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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   Screening a library of 1600 adamantyl ureas for anti-Mycobacterium tuberculosis activity in vitro and for better physical chemical properties for bioavailability [作者：SCHERMAN MICHAEL S; NORTH ELTON J; JONES VICTORIA; HESS TAMARA N; GRZEGORZEWICZ ANNA E; KASAGAMI TAKEO; KIM INHAE; MERZLIKIN OLEG; LENAERTS ANNE J; LEE RICHARD E; JACKSON MARY; MORISSEAU CHRISTOPHE; MCNEIL MICHAEL R,期刊：Bioorganic & Medicinal Chemistry, 页码：3255-3262 , 文章类型： Article，,卷期：2012年20-10] Adamantyl ureas were previously identified as a group of compounds active against Mycobacterium tuberculosis in culture with minimum inhibitor concentrations (MICs) below 0.1 mu g/ml. These compounds have been shown to t... Discovery of ipragliflozin (ASP1941): A novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus [作者：IMAMURA MASAKAZU; NAKANISHI KEITA; SUZUKI TAKAYUKI; IKEGAI KAZUHIRO; SHIRAKI RYOTA; OGIYAMA TAKASHI; MURAKAMI TAKESHI; KUROSAKI EIJI; NODA ATSUSHI; KOBAYASHI YOSHINORI; YOKOTA MASAYUKI; KOIDE TOMOKAZU; KOSAKAI KAZUHIRO; OHKURA YASUFUMI; TAKEUCHI MAKOTO; TOMIYAMA HIROSHI; OHTA MITSUAKI,期刊：Bioorganic & Medicinal Chemistry, 页码：3263-3279 , 文章类型： Article，,卷期：2012年20-10] A series of C-glucosides with various heteroaromatics has been synthesized and its inhibitory activity toward SGLTs was evaluated. Upon screening several compounds, the benzothiophene derivative (14a) was found to have p... Paviosides A-H, eight new oleane type saponins from Aesculus pavia with cytotoxic activity [作者：LANZOTTI VIRGINIA; TERMOLINO PASQUALE; DOLCI MARCELLO; CURIR PAOLO,期刊：Bioorganic & Medicinal Chemistry, 页码：3280-3286 , 文章类型： Article，,卷期：2012年20-10] A phytochemical analysis of Aesculus pavia has led to the isolation of eight novel triterpenoid saponins, based on oleane type skeleton and named paviosides A-H (1a, 1b-4a, 4b). On the basis of chemical, and 2D NMR and m... Evaluation of a synthetic C34 trimer of HIV-1 gp41 as AIDS vaccines [作者：HASHIMOTO CHIE; NOMURA WATARU; OHYA AKI; URANO EMIKO; MIYAUCHI KOSUKE; NARUMI TETSUO; AIKAWA HARUO; KOMANO JUN A; YAMAMOTO NAOKI; TAMAMURA HIROKAZU,期刊：Bioorganic & Medicinal Chemistry, 页码：3287-3291 , 文章类型： Article，,卷期：2012年20-10] An artificial antigen forming the C34 trimeric structure targeting membrane-fusion mechanism of HIV-1 has been evaluated as an HIV vaccine. The C34 trimeric molecule was previously designed and synthesized using a novel ... Investigating the activity of quinine analogues versus chloroquine resistant Plasmodium falciparum [作者：DINIO THERESA; GORKA ALEXANDER P; MCGINNISS ANDREW; ROEPE PAUL D; MORGAN JEREMY B,期刊：Bioorganic & Medicinal Chemistry, 页码：3292-3297 , 文章类型： Article，,卷期：2012年20-10] Plasmodium falciparum, the deadliest malarial parasite species, has developed resistance against nearly all man-made antimalarial drugs within the past century. However, quinine (QN), the first antimalarial drug, remains... A highly selective Hsp90 affinity chromatography resin with a cleavable linker [作者：HUGHES PHILIP F; BARROTT JARED J; CARLSON DAVID A; LOISELLE DAVID R; SPEER BRITTANY L; BODOOR KHALDON; RUND LAURETTA A; HAYSTEAD