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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32条记录   The therapeutic journey of benzimidazoles: A review [作者：BANSAL YOGITA; SILAKARI OM,期刊：Bioorganic & Medicinal Chemistry, 页码：6208-6236 , 文章类型： Review，,卷期：2012年20-21] Presence of benzimidazole nucleus in numerous categories of therapeutic agents such as antimicrobials, antivirals, antiparasites, anticancer, anti-inflammatory, antioxidants, proton pump inhibitors, antihypertensives, an... Tandem photoaffinity labeling-bioorthogonal conjugation in medicinal chemistry [作者：LAPINSKY DAVID J,期刊：Bioorganic & Medicinal Chemistry, 页码：6237-6247 , 文章类型： Review，,卷期：2012年20-21] Photoaffinity labeling has a longstanding history as a powerful biochemical technique. However, photoaffinity labeling has significantly evolved over the past decade principally due to its coupling with bioorthogonal/cli... The antitumor agent doxorubicin binds to Fanconi anemia group F protein [作者：KUSAYANAGI TOMOE; TSUKUDA SENKO; SHIMURA SATOMI; MANITA DAISUKE; IWAKIRI KANAKO; KAMISUKI SHINJI; TAKAKUSAGI YOICHI; TAKEUCHI TOSHIFUMI; KURAMOCHI KOUJI; NAKAZAKI ATSUO; SAKAGUCHI KENGO; KOBAYASHI SUSUMU; SUGAWARA FUMIO,期刊：Bioorganic & Medicinal Chemistry, 页码：6248-6255 , 文章类型： Article，,卷期：2012年20-21] Doxorubicin, a commonly used cancer chemotherapy agent, elicits several potent biological effects, including synergistic-antitumor activity in combination with cisplatin. However, the mechanism of this synergism remains ... Synthesis of 1,5-diarylhaloimidazole analogs and their inhibitory activities against PGE(2) production from LPS-treated RAW 264.7 cells [作者：YANG ZUNHUA; TRUONG TUYEN N; PHAM TUANANH N; LEE JAEWON; KIM SUNGSOO; PARK HAEIL,期刊：Bioorganic & Medicinal Chemistry, 页码：6256-6259 , 文章类型： Article，,卷期：2012年20-21] A number of 1,5-diarylimidazole analogs were synthesized and evaluated their inhibitory activities of cyclooxygenase-2 catalyzed prostaglandin E-2 production. Reactions of 1,5-diarylimidazoles with halogenating reagents ... Development and characterization of endocannabinoid hydrolases FAAH and MAGL inhibitors bearing a benzotriazol-1-yl carboxamide scaffold [作者：MORERA LUDOVICA; LABAR GEOFFRAY; ORTAR GIORGIO; LAMBERT DIDIER M,期刊：Bioorganic & Medicinal Chemistry, 页码：6260-6275 , 文章类型： Article，,卷期：2012年20-21] A series of (1H-benzo[d][1,2,3]triazol-1-yl)(4-benzylpiperazin-1-yl)methanones and of (1H-benzo[d] [1,2,3]triazol-1-yl)(4-phenylpiperazin-1-yl)methanones has been prepared and tested on human fatty acid amide hydrolase (... Conformational analysis of two novel cytotoxic C2-substituted pyrrolo[2,3-f]quinolines in aqueous media, organic solvents, membrane bilayers and at the putative active site [作者：VARVARIGOU NICOLE; MEGARIOTIS GRIGORIOS; LEONIS GEORGIOS; VRONTAKI ELENI; MANIATI ANTIGONIMARGARITA; VLACHOU MARILENA; EIKOSIPENTAKI APHRODITE; KOMPOGENNITAKI RODANTHI; PAPADOPOULOS MANTHOS G; GRDADOLNIK SIMONA GOLIC; KOMIOTIS DIMITRI; MAVROMOUSTAKOS THOMAS; TSOTINIS ANDREW,期刊：Bioorganic & Medicinal Chemistry, 页码：6276-6284 , 文章类型： Article，,卷期：2012年20-21] We have performed: (i) conformational analysis of two novel cytotoxic C2-substituted pyrrolo[2,3-f]quinolines Se and 5g in deuterated dimethylsulfoxide (DMSO-d(6)) utilizing NOE results from NMR spectroscopy; (ii) molecu... Synthesis and biological evaluation of a series of podophyllotoxins derivatives as a class of potent antitubulin agents [作者：LIU YINGQIAN; WEI DONGFENG; ZHAO YONGLONG; CHENG WEIDONG; LU YAN; MA YAQIONG; LI XIN; HAN CHAO; WEI YANXIA; CAO HUIMING; ZHAO CHUNYAN,期刊：Bioorganic & Medicinal Chemistry, 页码：6285-6295 , 文章类型： Article，,卷期：2012年20-21] A series of eight novel podophyllotoxin derivatives were designed, synthesized and evaluated for biological activities. The antiproliferative activities were tested against a panel of human cancer cell lines (1(562, SGC,... Pyrido[1,2-a]pyrimidin-4-ones as antiplasmodial falcipain-2 inhibitors [作者：MANE U R; LI H; HUANG J; GUPTA R C; NADKARNI S S; GIRIDHAR R; NAIK P P; YADAV M R,期刊：Bioorganic & Medicinal Chemistry, 页码：6296-6304 , 文章类型： Article，,卷期：2012年20-21] Plasmodium falciparum cysteine protease falcipain-2 (FP-2) is a promising target for antimalarial chemotherapy and inhibition of this protease affects the growth of parasite adversely. A series of pyrido[1,2-a]pyrimidin-... Synthesis of imidacloprid derivatives with a chiral alkylated imidazolidine ring and evaluation