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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21条记录   Synthesis, biological evaluation, and molecular docking studies of 2,5-substituted-1,4-benzoquinone as novel urease inhibitors [作者：YOU ZHONGLU; XIAN DONGMEI; ZHANG MEI; CHENG XIAOSHAN; LI XIAOFANG,期刊：Bioorganic & Medicinal Chemistry, 页码：4889-4894 , 文章类型： Article，,卷期：2012年20-16] A series of 2,5-substituted-1,4-benzoquinone (1-6) were prepared and structurally characterized by elemental analysis, IR spectra, H-1 and C-13 NMR spectra, and single crystal X-ray determination. The urease inhibitory a... Synthesis, biological evaluation, and molecular docking studies of N-((1,3-diphenyl-1H-pyrazol-4-yl)methyl)aniline derivatives as novel anticancer agents [作者：HUANG XIANFENG; LU XIANG; ZHANG YONG; SONG GUOQIANG; HE QILONG; LI QINGSHAN; YANG XIANHUI; WEI YAO; ZHU HAILIANG,期刊：Bioorganic & Medicinal Chemistry, 页码：4895-4900 , 文章类型： Article，,卷期：2012年20-16] A series of N-((1,3-diphenyl-1H-pyrazol-4-yl)methyl)aniline derivatives (5a-8d) have been designed and synthesized, and their biological activities were also evaluated as potential antitumor and cyclin dependent kinase 2... Synthesis of phenserine analogues and evaluation of their cholinesterase inhibitory activities [作者：SHINADA MASASHI; NARUMI FUMINORI; OSADA YUJI; MATSUMOTO KOJI; YOSHIDA TAKAYASU; HIGUCHI KAZUHIRO; KAWASAKI TOMOMI; TANAKA HIROYUKI; SATOH MITSUTOSHI,期刊：Bioorganic & Medicinal Chemistry, 页码：4901-4914 , 文章类型： Article，,卷期：2012年20-16] Phenserine is a potentially attractive drug for Alzheimer's disease. In order to further expand SAR study for inhibitions of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), the methyl group at the 3a-posit... Synthesis and characterization of a Ga-68-labeled N-(2-diethylaminoethyl)benzamide derivative as potential PET Probe for malignant melanoma [作者：KIM HEEJUNG; KIM DONGYEON; PARK JEONGHOON; YANG SEUNGDAE; HUR MINGOO; MIN JUNGJOON; YU KOOKHYUN,期刊：Bioorganic & Medicinal Chemistry, 页码：4915-4920 , 文章类型： Article，,卷期：2012年20-16] Radiolabeled benzamides have been reported to be attractive agents for targeting malignant melanoma as they bind melanin and display high accumulation in melanoma cells. Herein, we report the synthesis and bioevaluation ... Small molecules that protect against beta-amyloid-induced cytotoxicity by inhibiting aggregation of beta-amyloid [作者：LEE YUN SUK; KIM HYE YUN; KIM YOUNGSOO; SEO JAE HONG; ROH EUN JOO; HAN HOGYU; SHIN KYE JUNG,期刊：Bioorganic & Medicinal Chemistry, 页码：4921-4935 , 文章类型： Article，,卷期：2012年20-16] Aggregated beta-amyloid (A beta) plays crucial roles in Alzheimer's disease (AD) pathogenesis, therefore blockade of Ab aggregation is considered as a potential therapeutic target. We designed and synthesized small molec... Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT) [作者：KOZAKA TAKASHI; UNO IZUMI; KITAMURA YOJI; MIWA DAISUKE; OGAWA KAZUMA; SHIBA KAZUHIRO,期刊：Bioorganic & Medicinal Chemistry, 页码：4936-4941 , 文章类型： Article，,卷期：2012年20-16] A series of vesamicol analogues, o-iodo-trans-decalinvesamicol (OIDV) or o-bromo-trans-decalinvesamicol (OBDV), were synthesized and their affinities to vesicular acetylcholine transporter (VAChT) and sigma receptors (si... Rapid and efficient synthesis of a novel series of substituted aminobenzosuberone derivatives as potent, selective, non-peptidic neutral aminopeptidase inhibitors [作者：ALBRECHT SEBASTIEN; SALOMON EMMANUEL; DEFOIN ALBERT; TARNUS CELINE,期刊：Bioorganic & Medicinal Chemistry, 页码：4942-4953 , 文章类型： Article，,卷期：2012年20-16] Racemic 5-substituted 7-aminobenzocyclohepten-6-one were synthesized and evaluated for their ability to inhibit metalloaminopeptidase activities. Unexpectedly, 5-thio substituted compounds showed enhanced inhibition pote... Design and synthesis of marine fungal phthalide derivatives as PPAR-gamma agonists [作者：XIAO BIN; YIN JUN; PARK MINHI; LIU JUAN; LI JIAN LIN; KIM EUN LA; HONG JONGKI; CHUNG HAE YOUNG; JUNG JEE H,期刊：Bioorganic & Medicinal Chemistry, 页码：4954-4961 , 文章类型： Article，,卷期：2012年20-16] On the basis of a marine fungal phthalide (paecilocin A) skeleton, we synthesized 20 analogs and evaluated them for peroxisome proliferator-activated receptor gamma (PPAR-gamma) binding and activation. Among these analog... Synthesis of benzo-annulated tryptanthrins and their biological properties [作者：LIANG JING LU; PARK