TIMOTHY A J,期刊：Bioorganic & Medicinal Chemistry, 页码：3298-3305 , 文章类型： Article，,卷期：2012年20-10] Over 200 proteins have been identified that interact with the protein chaperone Hsp90, a recognized therapeutic target thought to participate in non-oncogene addiction in a variety of human cancers. However, defining Hsp... Synthesis, biological evaluation and molecular modeling study of pyrazole and pyrazoline derivatives as selective COX-2 inhibitors and anti-inflammatory agents. Part 2 [作者：ELSAYED MAGDA A A; ABDELAZIZ NAGLAA I; ABDELAZIZ ALAA A M; ELAZAB ADEL S; ELTAHIR KAMAL E H,期刊：Bioorganic & Medicinal Chemistry, 页码：3306-3316 , 文章类型： Article，,卷期：2012年20-10] New pyrazole and pyrazoline derivatives have been synthesized and their ability to inhibit ovine COX-1/COX-2 isozymes was evaluated using in vitro cyclooxygenase (COX) inhibition assay. Among the tested compounds, N-((5-... A comparative study of backbone versus side chain peptide cyclization: Application for HIV-1 integrase inhibitors [作者：HAYOUKA ZVI; LEVIN AVIAD; HUREVICH MATTAN; SHALEV DEBORAH E; LOYTER ABRAHAM; GILON CHAIM; FRIEDLER ASSAF,期刊：Bioorganic & Medicinal Chemistry, 页码：3317-3322 , 文章类型： Article，,卷期：2012年20-10] Peptide cyclization is an important tool for overcoming the limitations of linear peptides as drugs. Backbone cyclization (BC) has advantages over side chain (SC) cyclization because it combines N-alkylation for extra pe... Synthesis, sigma(1), sigma(2)-receptors binding affinity and antiproliferative action of new C1-substituted adamantanes [作者：RIGANAS STEFANOS; PAPANASTASIOU IOANNIS; FOSCOLOS GEORGE B; TSOTINIS ANDREW; BOURGUIGNON JEANJACQUES; SERIN GUILLAUME; MIRJOLET JEANFRANCOIS; DIMAS KOSTAS; KOURAFALOS VASSILIOS N; ELEUTHERIADES ANDREAS; MOUTSOS VASSILIOS I; KHAN HUMAIRA; GEORGAKOPOULOU STAVROULA; ZANIOU ANGELIKI; PRASSA MARGARITA; THEODOROPOULOU MARIA; PONDIKI STAVROULA; VAMVAKIDES ALEXANDRE,期刊：Bioorganic & Medicinal Chemistry, 页码：3323-3331 , 文章类型： Article，,卷期：2012年20-10] The synthesis of N-{4-[a-(1-adamantyl)benzyl]phenyl}piperazines 2a-e is described. The in vitro antiproliferative activity of most compounds against main cancer cell lines is significant. The sigma(1),sigma(2)-receptors ... Structure-activity relationships and key structural feature of pyridyloxybenzene-acylsulfonamides as new, potent, and selective peroxisome proliferator-activated receptor (PPAR) gamma Agonists [作者：RIKIMARU KENTARO; WAKABAYASHI TAKESHI; ABE HIDENORI; TAWARAISHI TAISUKE; IMOTO HIROSHI; YONEMORI JINICHI; HIROSE HIDEKI; MURASE KATSUHITO; MATSUO TAKANORI; MATSUMOTO MITSUHARU; NOMURA CHISAKO; TSUGE HIROKO; ARIMURA NAOTO; KAWAKAMI KAZUTOSHI; SAKAMOTO JUNICHI; FUNAMI MIYUKI; MOL CLIFFORD D; SNELL GYORGY P; BRAGSTAD KENNETH A; SANG BICHING; DOUGAN DOUGLAS R; TANAKA TOSHIMASA; KATAYAMA NOZOMI; HORIGUCHI YOSHIAKI; MOMOSE YU,期刊：Bioorganic & Medicinal Chemistry, 页码：3332-3358 , 文章类型： Article，,卷期：2012年20-10] In our search for a novel class of non-TZD, non-carboxylic acid peroxisome proliferator-activated receptor (PPAR) gamma agonists, we explored alternative lipophilic templates to replace benzylpyrazole core of the previou... Synthesis, biological evaluation and molecular