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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34条记录   Synthetic pseudopterosin analogues: A novel class of antiinflammatory drug candidates [作者：FLACHSMANN FELIX; SCHELLHAAS KURT; MOYA CLAUDIA E; JACOBS ROBERT S; FENICAL WILLIAM,期刊：Bioorganic & Medicinal Chemistry, 页码：8324-8333 , 文章类型： Article，,卷期：2010年18-23] The synthesis and in vivo anti-inflammatory activity of a series of pseudopterosin analogues are presented. Synthetic tricyclic catechol aglycons with different substitution patterns were monofucosylated or -xylosylated.... Acetazolamide-based fungal chitinase inhibitors [作者：SCHUETTELKOPF ALEXANDER W; GROS LUDOVIC; BLAIR DAVID E; FREARSON JULIE A; VAN AALTEN DAAN M F; GILBERT IAN H,期刊：Bioorganic & Medicinal Chemistry, 页码：8334-8340 , 文章类型： Article，,卷期：2010年18-23] Chitin is an essential structural component of the fungal cell wall. Chitinases are thought to be important for fungal cell wall remodelling, and inhibition of these enzymes has been proposed as a potential strategy for ... Towards the identification of unknown neuropeptide precursor-processing enzymes: Design and synthesis of a new family of dipeptidyl phosphonate activity probes for substrate-based protease identification [作者：SABIDO EDUARD; TARRAGO TERESA; GIRALT ERNEST,期刊：Bioorganic & Medicinal Chemistry, 页码：8350-8355 , 文章类型： Article，,卷期：2010年18-23] Specific proteolytic processing of inactive precursors is an exquisite cellular mechanism that triggers the activation of numerous physiologic peptides and proteins. This process ensures the generation of biologically ac... 1,3-Diphenyl-1H-pyrazole derivatives as a new series of potent PPAR gamma partial agonists [作者：CHOI JIWON; PARK YUNSUN; LEE HUI SUN; YANG YOUNG; YOON SUKJOON,期刊：Bioorganic & Medicinal Chemistry, 页码：8315-8323 , 文章类型： Article，,卷期：2010年18-23] A new series of PPAR gamma partial agonists, 1,3-diphenyl-1H-pyrazole derivatives, were identified using an improved virtual screening scheme combining ligand-centric and receptor-centric methods. An in vitro assay confi... Design, synthesis and inhibitory effect of pentapeptidyl chloromethyl ketones on proteinase K [作者：KORE ANILKUMAR R; SHANMUGASUNDARAM MUTHIAN,期刊：Bioorganic & Medicinal Chemistry, 页码：8383-8387 , 文章类型： Article，,卷期：2010年18-23] The synthesis and proteolytic inhibitor function of new modified pentapeptide MeOSuc-AAAPF-CH2Cl 6 is described. The efficacy of 6 in inhibiting the proteolytic activity of proteinase K at a concentration of 0.10 mM allo... Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands [作者：GU XIAOBO; IZENWASSER SARI; WADE DEAN; HOUSMAN AMY; GULASEY GERARD; RHODEN JILL B; SAVOIE CHRISTOPHER D; MOBLEY DAVID L; LOMENZO STACEY A; TRUDELL MARK L,期刊：Bioorganic & Medicinal Chemistry, 页码：8356-8364 , 文章类型： Article，,卷期：2010年18-23] A series of benzyl esters of meperidine and normeperidine were synthesized and evaluated for binding affinity at serotonin, dopamine and norepinephrine transporters. The 4-methoxybenzyl ester 8b and 4-nitrobenzyl ester 8... Design, synthesis and inhibition activity of novel cyclic peptides against protein tyrosine phosphatase A from Mycobacterium tuberculosis [作者：CHANDRA KOUSHIK; DUTTA DEBAJYOTI; DAS AMIT K; BASAK AMIT,期刊：Bioorganic & Medicinal Chemistry, 页码：8365-8373 , 文章类型： Article，,卷期：2010年18-23] Mycobacterium tuberculosis, the causative agent for tuberculosis has employed several signalling molecules to sense the host cellular environment and act accordingly. For example, protein tyrosine phosphatase A (MPtpA) o... Developing dual functional allosteric modulators of GABA(A) receptors [作者：LIU XIAODONG F; CHANG HUIFANG; SCHMIESING RICHARD JON; WESOLOWSKI STEVEN S; KNAPPENBERGER KATHARINE S; ARRIZA JEFFREY L; CHAPDELAINE MARC J,期刊：Bioorganic & Medicinal Chemistry, 页码：8374-8382 , 文章类型： Article，,卷期：2010年18-23] Positive modulators at benzodiazepine sites of alpha 2- and alpha 3-containing GABA(A) receptors are believed to be anxiolytic. Negative allosteric modulators of alpha 5-containing GABA(A) receptors enhance cognition. By... Cyclic peptide inhibitors of HIV-1 integrase derived from the LEDGF/p75 protein [作者：HAYOUKA