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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85条记录   Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists [作者：McIntyre, CJ; McCauley, JA; Bednar, B; Bednar, RA; Butcher, JW; Claremon, DA; Cunningham, ME; Freidinger, RM; Gaul, SL; Homnick, CF; Koblan, KS; Mosser, SD; Romano, JJ; Liverton, NJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5132-5135 , 文章类型： Article，,卷期：2009年19-17] A novel series of annulated tricyclic compounds was synthesized and evaluated as NMDA/NR2B antagonists. Structure-activity development was directed towards in vitro optimization of NR2B activity and selectivity over the ... Inhibitors of HIV-1 attachment. Part 3: A preliminary survey of the effect of structural variation of the benzamide moiety on antiviral activity [作者：Meanwell, NA; Wallace, OB; Wang, H; Deshpande, M; Pearce, BC; Trehan, A; Yeung, KS; Qiu, ZL; Wright, JJK; Robinson, BA; Gong, YF; Wang, HGH; Blair, WS; Shi, PY; Lin, PF,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5136-5139 , 文章类型： Article，,卷期：2009年19-17] 1-(4-Benzoylpiperazin-1-yl)-2-(1H-indol-3-yl) ethane-1,2-dione (1a) has been characterized as an inhibitor of HIV-1 attachment that interferes with the interaction of viral gp120 with the host cell receptor CD4. In previ... Inhibitors of HIV-1 attachment. Part 4: A study of the effect of piperazine substitution patterns on antiviral potency in the context of indole-based derivatives [作者：Wang, T; Kadow, JF; Zhang, ZX; Yin, ZW; Gao, Q; Wu, DD; Parker, DD; Yang, Z; Zadjura, L; Robinson, BA; Gong, YF; Blair, WS; Shi, PY; Yamanaka, G; Lin, PF; Meanwell, NA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5140-5145 , 文章类型： Article，,卷期：2009年19-17] 4-Fluoro- and 4-methoxy-1-(4-benzoylpiperazin-1-yl)-2-(1H-indol-3-yl) ethane-1,2-dione (2 and 3, respectively) have been characterized as potent inhibitors of HIV-1 attachment that interfere with the interaction of viral... Synthesis of chiral fluorine-tagged reference standards for the F-19 NMR-based stereochemical analysis of sulfoxides at trace analytical levels [作者：Tremblay, AE; Lao, KYY; Hodgson, DJ; Dawson, B; Buist, PH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5146-5150 , 文章类型： Article，,卷期：2009年19-17] Chiral fluorine-tagged sulfoxides of known absolute configuration have been synthesized. These compounds are required as reference standards to validate a F-19 NMR-based micromethod for the stereochemical analysis of bio... Towards to hENT(1)-nucleoside transporter selective imaging agents. Synthesis and in vitro evaluation of the radiolabeled SAENTA analogues [作者：Zlatopolskiy, BD; Morgenroth, A; Urusova, EA; Dinger, C; Kull, T; Pape, M; Glatting, G; Reske, SN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5151-5154 , 文章类型： Article，,卷期：2009年19-17] Three new potential hENT(1) inhibitors suitable for labeling with PET/SPECT radioisotopes were prepared from an advanced intermediate 4. They were tested for their capability to inhibit binding of SAENTA-fluorescein to H... Inhibitory effect of chalcones and their derivatives from Glycyrrhiza inflata on protein tyrosine phosphatase 1B [作者：Yoon, G; Lee, W; Kim, SN; Cheon, SH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5155-5157 , 文章类型： Article，,卷期：2009年19-17] Compounds (1-6) isolated from the CH2Cl2 extract of Glycyrrhiza inflata and semisynthetic licochalcone A derivatives (7-14) were evaluated for their protein tyrosine phosphatase 1B (PTP1B) inhibitory activities. Licochal... 2-Aminobenzimidazoles as potent Aurora kinase inhibitors [作者：Zhong, M; Bui, M; Shen, W; Baskaran, S; Allen, DA; Elling, RA; Flanagan, WM; Fung, AD; Hanan, EJ; Harris, SO; Heumann, SA; Hoch, U; Ivy, SN; Jacobs, JW; Lam, S; Lee, H; McDowell, RS; Oslob, JD; Purkey, HE; Romanowski, MJ; Silverman, JA; Tangonan, BT; Taverna, P; Yang, WJ; Yoburn, JC; Yu, CH; Zimmerman, KM; O'Brien, T; Lew, W,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5158-5161 , 文章类型： Article，,卷期：2009年19-17] This Letter describes the discovery and key structure-activity relationship (SAR) of a series of 2-aminobenzimidazoles as potent Aurora kinase inhibitors. 