个性化文献订阅>文章检索

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81条记录   Identification of chemicals to inhibit the kinase activity of leucine-rich repeat kinase 2 (LRRK2), a Parkinson's disease-associated protein [作者：Yun, H; Heo, HY; Kim, HH; DooKim, N; Seol, W,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2953-2957 , 文章类型： Article，,卷期：2011年21-10] Parkinson's disease (PD) is a late-onset neurodegenerative disease which occurs at more than 1% in populations aging 65-years and over. Recently, leucine-rich repeat kinase 2 (LRRK2) has been identified as a causative ge... In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors [作者：Wang, T; Ioannidis, S; Almeida, L; Block, MH; Davies, AM; Lamb, ML; Scott, DA; Su, M; Zhang, HJ; Alimzhanov, M; Bebernitz, G; Bell, K; Zinda, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2958-2961 , 文章类型： Article，,卷期：2011年21-10] Synthesis and biological evaluation of a series of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors was reported. Biochemical screening, followed by profile optimization, resulted in JAK2 inhibitors ex... Synthesis and evaluation of novel N-fluoropyridyl derivatives of tropane as potential PET imaging agents for the dopamine transporter [作者：Liu, JY; Zhu, L; Plossl, K; Lieberman, BP; Kung, HF,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2962-2965 , 文章类型： Article，,卷期：2011年21-10] A series of novel N-fluoropyridyl-containing tropane derivatives were synthesized and their binding affinities for the dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine (NET) were determined via... 2-Arylimidazo[2,1-b]benzothiazoles: A new family of amyloid binding agents with potential for PET and SPECT imaging of Alzheimer's brain [作者：Alagille, D; DaCosta, H; Baldwin, RM; Tamagnan, GD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2966-2968 , 文章类型： Article，,卷期：2011年21-10] We designed and synthesized a small series of 2-aryl-imidazo[2,1-b]benzothiazole, representing a combination of motifs from the two most potent amyloid imaging agents, PIB and IMPY. The binding affinity of the new compou... NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor [作者：Beria, I; Bossi, RT; Brasca, MG; Caruso, M; Ceccarelli, W; Fachin, G; Fasolini, M; Forte, B; Fiorentini, F; Pesenti, E; Pezzetta, D; Posteri, H; Scolaro, A; Depaolini, SR; Valsasina, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2969-2974 , 文章类型： Article，,卷期：2011年21-10] As part of our drug discovery effort, we identified and developed 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as PLK1 inhibitors. We now report the optimization of this class that led to the identification of N... Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII [作者：Rami, M; Maresca, A; Smaine, FZ; Montero, JL; Scozzafava, A; Winum, JY; Supuran, CT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2975-2979 , 文章类型： Article，,卷期：2011年21-10] A new series of sulfonamides was synthesized by the reaction of the boroxazolidone complex of L-lysine with isothiocyanates incorporating sulfamoyl moieties and diverse organic scaffolds. The obtained thioureas have been... Diaryl urea analogues of SB-334867 as orexin-1 receptor antagonists [作者：Perrey, DA; Gilmour, BP; Runyon, SP; Thomas, BF; Zhang, YN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2980-2985 , 文章类型： Article，,卷期：2011年21-10] As a part of our program to develop OX1-CB1 bivalent ligands, we required a better understanding of the basic structure-activity relationships (SARs) of orexin antagonists. A series of SB-334867 analogues were synthesize... Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors [作者：Zhao, XZ; Maddali, K; Metifiot, M; Smith, SJ; Vu, BC; Marchand, C; Hughes, SH; Pommier, Y; Burke, TR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2986-2990 , 文章类型： Article，,卷期：2011年21-10] New tricyclic HIV-1 integrase (IN) inhibitors were prepared that combined structural features of bicyclic pyrimidinones with recently disclosed 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones. This combination resulted in the ... Discovery of small molecule human FPR1 receptor antagonists [作者：Unitt, J; Fagura, M; Phillips, T; King, S; Perry, M; Morley, A; MacDonald, C; Weaver, R; Christie, J; Barber, S; Mohammed, R; Paul, M; Cook, A; Baxter, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2991-2997 , 文章类型： Article，,卷期：2011年21-10] The identification of two novel series of formyl peptide receptor 1 (FPR1) antagonists are reported, represented by methionine benzimidazole 6 and diamide 7. Both series specifically inhibited the binding of labelled fML... Radiosynthesis and preliminary evaluation of 4-[F-18]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1 [作者：Yamasaki, T; Fujinaga, M; Yoshida, Y; Kumata, K; Yui, JJ; Kawamura, K; Hatori, A; Fukumura, T; Zhang, MR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2998-3001 , 文章类型： Article，,卷期：2011年21-10] The purpose of this study was to develop 4-[F-18]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide ([F-18]FITM, [F-18]4) as a new PET ligand for imaging metabotropic glutamate receptor su... Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors [作者：Kim, S; Jung, JK; Lee, HS; Kim, Y; Kim, J; Choi, K; Baek, DJ; Moon, B; Oh, KS; Lee, BH; Shin, KJ; Pae, AN; Nam, G; Roh, EJ; Cho, YS; Choo, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3002-3006 , 文章类型： Article，,卷期：2011年21-10] A serine-threonine kinase IKK-2 plays an important role in activation of NF-kappa B through phosphorylation of the inhibitor of NF-kappa B (I kappa B). As NF-kappa B is a major transcription factor that regulates genes r... Synthesis and evaluation of quinoxaline derivatives as potential influenza NS1A protein inhibitors [作者：You, L; Cho, EJ; Leavitt, J; Ma, LC; Montelione, GT; Anslyn, EV; Krug, RM; Ellington, A; Robertus, JD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3007-3011 , 文章类型： Article，,卷期：2011年21-10] A library of quinoxaline derivatives were prepared to target non-structural protein 1 of influenza A (NS1A) as a means to develop anti-influenza drug leads. An in vitro fluorescence polarization assay demonstrated that t... A green expedient synthesis of pyridopyrimidine-2-thiones and their antitubercular activity [作者：Rajesh, SM; Kumar, RS; Libertsen, LA; Perumal, S; Yogeeswari, P; Sriram, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3012-3016 , 文章类型： Article，,卷期：2011年21-10] The pseudo four-component domino reactions of N-substituted-4-piperidones, substituted aromatic aldehydes and thiourea in the presence of solid sodium ethoxide under solvent-free conditions afforded pyridopyrimidine-2-th... Synthesis and in vitro cytotoxic evaluation of N-alkylbromo and N-alkylphthalimido-isatins [作者：Singh, P; Kaur, S; Kumar, V; Bedi, PMS; Mahajan, MP; Sehar, I; Pal, HC; Saxena, AK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3017-3020 , 文章类型： Article，,卷期：2011年21-10] The manuscript pertains to the synthesis and in vitro cytotoxic evaluation of a series of N-alkylbromo and N-alkylphthalimido-isatins against four different human cancer cell lines namely Colon: HCT-15; Liver: Hep-2; Lun... Structure and characteristics of reassembled fluorescent protein, a new insight into the reassembly mechanisms [作者：Isogai, M; Kawamoto, Y; Inahata, K; Fukada, H; Sugimoto, K; Tada, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3021-3024 , 文章类型： Article，,卷期：2011年21-10] Bimolecular fluorescence complementation (BiFC) assay has been used widely to visualize protein-protein interactions in cells. However, there is a problem that fluorescent protein fragments have an ability to associate w... Novel 3-chlorooxazolidin-2-ones as antimicrobial agents [作者：Shiau, TP; Turtle, ED; Francavilla, C; Alvarez, NJ; Zuck, M; Friedman, L; O'Mahony, DJR; Low, E; Anderson, MB; Najafi, R; Jain, RK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3025-3028 , 文章类型： Article，,卷期：2011年21-10] Antimicrobial resistance against many known therapeutics is on the rise. We examined derivatives of 3-chlorooxazolidin-2-one 1a (X = H) as antibacterial and antifungal agents. The key findings were that the activity and ...