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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45条记录   Syntheses and pharmacological characterization of novel thiazole derivatives as potential mGluR5 PET ligands [作者：BAUMANN CINDY A; MU LINJING; WERTLI NICOLE; KRAEMER STEFANIE D; HONER MICHAEL; SCHUBIGER PIUS A; AMETAMEY SIMON M,期刊：Bioorganic & Medicinal Chemistry, 页码：6044-6054 , 文章类型： Article，,卷期：2010年18-16] Four novel thiazole containing ABP688 derivatives were synthesized and evaluated for their binding affinity towards the metabotropic glutamate receptor subtype 5 (mGluR5). (E)-3-((2-(Fluoromethyl)thiazol-4-yl)ethynyl)cyc... Synergistic experimental/computational studies on arylazoenamine derivatives that target the bovine viral diarrhea virus RNA-dependent RNA polymerase [作者：GILIBERTI GABRIELE; IBBA CRISTINA; MARONGIU ESTHER; LODDO ROBERTA; TONELLI MICHELE; BOIDO VITO; LAURINI ERIK; POSOCCO PAOLA; FERMEGLIA MAURIZIO; PRICL SABRINA,期刊：Bioorganic & Medicinal Chemistry, 页码：6055-6068 , 文章类型： Article，,卷期：2010年18-16] Starting from a series of arylazoenamine derivatives, shown to be selectively and potently active against the bovine viral diarrhea virus (BVDV), we developed a hierarchical combined experimental/molecular modeling strat... Synthesis of pyridazine and thiazole analogs as SGLT2 inhibitors [作者：KANG SUK YOUN; SONG KWANGSEOP; LEE JUNWON; LEE SUNGHAN; LEE JINHWA,期刊：Bioorganic & Medicinal Chemistry, 页码：6069-6079 , 文章类型： Article，,卷期：2010年18-16] With anticipation of the improvement in biological aspects in our SGLT2 program, novel pyridazinyl and thiazolyl analogs were designed and efficiently synthesized. The installation of the pyridazine ring at the anomeric ... Dimethylaminopyridine derivatives of lupane triterpenoids are potent disruptors of mitochondrial structure and function [作者：HOLY JON; KOLOMITSYNA OKSANA; KRASUTSKY DMYTRO; OLIVEIRA PAULO J; PERKINS EDWARD; KRASUTSKY PAVEL A,期刊：Bioorganic & Medicinal Chemistry, 页码：6080-6088 , 文章类型： Article，,卷期：2010年18-16] Development of mitochondrially-targeted drugs is receiving increasing attention because of the central roles these organelles play in energy production, reactive oxygen generation, and regulation of cell death pathways. ... A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity [作者：STANLEY NATHAN J; HUTCHINSON MARK R; KVIST TRINE; NIELSEN BIRGITTE; MATHIESEN JESPER MOSOLFF; BRAUNEROSBORNE HANS; AVERY THOMAS D; TIEKINK EDWARD R T; PEDERSEN DANIEL SEJER; IRVINE RODNEY J; ABELL ANDREW D; TAYLOR DENNIS K,期刊：Bioorganic & Medicinal Chemistry, 页码：6089-6098 , 文章类型： Article，,卷期：2010年18-16] As part of the vital search towards improved therapeutic agents for the treatment of neuropathic pain, the central nervous system glutamate receptors have become a major focus of research. Outlined herein are the synthes... Functional profiling of p53-binding sites in Hdm2 and Hdmx using a genetic selection system [作者：DATTA SHREYA; BUCKS MEGAN E; KOLEY DIPANKAR; LIM PEI XIN; SAVINOV SERGEY N,期刊：Bioorganic & Medicinal Chemistry, 页码：6099-6108 , 文章类型： Article，,卷期：2010年18-16] Upregulation of structurally homologous oncoproteins Hdm2 and Hdmx has been linked to the depletion or inactivation of their common regulation target the tumor suppressor p53 protein leading to the progression of cancer.... CLEFMA-An anti-proliferative curcuminoid from structure-activity relationship studies on 3,5-bis(benzylidene)-4-piperidones [作者：LAGISETTY PALLAVI; VILEKAR PRACHI; SAHOO KAUSTUV; ANANT SHRIKANT; AWASTHI VIBHUDUTTA,期刊：Bioorganic & Medicinal Chemistry, 页码：6109-6120 , 文章类型： Article，,卷期：2010年18-16] 3,5-Bis(benzylidene)-4-piperidones are being advanced as synthetic analogs of curcumin for anti-cancer and anti-inflammatory properties. We performed structure-activity relationship studies, by testing several synthesize... Large flanking sequence effects in single nucleotide mismatch detection using fluorescent nucleoside C-f [作者：GARDARSSON HARALDUR; SIGURDSSON SNORRI TH,期刊：Bioorganic & Medicinal Chemistry, 页码：6121-6126 , 文章类型： Article，,卷期：2010年18-16] The first systematic study of flanking sequence effects on mismatch detection by a fluorescent nucleotide is described, using fluoroside C-f. Although a high degree of variance was observed in fluorescence intensity of m... Anhydrotetracycline-peptide