ZVI; HUREVICH MATTAN; LEVIN AVIAD; BENYAMINI HADAR; IOSUB ANAT; MAES MICHAL; SHALEV DEBORAH E; LOYTER ABRAHAM; GILON CHAIM; FRIEDLER ASSAF,期刊：Bioorganic & Medicinal Chemistry, 页码：8388-8395 , 文章类型： Article，,卷期：2010年18-23] Restricting linear peptides to their bioactive conformation is an attractive way of improving their stability and activity. We used a cyclic peptide library with conformational diversity for selecting an active and stabl... N-6-Alkyladenosines: Synthesis and evaluation of in vitro anticancer activity [作者：OTTRIA ROBERTA; CASATI SILVANA; BALDOLI ERIKA; MAIER JEANETTE A M; CIUFFREDA PIERANGELA,期刊：Bioorganic & Medicinal Chemistry, 页码：8396-8402 , 文章类型： Article，,卷期：2010年18-23] A series of adenosine analogues differently substituted in N-6-position were synthesized to continue our studies on the relationships between structure and biological activity of iPA. The structures of the compounds were... Tuning hydrophobicity of highly cationic tetradecameric Gramicidin S analogues using adamantane amino acids [作者：KNIJNENBURG ANNEMIEK D; KAPOERCHAN VARSHA V; SPALBURG EMILE; DE NEELING ALBERT J; MARSGROENENDIJK ROOS H; NOORT DAAN; VAN DER MAREL GIJS A; OVERKLEEFT HERMAN S; OVERHAND MARK,期刊：Bioorganic & Medicinal Chemistry, 页码：8403-8409 , 文章类型： Article，,卷期：2010年18-23] Ring extended Gramicidin S analogues containing adamantane amino acids and six cationic residues were designed and evaluated. Systematic replacement of the hydrophobic residues with adamantane amino acids resulted in a s... Identification of novel antitubercular compounds through hybrid virtual screening approach (vol 18, pg 6914, 2010) [作者：MUDDASSAR MUHAMMAD; JANG JAE WAN; HONG SEUNG KON; CHO YONG SEO; KIM EUNICE EUNKYUNG; KEUM KYO CHANG; OH TAEGWON; CHO SANGNAE; PAE AE NIM,期刊：Bioorganic & Medicinal Chemistry, 页码：8410-8410 , 文章类型： Correction，,卷期：2010年18-23] Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer [作者：YOSHINO HITOSHI; SATO HARUHIKO; SHIRAISHI TAKUYA; TACHIBANA KAZUTAKA; EMURA TAKASHI; HONMA AKIE; ISHIKURA NOBUYUKI; TSUNENARI TOSHIAKI; WATANABE MIHO; NISHIMOTO AYAKO; NAKAMURA RYO; NAKAGAWA TOSHITO; OHTA MASATERU; TAKATA NORIYUKI; FURUMOTO KENTARO; KIMURA KAZUYA; KAWATA HIROMITSU,期刊：Bioorganic & Medicinal Chemistry, 页码：8150-8157 , 文章类型： Article，,卷期：2010年18-23] A series of 5,5-dimethylthiohydantoin derivatives were synthesized and evaluated for androgen receptor pure antagonistic activities for the treatment of castration-resistant prostate cancer. Since CH4933468, which we rep... Development of novel bisubstrate-type inhibitors of histone methyltransferase SET7/9 [作者：MORI SHUICHI; IWASE KENTA; IWANAMI NAOKO; TANAKA YUJIRO; KAGECHIKA HIROYUKI; HIRANO TOMOYA,期刊：Bioorganic & Medicinal Chemistry, 页码：8158-8166 , 文章类型： Article，,卷期：2010年18-23] Histone modification, for example, by histone deacetylase (HDAC) and histone lysine methyltransferase (HMT), plays an important role in regulating gene expression. To obtain novel inhibitors as tools for investigating th... Highly efficient controllable oxidation of alcohols to aldehydes and acids with sodium periodate catalyzed by water-soluble metalloporphyrins as biomimetic catalyst [作者：REN QINGGANG; CHEN SHAOYUN; ZHOU XIANTAI; JI HONGBING,期刊：Bioorganic & Medicinal Chemistry, 页码：8144-8149 , 文章类型： Article，,卷期：2010年18-23] Highly efficient controllable oxidation of alcohols to aldehydes or acids by sodium periodate in the presence of water-soluble manganese porphyrins (meso-tetrakis(N-ethylpyridinium-4-yl) manganese porphyrin, MnTEPyP) wit... Synthesis, antiproliferative activity in cancer cells and theoretical studies of novel 6 alpha,7 beta-dihydroxyvouacapan-17 beta-oic acid Mannich base derivatives [作者：EUZEBIO FELIPE P G; DOS SANTOS FLAVIO J L; PILOVELOSO DORILA; ALCANTARA ANTONIO F C; RUIZ ANA L T G; DE CARVALHO JOAO ERNESTO; FOGLIO MARY A; FERREIRAALVES DALTON L; DE FATIMA ANGELO,期刊：Bioorganic & Medicinal Chemistry, 页码：8172-8177 , 文章类型： Article，,卷期：2010年18-23] Natural products are great prototypes for the design of new anticancer agents. The plant-derived natural product 6 alpha,7 beta-dihydroxyvouacapan-17 beta-oic acid (1) is promising for the development of more potent anti...