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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19条记录   Identification of novel small molecule inhibitors of 4-diphosphocytidyl-2-C-methyl-D-erythritol (CDP-ME) kinase of Gram-negative bacteria [作者：TANG M; ODEJINMI S I; ALLETTE Y M; VANKAYALAPATI H; LAI K,期刊：Bioorganic & Medicinal Chemistry, 页码：5886-5895 , 文章类型： Article，,卷期：2011年19-19] The biosyntheses of isoprenoids is essential for the survival in all living organisms, and requires one of the two biochemical pathways: (a) Mevalonate (MVA) Pathway or (b) Methylerythritol Phosphate (MEP) Pathway. The l... Evaluation of PI polyamide conjugates with eight-base pair recognition and improvement of the aqueous solubility by PEGylation [作者：TAKAGAKI TOSHIKI; BANDO TOSHIKAZU; KITANO MASAAKI; HASHIYA KAORI; KASHIWAZAKI GENGO; SUGIYAMA HIROSHI,期刊：Bioorganic & Medicinal Chemistry, 页码：5896-5902 , 文章类型： Article，,卷期：2011年19-19] To investigate the effect of elongating base-pair (bp) recognition sequences, we synthesized N-methylpyrrole-N-methylimidazole (PI) polyamide conjugates with eight-bp recognition (3-5). The DNA alkylating activities of c... Modeling the molecular basis for alpha 4 beta 1 integrin antagonism [作者：HUTT OLIVER E; SAUBERN SIMON; WINKLER DAVID A,期刊：Bioorganic & Medicinal Chemistry, 页码：5903-5911 , 文章类型： Article，,卷期：2011年19-19] We report a 3D QSAR study of almost 300 structurally diverse small molecule antagonists of the integrin alpha 4 beta 1 whose biological activity spans six orders of magnitude. The alignment of the molecules was based on ... Synthesis of new six- and seven-membered 1-N-iminosugars as promising glycosidase inhibitors [作者：JABGUNDE AMIT M; KALAMKAR NAVNATH B; CHAVAN SANJAY T; SABHARWAL SUSHMA G; DHAVALE DILIP D,期刊：Bioorganic & Medicinal Chemistry, 页码：5912-5915 , 文章类型： Article，,卷期：2011年19-19] New six- and seven-membered 1-N-iminosugars were prepared from D-glucose by the stereoselective Michael addition of nitromethane to D-glucose derived alpha,beta-unsaturated ester A followed by one pot reduction of nitro/... Design and synthesis of inhibitors of noroviruses by scaffold hopping [作者：DOU DENGFENG; MANDADAPU SIVAKOTESWARA RAO; ALLISTON KEVIN R; KIM YUNJEONG; CHANG KYEONGOK; GROUTAS WILLIAM C,期刊：Bioorganic & Medicinal Chemistry, 页码：5749-5755 , 文章类型： Article，,卷期：2011年19-19] A scaffold hopping strategy was employed to identify new chemotypes that inhibit noroviruses. The replacement of the cyclosulfamide scaffold by an array of heterocyclic scaffolds lead to the identification of additional ... CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs [作者：LEBAR MATTHEW D; HAHN KRISTOPHER N; MUTKA TINA; MAIGNAN PATRICK; MCCLINTOCK JAMES B; AMSLER CHARLES D; VAN OLPHEN ALBERTO; KYLE DENNIS E; BAKER BILL J,期刊：Bioorganic & Medicinal Chemistry, 页码：5756-5762 , 文章类型： Article，,卷期：2011年19-19] The marine invertebrate-derived meridianin A. the originally proposed structure for psammopemmin A. and several related 3-pyrimidylindole analogs were synthesized and subsequently investigated for central nervous system,... Deep understanding of structure-solubility relationship for a diverse set of organic compounds using matched molecular pairs [作者：ZHANG LYING; ZHU HONGYAO; MATHIOWETZ ALAN; GAO HUA,期刊：Bioorganic & Medicinal Chemistry, 页码：5763-5770 , 文章类型： Article，,卷期：2011年19-19] Aqueous solubility is an important biopharmaceutical property in drug discovery and development. Although it has been studied for decades, the impact on solubility by the substructures (or fragments) of compounds are sti... A ribonucleopeptide module for effective conversion of an RNA aptamer to a fluorescent sensor [作者：LIEW FONG FONG; HAYASHI HIRONORI; NAKANO SHUN; NAKATA EIJI; MORII TAKASHI,期刊：Bioorganic & Medicinal Chemistry, 页码：5771-5775 , 文章类型： Article，,卷期：2011年19-19] Ribonucleopeptide (RNP) is a new class of scaffold for modular fluorescent sensors. We report here a short RNA motif that induces an efficient communication between the structural changes associated with the ligand-bindi... Potential AMPK activators of cucurbitane triterpenoids from Siraitia grosvenorii Swingle [作者：CHEN XUBING; ZHUANG JINGJING; LIU JUNHUA; LEI MIN; MA LEI; CHEN JING; SHEN XU; HU LIHONG,期刊：Bioorganic & Medicinal Chemistry, 页码：5776-5781 , 