conjugates as representatives for ligand-based transactivating systems [作者：LOCHNER SUSANNE; EINSIEDEL JUERGEN; SCHAEFER GESA; BERENS CHRISTIAN; HILLEN WOLFGANG; GMEINER PETER,期刊：Bioorganic & Medicinal Chemistry, 页码：6127-6133 , 文章类型： Article，,卷期：2010年18-16] Bioconjugates of anhydrotetracycline and minimal activation sequences (VP1, VP2) derived from the Herpes simplex virus protein VP16 were synthesized. Different ligation strategies were applied and the resulting molecules... Design, synthesis, and anticonvulsant activity of new N-Mannich bases derived from spirosuccinimides and spirohydantoins [作者：OBNISKA JOLANTA; BYRTUS HANNA; KAMINSKI KRZYSZTOF; PAWLOWSKI MACIEJ; SZCZESIO MALGORZATA; KAROLAKWOJCIECHOWSKA JANINA,期刊：Bioorganic & Medicinal Chemistry, 页码：6134-6142 , 文章类型： Article，,卷期：2010年18-16] The synthesis and anticonvulsant properties of new N-Mannich bases of [7,8-f]benzo-2-azaspiro[4.5]decane-1,3-diones (5a-h) and [7,8-f]benzo-1,3-diaza-spiro[4.5]decane-2,4-diones (7a-h) were described. Initial anticonvuls... Synthesis and anti-hepatitis C virus activity of novel ethyl 1H-indole-3-carboxylates in vitro [作者：SELLITTO GRAZIA; FARUOLO AURORA; DE CAPRARIIS PAOLO; ALTAMURA SERGIO; PAONESSA GIACOMO; CILIBERTO GENNARO,期刊：Bioorganic & Medicinal Chemistry, 页码：6143-6148 , 文章类型： Article，,卷期：2010年18-16] A series of ethyl 1H-indole-3-carboxylates 9a(1-6) and 9b(1-2) were prepared and evaluated in Huh-7.5 cells. Most of the compounds exhibited anti-hepatitis C virus (HCV) activities at low concentration. The selectivity i... Synthesis of novel 3,5-diaryl pyrazole derivatives using combinatorial chemistry as inhibitors of tyrosinase as well as potent anticancer, anti-inflammatory agents [作者：BANDGAR BABASAHEB P; TOTRE JALINDER V; GAWANDE SHRIKANT S; KHOBRAGADE C N; WARANGKAR SUCHITA C; KADAM PRASAD D,期刊：Bioorganic & Medicinal Chemistry, 页码：6149-6155 , 文章类型： Article，,卷期：2010年18-16] In the present article, we have synthesized a combinatorial library of 3,5-diaryl pyrazole derivatives using 8-(2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-5,7-dimethoxy-2-phenyl-4H -chromen-4-one (1) and hydrazine hydrat... Further optimization of novel pyrrole 3-carboxamides for targeting serotonin 5-HT2A, 5-HT2C, and the serotonin transporter as a potential antidepressant [作者：KANG SUK YOUN; PARK EUNJUNG; PARK WOOKYU; KIM HYUN JUNG; CHOI GILDON; JUNG MYUNG EUN; SEO HEE JEONG; KIM MIN JU; PAE AE NIM; KIM JEONGMIN; LEE JINHWA,期刊：Bioorganic & Medicinal Chemistry, 页码：6156-6169 , 文章类型： Article，,卷期：2010年18-16] In the continuing search for novel compounds targeting serotonin 5-HT2A, 5-HT2C, and serotonin transporter, new arylpiperazine-containing pyrrole 3-carboxamide derivatives were synthesized and evaluated. Based on the lea... New porphyrin amino acid conjugates: Synthesis and photodynamic effect in human epithelial cells [作者：SERRA V VAZ; ZAMARRON A; FAUSTINO M A F; IGLESIASDE LA CRUZ M C; BLAZQUEZ A; RODRIGUES J M M; NEVES M G P M S; CAVALEIRO J A S; JUARRANZ A; SANZRODRIGUEZ F,期刊：Bioorganic & Medicinal Chemistry, 页码：6170-6178 , 文章类型： Article，,卷期：2010年18-16] The efficacy of new porphyrin amino acid conjugates as photosensitizers for photodynamic therapy (PDT) were assayed in vitro on tumoral (HeLa) and on non tumoral (HaCaT) human cell lines. The conjugates stable in liposom... Intramolecular acyl migration and enzymatic hydrolysis of a novel monoacylated ascorbic acid derivative, 6-O-dodecanoyl-2-O-alpha-D-glucopyranosyl-L-ascorbic acid [作者：TAI AKIHIRO; MORI TASUKU; URUSHIHARA MASAYA; ITO HIDEYUKI; KAWASAKI DAISUKE; YAMAMOTO ITARU,期刊：Bioorganic & Medicinal Chemistry, 页码：6179-6183 , 文章类型： Article，,卷期：2010年18-16] A stable ascorbic acid derivative, 2-O-alpha-D-glucopyranosyl-L-ascorbic acid (AA-2G), exhibits vitamin C activity in vitro and in vivo after enzymatic hydrolysis to ascorbic acid. AA-2G has been approved by the Japanese... Anti-Plasmodium activity of imidazolium and triazolium salts [作者：VLAHAKIS JASON Z; LAZAR CARMEN; CRANDALL IAN E; SZAREK WALTER A,期刊：Bioorganic & Medicinal Chemistry, 页码：6184-6196 , 文章类型： Article，,卷期：2010年18-16] We have previously reported that tetrazolium salts were both potent and specific inhibitors of Plasmodium replication, and that they appear to interact with a parasite component that is both essential and conserved. The ...