of their insecticidal activity and affinity to the nicotinic acetylcholine receptor [作者：NISHIWAKI HISASHI; KURIYAMA MITUHIRO; NAGAOKA HIKARU; KATO AKIRA; AKAMATSU MIKI; YAMAUCHI SATOSHI; SHUTO YOSHIHIRO,期刊：Bioorganic & Medicinal Chemistry, 页码：6305-6312 , 文章类型： Article，,卷期：2012年20-21] A series of imidacloprid (IMI) derivatives with an alkylated imidazolidine ring were asymmetrically synthesized to evaluate their insecticidal activity against adult female housefly, Musca domestica, and affinity to the ... Lead optimization studies towards the discovery of novel carbamates as potent AChE inhibitors for the potential treatment of Alzheimer's disease [作者：ROY KULDEEP K; TOTA SANTOSHKUMAR; TRIPATHI TUSHA; CHANDER SUBHASH; NATH CHANDISHWAR; SAXENA ANIL K,期刊：Bioorganic & Medicinal Chemistry, 页码：6313-6320 , 文章类型： Article，,卷期：2012年20-21] The optimization of our previous lead compound 1 (AChE IC50 = 3.31 mu M) through synthesis and pharmacology of a series of novel carbamates is reported. The synthesized compounds were evaluated against mouse brain AChE e... Role of the side chain stereochemistry in the alpha-glucosidase inhibitory activity of kotalanol, a potent natural alpha-glucosidase inhibitor. Part 2 [作者：TANABE GENZOH; MATSUOKA KANJYUN; YOSHINAGA MASAHIRO; XIE WEIJIA; TSUTSUI NOZOMI; AMER MUMEN F A; NAKAMURA SHINYA; NAKANISHI ISAO; WU XIAOMING; YOSHIKAWA MASAYUKI; MURAOKA OSAMU,期刊：Bioorganic & Medicinal Chemistry, 页码：6321-6334 , 文章类型： Article，,卷期：2012年20-21] To examine the role of the side chain of kotalanol (2), a potent natural alpha-glucosidase inhibitor isolated from Salacia reticulata, on inhibitory activity, four diastereomers (11a-11d) with reversed configuration (S) ... Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives [作者：VARAMINI PEGAH; HUSSEIN WALEED M; MANSFELD FRIEDERIKE M; TOTH ISTVAN,期刊：Bioorganic & Medicinal Chemistry, 页码：6335-6343 , 文章类型： Article，,卷期：2012年20-21] Endomorphins have been shown to produce potent analgesia in various rodent models of pain. However, their central administration led to the development of tolerance and physical dependence. Conjugation of C-terminal subs... A novel spirocyclic tropanyl-Delta(2)-isoxazoline derivative enhances citalopram and paroxetine binding to serotonin transporters as well as serotonin uptake [作者：DALLANOCE CLELIA; CANOVI MARA; MATERA CARLO; MENNINI TIZIANA; DE AMICI MARCO; GOBBI MARCO; DE MICHELI CARLO,期刊：Bioorganic & Medicinal Chemistry, 页码：6344-6355 , 文章类型： Article，,卷期：2012年20-21] A group of spirocyclic tropanyl-Delta(2)-isoxazolines was synthesized exploiting the 1,3-dipolar cycloaddition of nitrite oxides to olefins. Their interaction with the dopamine and serotonin transporters (DAT and SERT, r... Design, synthesis and biological evaluation of heterocyclic azoles derivatives containing pyrazine moiety as potential telomerase inhibitors [作者：ZHANG YANBIN; WANG XIAOLIANG; LIU WEN; YANG YUSHUN; TANG JIANFENG; ZHU HAILIANG,期刊：Bioorganic & Medicinal Chemistry, 页码：6356-6365 , 文章类型： Article，,卷期：2012年20-21] Three series of novel heterocyclic azoles derivatives containing pyrazine (5a-5k, 8a-8k and ha-ilk) have been designed, synthesized, structurally determined, and their biological activities were evaluated as potential te... Identification of a 2-phenyl-substituted octahydrobenzo[f]quinoline as a dopamine D-3 receptor-selective full agonist ligand [作者：CLARK ALIA H; MCCORVY JOHN D; CONLEY JASON M; WILLIAMS WHITNEY K; BEKKAM MARKONDAIAH; WATTS VAL J; NICHOLS DAVID E,期刊：Bioorganic & Medicinal Chemistry, 页码：6366-6374 , 文章类型： Article，,卷期：2012年20-21] This work describes the identification of a novel class of octahydrobenzo[f]quinolines as dopamine D-3-selective full agonists. We developed a facile method that utilizes Suzuki coupling for easy incorporations of variou... Design, synthesis and in vitro evaluation of a series of alpha-substituted phenylpropanoic acid PPAR gamma agonists to further investigate the stereochemistry-activity relationship [作者：OHASHI MASAO; NAKAGOME IZUMI; KASUGA JUNICHI; NOBUSADA HIROMI; MATSUNO KENJI; MAKISHIMA MAKOTO; HIRONO SHUICHI; HASHIMOTO YUICHI; MIYACHI HIROYUKI,期刊：Bioorganic & Medicinal Chemistry, 页码：6375-6383 , 文章类型： Article，,卷期：2012年20-21] We previously demonstrated that the alpha-benzylphenylpropanoic-benzylphenylpropanoic acid-type PPAR gamma-selective agonist 6 exhibited a reversed stereochemistry-activity relationship, that is, the (R)-enantiomer is a ...