepine site on the gamma-aminobutyric acid type A (GABA(A)) receptor [作者：GUERRINI GABRIELLA; CICIANI GIOVANNA; BRUNI FABRIZIO; SELLERI SILVIA; MELANI FABRIZIO; DANIELE SIMONA; MARTINI CLAUDIA; COSTANZO ANNARELLA,期刊：Bioorganic & Medicinal Chemistry, 页码：3074-3085 , 文章类型： Article，,卷期：2011年19-10] The pharmacophoric model using ADLR procedure, based on pyrazolo[5,1-c][1,2,4]benzotriazine system, studied in our laboratory, allowed us to identify the essential interaction points (HBp-1, HBp-2, and Lp-1) and the impo... Virtual screening and further development of novel ALK inhibitors [作者：OKAMOTO MASAKO; KOJIMA HIROTATSU; SAITO NAE; OKABE TAKAYOSHI; MASUDA YOSHIAKI; FURUYA TOSHIO; NAGANO TETSUO,期刊：Bioorganic & Medicinal Chemistry, 页码：3086-3095 , 文章类型： Article，,卷期：2011年19-10] Anaplastic lymphoma kinase (ALK) has been in the spotlight in recent years as a promising new target for therapy of non-small-cell lung cancer (NSCLC). Since the identification of the echinoderm microtubule-associated pr... Synthesis and biological evaluation of unique stereodimers of sinomenine analogues as potential inhibitors of NO production [作者：TENG PENG; LIU HAILIANG; DENG ZHANGSHUANG; SHI ZHIBING; HE YUNMIAN; FENG LILI; XU QIANG; LI JIANXIN,期刊：Bioorganic & Medicinal Chemistry, 页码：3096-3104 , 文章类型： Article，,卷期：2011年19-10] Inhibition of the excessive NO production has been recognized as a potential means for the treatment of rheumatoid arthritis (RA). In order to discover more potent inhibitors and explore the preliminary structure activit... Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies [作者：CARTA FABRIZIO; GARAJ VLADIMIR; MARESCA ALFONSO; WAGNER JASON; AVVARU BALENDU SANKARA; ROBBINS ARTHUR H; SCOZZAFAVA ANDREA; MCKENNA ROBERT; SUPURAN CLAUDIU T,期刊：Bioorganic & Medicinal Chemistry, 页码：3105-3119 , 文章类型： Article，,卷期：2011年19-10] Reaction of cyanuryl chloride with D, L-amino acids and amino alcohols afforded a new series of triazinyl-substituted benzenesulfonamides incorporating amino acyl/hydroxyalkyl-amino moieties. Inhibition studies of physio... Tryptamine derivatives as novel non-nucleosidic inhibitors against hepatitis B virus [作者：QU SHIJIN; WANG GUIFENG; DUAN WENHU; YAO SHANYAN; ZUO JIANPING; TAN CHANGHENG; ZHU DAYUAN,期刊：Bioorganic & Medicinal Chemistry, 页码：3120-3127 , 文章类型： Article，,卷期：2011年19-10] A series of tryptamine derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. The preliminary SAR was discussed. Compounds 2e and 4a showe... Cellular zwitterionic metabolite analogs simultaneously enhance reaction rate, thermostability, salt tolerance, and substrate specificity of alpha-glucosidase [作者：DEGUCHI EISUKE; KOUMOTO KAZUYA,期刊：Bioorganic & Medicinal Chemistry, 页码：3128-3134 , 文章类型： Article，,卷期：2011年19-10] We investigated the structural effects of metabolite analogs derived from a naturally-occurring zwitterionic metabolite, glycine betaine, on the activity of several hydrolases. The initial velocities of the hydrolases we... Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation [作者：LIARAS K; GERONIKAKI A; GLAMOCLIJA J; CIRIC A; SOKOVIC M,期刊：Bioorganic & Medicinal Chemistry, 页码：3135-3140 , 文章类型： Article，,卷期：2011年19-10] As part of ongoing studies in developing new antimicrobials, we report the synthesis of a new class of structurally novel derivatives, that incorporate two known bioactive structures a thiazole and chalcone, to yield a c... Design, synthesis and pharmacological evaluation of spirocyclic sigma(1) receptor ligands with exocyclic amino moiety (increased distance 1) [作者：RACK ELISABETH; FROEHLICH ROLAND; SCHEPMANN DIRK; WUENSCH BERNHARD,期刊：Bioorganic & Medicinal Chemistry, 页码：3141-3151 , 文章类型： Article，,卷期：2011年19-10] Various pharmacophore models for potent sigma(1) ligands specify a basic amino group flanked by two different hydrophobic regions in defined distances to the basic amine (distance 1 and distance 2, respectively). Accordi... Protective effect of epsilon-viniferin on beta-amyloid peptide aggregation investigated by electrospray ionization mass spectrometry [作者：RICHARD TRISTAN; POUPARD PASCAL; NASSRA MERIAN; PAPASTAMOULIS YORGOS; IGLESIAS MARIELAURE; KRISA STEPHANIE; WAFFOTEGUO PIERRE; MERILLON JEANMICHEL; MONTI JEANPIERRE,期刊：Bioorganic & Medicinal Chemistry, 页码：3152-3155 , 文章类型： Article，,卷期：2011年19-10] Abnormal beta-amyloid peptide accumulation and aggregation is considered to be responsible for the formation and cerebral deposition of senile plaques in the brains of patients with Alzheimer's disease (AD). Inhibition o... Peroxisome proliferator-activated receptor agonists with phenethylphenylphthalimide skeleton derived from thalidomide-related liver X receptor antagonists: Relationship between absolute configuration and subtype selectivity [作者：MOTOSHIMA KAZUNORI; ISHIKAWA MINORU; HASHIMOTO YUICHI; SUGITA KAZUYUKI,期刊：Bioorganic & Medicinal Chemistry, 页码：3156-3172 , 文章类型： Article，,卷期：2011年19-10] Introduction of an alkylcarboxylic acid unit, which is a partial structure of endogenous peroxisome proliferator-activated receptor (PPAR) ligands, into a phenethylphenylphthalimide skeleton, which possesses liver X rece... Avoidance of the Ames test liability for aryl-amines via computation [作者：MCCARREN PATRICK; BEBERNITZ GREGORY R; GEDECK PETER; GLOWIENKE SUSANNE; GRONDINE MELISSA S; KIRMAN LOUISE C; KLICKSTEIN JACOB; SCHUSTER HERBERT F; WHITEHEAD LEWIS,期刊：Bioorganic & Medicinal Chemistry, 页码：3173-3182 , 文章类型： Article，,卷期：2011年19-10] Aryl-amines are commonly used synthons in modern drug discovery, however a minority of these chemical templates have the potential to cause toxicity through mutagenicity. The toxicity mostly arises through a series of me...