2-Aminobenzimidazole serves as a bioisostere of the biaryl urea r... Metallo-beta-lactamase inhibitory activity of phthalic acid derivatives [作者：Hiraiwa, Y; Morinaka, A; Fukushima, T; Kudo, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5162-5165 , 文章类型： Article，,卷期：2009年19-17] 4-Butyl-3-methylphthalic acid was recognized as a metallo-beta-lactamase inhibitor. The structure-activity relationship study of substituted phthalic acids afforded 3-phenylphthalic acid derivatives as potent IMP-1 inhib... Synthesis of biotinylated OSW-1 [作者：Kang, Y; Lou, CG; Ahmed, KBR; Huang, P; Jin, ZD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5166-5168 , 文章类型： Article，,卷期：2009年19-17] OSW-1 is a highly potent anticancer natural saponin with an unknown mode of action. To determine its cellular target(s) biotinylated OSW-1 was successfully synthesized in nine steps. (C) 2009 Elsevier Ltd. All rights res... Parallel synthesis of chiral pentaamines and pyrrolidine containing bis-heterocyclic libraries. Multiple scaffolds with multiple building blocks: A double diversity for the identification of new antitubercular compounds [作者：Nefzi, A; Appel, J; Arutyunyan, S; Houghten, RA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5169-5175 , 文章类型： Article，,卷期：2009年19-17] Combinatorial chemistry offers a unique opportunity for the synthesis and screening of large numbers of compounds and significantly enhances the prospect of finding new drugs. Collaborative efforts with the Tuberculosis ... Semi-rigid tripeptide agonists of melanocortin receptors [作者：Ruwe, AR; Koikov, L; Abdel-Malek, Z; Haskell-Luevano, C; Dirain, ML; Portillo, F; Xiang, ZM; Wortman, M; Knittel, JJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5176-5181 , 文章类型： Article，,卷期：2009年19-17] A series of 30 RCO-HfR-NH2 derivatives show preference for the mouse MC1R vs MC3-5Rs. trans-4-HOC6H4CH=CHCO-HfR-NH2 (13) [EC50 (nM): MC1R 83, MC3R 20500, MC4R 18130 and MC5R 935; ratio 1: 246: 217: 11] is 11 times more p... Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors [作者：Patel, HK; Grotzfeld, RM; Lai, AG; Mehta, SA; Milanov, ZV; Chao, Q; Sprankle, KG; Carter, TA; Velasco, AM; Fabian, MA; James, J; Treiber, DK; Lockhart, DJ; Zarrinkar, PP; Bhagwat, SS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5182-5185 , 文章类型： Article，,卷期：2009年19-17] A series of diaryl ureas with an amide substitution at the 4-position was prepared and found to be potent and selective FLT3 inhibitors with good oral bioavailability and efficacy in a tumor xenograft model. (C) 2009 Els... Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists [作者：Ando, M; Sekino, E; Haga, Y; Moriya, M; Ito, M; Ito, J; Iwaasa, H; Ishihara, A; Kanatani, A; Ohtake, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5186-5190 , 文章类型： Article，,卷期：2009年19-17] Novel phenethylpyridone derivatives were identified as potent human melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. A search for surrogates for the 4-(2-aminoethoxy) phenyl moiety of 1 resulted in discover... 4-(Benzimidazol-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: Potent and selective p70S6 kinase inhibitors [作者：Bandarage, U; Hare, B; Parsons, J; Pham, L; Marhefka, C; Bemis, G; Tang, Q; Moody, CS; Rodems, S; Shah, S; Adams, C; Bravo, J; Charonnet, E; Savic, V; Come, JH; Green, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5191-5194 , 文章类型： Article，,卷期：2009年19-17] We report herein the design and synthesis of 4-(benzimidazol-2-yl)-1,2,5-oxadiazol-3-amine derivatives as inhibitors of p70S6 kinase. Screening hits containing the 4-(benzimidazol-2-yl)-1,2,5-oxadiazol-3-ylamine scaffold... Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists [作者：Du, W; Jewell, JP; Lin, LS; Colandrea, VJ; Xiao, JC; Lao, J; Shen, CP; Bateman, TJ; Reddy, VBG; Ha, SN; Shah, SK; Fong, TM; Hale, JJ; Hagmann, WK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5195-5199 , 文章类型： Article，,卷期：2009年19-17] Obesity is a chronic medical condition that is affecting large population throughout the world. CB1 as a target for treatment of obesity has been under intensive studies. Taranabant was discovered and then developed by M... Imidazo-pyrazine derivatives as potent CXCR3 antagonists [作者：Du, XH; Gustin, DJ; Chen, XQ; Duquette, J; Mcgee, LR; Wang, ZL; Ebsworth, K; Henne, K; Lemon, B; Ma, J; Miao, S; Sabalan, E; Sullivan, TJ; Tonn, G; Collins, TL; Medina, JC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5200-5204 , 文章类型： Article，,卷期：2009年19-17] A general way of improving the potency of CXCR3 antagonists with fused hetero-bicyclic cores was identified. Optimization efforts led to the discovery of a series of imidazo-pyrazine derivatives with improved pharmacokin...