docking studies of 1,3,4-oxadiazole derivatives as potential immunosuppressive agents [作者：ZHANG ZHIMING; ZHANG XUEWEI; ZHAO ZONGZHENG; YAN RU; XU RUI; GONG HAIBIN; ZHU HAILIANG,期刊：Bioorganic & Medicinal Chemistry, 页码：3359-3367 , 文章类型： Article，,卷期：2012年20-10] A series of 1,3,4-oxadiazole derivatives derived from 4-methoxysalicylic acid or 4-methylsalicylic acid (6a-6z) have been first synthesized for their potential immunosuppressive activity. Among them, compound 6z displaye... Hepatitis C RNA-dependent RNA polymerase inhibitors: A review of structure-activity and resistance relationships; different scaffolds and mutations [作者：MAYHOUB ABDELRAHMAN S,期刊：Bioorganic & Medicinal Chemistry, 页码：3150-3161 , 文章类型： Review，,卷期：2012年20-10] Hepatitis C virus (HCV), like many other flaviviruses, is widely distributed worldwide with estimated chronically infected victims between 170 and 200 million. HCV inherent error-prone RNA-dependent RNA polymerase (RdRp)... Abscinazole-E2B, a practical and selective inhibitor of ABA 8 '-hydroxylase CYP707A [作者：OKAZAKI MARIKO; KITTIKORN MONRUDEE; UENO KOTOMI; MIZUTANI MASAHARU; HIRAI NOBUHIRO; KONDO SATORU; OHNISHI TOSHIYUKI; TODOROKI YASUSHI,期刊：Bioorganic & Medicinal Chemistry, 页码：3162-3172 , 文章类型： Article，,卷期：2012年20-10] We developed abscinazole-E2B (Abz-E2B), a practical and specific inhibitor of abscisic acid (ABA) 80hydroxylase (CYP707A), by structural modification of abscinazole-E1 (Abz-E1), another compound we developed. A butoxy gr... 3-Deoxy-3,4-dehydro analogs of XM462. Preparation and activity on sphingolipid metabolism and cell fate [作者：CAMACHO LUZ; SIMBARI FABIO; GARRIDO MARIA; LUIS ABAD JOSE; CASAS JOSEFINA; DELGADO ANTONIO; FABRIAS GEMMA,期刊：Bioorganic & Medicinal Chemistry, 页码：3173-3179 , 文章类型： Article，,卷期：2012年20-10] Three analogs of the dihydroceramide desaturase inhibitor XM462 are reported. The compounds inhibit both dihydroceramide desaturase and acid ceramidase, but with different potencies depending on the N-acyl moiety. Other ... An efficient and convenient microwave-assisted chemical synthesis of (thio)xanthones with additional in vitro and in silico characterization [作者：VERBANAC DONATELLA; JAIN SUBHASH C; JAIN NIDHI; CHAND MAHESH; PALJETAK HANA CIPCIC; MATIJASIC MARIO; PERIC MIHAELA; STEPANIC VISNJA; SASO LUCIANO,期刊：Bioorganic & Medicinal Chemistry, 页码：3180-3185 , 文章类型： Article，,卷期：2012年20-10] Xanthones and their thio-derivatives are a class of pleiotropic compounds with various reported pharmacological and biological activities. Although these activities are mainly determined in laboratory conditions, the cla... Synthesis and biological evaluation of a new class of glycoconjugated disulfides that exhibit potential anticancer properties [作者：BONACCORSI PAOLA; MARINOMERLO FRANCESCA; BARATTUCCI ANNA; BATTAGLIA GIANLUCA; PAPAIANNI EMANUELA; PAPALIA TERESA; AVERSA MARIA C; MASTINO ANTONIO,期刊：Bioorganic & Medicinal Chemistry, 页码：3186-3195 , 文章类型： Article，,卷期：2012年20-10] A synthetic strategy, based on the in situ generation of sulfenic acids and their thermolysis in the presence of thiols, was developed for obtaining a collection of polyvalent disulfides in which a benzene scaffold accom...