文章类型： Article，,卷期：2011年19-19] AMP-activated kinase (AMPK) as a key controller in the regulation of whole-body energy homeostasis, plays an important role in protecting the body from metabolic diseases. Recently, improved glucose, lipid utility and in... Antifungal activity of a series of 1,2-benzisothiazol-3(2H)-one derivatives [作者：DOU DENGFENG; ALEX DEEPU; DU BINGFAN; TIEW KOKCHUAN; ARAVAPALLI SRIDHAR; MANDADAPU SIVAKOTESWARA RAO; CALDERONE RICHARD; GROUTAS WILLIAM C,期刊：Bioorganic & Medicinal Chemistry, 页码：5782-5787 , 文章类型： Article，,卷期：2011年19-19] A series of broad-spectrum antifungal agents based on the 1,2-benzisothiazol-3(2H)-one scaffold is reported. Preliminary structure-activity relationship studies have established the importance of the presence of the hete... Probing DNA interstrand cross-link formation by an oxidized abasic site using nonnative nucleotides [作者：SCZEPANSKI JONATHAN T; HIEMSTRA CHRISTINE N; GREENBERG MARC M,期刊：Bioorganic & Medicinal Chemistry, 页码：5788-5793 , 文章类型： Article，,卷期：2011年19-19] The C4'-oxidized abasic site (C4-AP) forms two types of interstrand cross-links with the adjacent nucleotides in DNA. Previous experiments revealed that dG does not react with the lesion and that formation of one type of... 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents [作者：NOVIKOV MIKHAIL S; IVANOVA OLGA N; IVANOV ALEXANDER V; OZEROV ALEXANDER A; VALUEVELLISTON VLADIMIR T; TEMBURNIKAR KARTIK; GURSKAYA GALINA V; KOCHETKOV SERGEY N; PANNECOUQUE CHRISTOPHE; BALZARINI JAN; SELEYRADTKE KATHERINE L,期刊：Bioorganic & Medicinal Chemistry, 页码：5794-5802 , 文章类型： Article，,卷期：2011年19-19] Non-nucleoside reverse transcriptase inhibitors (NNRTI) are key components in highly active antiretroviral therapy for treating HIV-1. Herein we present the synthesis for a series of N1-alkylated uracil derivatives beari... Inhibitory effect of novel 5-O-acyl juglones on mammalian DNA polymerase activity, cancer cell growth and inflammatory response [作者：MARUO SAYAKO; KURIYAMA ISOKO; KURAMOCHI KOUJI; TSUBAKI KAZUNORI; YOSHIDA HIROMI; MIZUSHINA YOSHIYUKI,期刊：Bioorganic & Medicinal Chemistry, 页码：5803-5812 , 文章类型： Article，,卷期：2011年19-19] We previously found that vitamin K(3) (menadione, 2-methyl-1,4-naphthoquinone) inhibits the activity of human mitochondrial DNA polymerase gamma (pol gamma). In this study, we focused on juglone (5-hydroxy-1,4-naphthoqui... Novel thiophenyl C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents [作者：LEE SUK HO; SONG KWANGSEOP; KIM JONG YUP; KANG MISUK; LEE JUN SUNG; CHO SEUNGHWAN; PARK HYUNJU; KIM JEONGMIN; LEE JINHWA,期刊：Bioorganic & Medicinal Chemistry, 页码：5813-5832 , 文章类型： Article，,卷期：2011年19-19] Novel thiophene C-aryl glucoside SGLT2 inhibitors were designed and synthesized. Two different types of thiophene derivatives were readily prepared. Among the compounds tested, ethylphenyl at the distal ring 71p showed t... Exploiting differences in caspase-2 and-3 S(2) subsites for selectivity: Structure-based design, solid-phase synthesis and in vitro activity of novel substrate-based caspase-2 inhibitors [作者：MAILLARD MICHEL C; BROOKFIELD FREDERICK A; COURTNEY STEPHEN M; EUSTACHE FLORENCE M; GEMKOW MARK J; HANDEL REBECCA K; JOHNSON LAURA C; JOHNSON PETER D; KERRY MARK A; KRIEGER FLORIAN; MENICONI MIRCO; MUNOZSANJUAN IGNACIO; PALFREY JORDAN J; PARK HYUNSUN; SCHAERTL SABINE; TAYLOR MALCOLM G; WEDDELL DEREK; DOMINGUEZ CELIA,期刊：Bioorganic & Medicinal Chemistry, 页码：5833-5851 , 文章类型： Article，,卷期：2011年19-19] Several caspases have been implicated in the pathogenesis of Huntington's disease (HD); however, existing caspase inhibitors lack the selectivity required to investigate the specific involvement of individual caspases in... Searching for new NO-donor aspirin-like molecules: Furoxanylacyl derivatives of salicylic acid and related furazans [作者：LAZZARATO LORETTA; CENA CLARA; ROLANDO BARBARA; MARINI ELISABETTA; LOLLI MARCO LUCIO; GUGLIELMO STEFANO; GUAITA ELENA; MORINI GIUSEPPINA; CORUZZI GABRIELLA; FRUTTERO ROBERTA; GASCO ALBERTO,期刊：Bioorganic & Medicinal Chemistry, 页码：5852-5860 , 文章类型： Article，,卷期：2011年19-19] A new group of derivatives of salicylic acid containing NO-donor furoxans, and the related des-NO-furazans, were synthesized and evaluated as new aspirin-like molecules. Their stability was assessed in acid (pH 1) and ph...