SOEUN; KWON YOUNGJOO; JAHNG YURNGDONG,期刊：Bioorganic & Medicinal Chemistry, 页码：4962-4967 , 文章类型： Article，,卷期：2012年20-16] A series of benzo-annulated derivatives of tryptanthrin were prepared and their optical and redox properties were studied. Tryptanthrin and its benzo-annulated derivatives showed selective inhibitory activity on topo I w... Suppressive effects of coumarins from Mammea siamensis on inducible nitric oxide synthase expression in RAW264.7 cells [作者：MORIKAWA TOSHIO; SUEYOSHI MAYUMI; CHAIPECH SAOWANEE; MATSUDA HISASHI; NOMURA YUKIKO; YABE MIKUKO; MATSUMOTO TOMOKO; NINOMIYA KIYOFUMI; YOSHIKAWA MASAYUKI; PONGPIRIYADACHA YUTANA; HAYAKAWA TAKAO; MURAOKA OSAMU,期刊：Bioorganic & Medicinal Chemistry, 页码：4968-4977 , 文章类型： Article，,卷期：2012年20-16] A methanol extract of the flowers of Mammea siamensis (Calophyllaceae) was found to inhibit nitric oxide (NO) production in lipopolysaccharide-activated RAW264.7 cells. From the extract, two new geranylated coumarins, ma... Synthesis and biological activity of novel bifunctional isoxazolidinyl polycyclic aromatic hydrocarbons [作者：RESCIFINA ANTONIO; ZAGNI CHIARA; ROMEO GIOVANNI; SORTINO SALVATORE,期刊：Bioorganic & Medicinal Chemistry, 页码：4978-4984 , 文章类型： Article，,卷期：2012年20-16] This paper reports the synthesis and the biological properties of two novel pyrene-bearing isoxazolidinyl derivatives able to exhibit antitumor activity by DNA intercalation. The synthetic approach exploits a consolidate... Acyl-sulfamates target the essential glycerol-phosphate acyltransferase (PlsY) in Gram-positive bacteria [作者：CHERIAN PHILIP T; YAO JIANGWEI; LEONARDI ROBERTA; MADDOX MARCUS M; LUNA VICKI A; ROCK CHARLES O; LEE RICHARD E,期刊：Bioorganic & Medicinal Chemistry, 页码：4985-4994 , 文章类型： Article，,卷期：2012年20-16] PlsY is the essential first step in membrane phospholipid synthesis of Gram-positive pathogens. PlsY catalyzes the transfer of the fatty acid from acyl-phosphate to the 1-position of glycerol-3-phosphate to form the firs... New oxirane derivatives of 1,4-naphthoquinones and their evaluation against T. cruzi epimastigote forms [作者：CARNEIRO PAULA F; DO NASCIMENTO SAMARA B; PINTO ANTONIO V; PINTO MARIA DO CARMO F R; LECHUGA GUILHERME C; SANTOS DILVANI O; DOS SANTOS JUNIOR HELVECIO M; RESENDE JACKSON A L C; BOURGUIGNON SAULO C; FERREIRA VITOR F,期刊：Bioorganic & Medicinal Chemistry, 页码：4995-5000 , 文章类型： Article，,卷期：2012年20-16] New oxirane derivatives were synthesized using six naphthoquinones as the starting materials. Our biological results showed that these oxiranes acted as trypanocidal agents against Trypanosoma cruzi with minimal cytotoxi... Synthesis of benzamide derivatives and their evaluation as antiprion agents [作者：FIORINO FERDINANDO; EIDEN MARTIN; GIESE ARMIN; SEVERINO BEATRICE; ESPOSITO ANTONELLA; GROSCHUP MARTIN H; PERISSUTTI ELISA; MAGLI ELISA; INCISIVO GIUSEPPINA MARIA; CIANO ANTONIO; FRECENTESE FRANCESCO; KRETZSCHMAR HANS A; WAGNER JENS; SANTAGADA VINCENZO; CALIENDO GIUSEPPE,期刊：Bioorganic & Medicinal Chemistry, 页码：5001-5011 , 文章类型： Article，,卷期：2012年20-16] A new set of 5-(2-(pyrrolidin-1-yl)acetamido)-N-butyl-2-(substituted) benzamide and 5-(2-(piperidin-1-yl)acetamido)-N-butyl-2-(substituted) benzamide derivatives were synthesized in which as structural features the 2-(1-... Identification of new gamma-hydroxybutenolides that preferentially inhibit the activity of mPGES-1 [作者：DE SIMONE ROSA; BRUNO INES; RICCIO RAFFAELE; STADLER KATHARINA; BAUER JULIA; SCHAIBLE ANJA M; LAUFER STEFAN; WERZ OLIVER,期刊：Bioorganic & Medicinal Chemistry, 页码：5012-5016 , 文章类型： Article，,卷期：2012年20-16] Microsomal prostaglandin E-2 synthase-1 (mPGES-1) has been recognized as novel, promising drug target for anti-inflammatory and anticancer drugs. mPGES-1 catalyzes the synthesis of the inducible prostaglandin E-2 in resp... Synthesis and biological evaluation of alpha-methylidene-delta-lactones with 3,4-dihydrocoumarin skeleton [作者：MODRANKA JAKUB; ALBRECHT ANNA; JAKUBOWSKI RAFAL; KRAWCZYK HENRYK; ROZALSKI MAREK; KRAJEWSKA URSZULA; JANECKA ANNA; WYREBSKA ANNA; ROZALSKA BARBARA; JANECKI TOMASZ,期刊：Bioorganic & Medicinal Chemistry, 页码：5017-5026 , 文章类型： Article，,卷期：2012年20-16] A series of new 3-methylidenechroman-2-ones bearing various aromatic moieties and various substituents at position 4 were synthesized in a three step reaction sequence. Friedel-Crafts alkylation of phenols or naphthols u...