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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61条记录   Highly potent and selective chiral inhibitors of PDE5: An illustration of Pfeiffer's rule [作者：Bunnage, ME; Mathias, JP; Wood, A; Miller, D; Street, SDA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6033-6036 , 文章类型： Article，,卷期：2008年18-23] A series of potent chiral PDE5 inhibitors are described that are based on the sildenafil architecture but exhibit much greater selectivity over PDE6. Eudismic analysis of the SAR in this series provided a clear illustrat... Rotational deviation of 3-acetyl group from cyclic tetrapyrrole pi-plane in synthetic bacteriochlorophyll-a analogs by 20-substitution [作者：Tamiaki, H; Kotegawa, Y; Mizutani, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6037-6040 , 文章类型： Article，,卷期：2008年18-23] The 3-acetyl groups of synthetic methyl pyropheophorbides were rotated around the 3-3(1) bond and the rotational conformers were obtained in a dichloromethane solution of 20-bromo- and methyl-substituted compounds, based... Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H-3 receptor inverse agonists [作者：Mizutani, T; Nagase, T; Ito, S; Miyamoto, Y; Tanaka, T; Takenaga, N; Tokita, S; Sato, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6041-6045 , 文章类型： Article，,卷期：2008年18-23] Novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives were identified as potent human H-3 receptor inverse agonists. After systematic modi. cation of lead 5a, the potent and selective analog 5r was identified. ... Pterocarpans and flavanones from Sophora flavescens displaying potent neuraminidase inhibition [作者：Ryu, YB; Curtis-Long, MJ; Kim, JH; Jeong, SH; Yang, MS; Lee, KW; Lee, WS; Park, KH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6046-6049 , 文章类型： Article，,卷期：2008年18-23] Pterocarpans (1-3) and flavanones (4-10) were isolated from Sophora flavescens and screened for their ability to inhibit neuraminidase (an enzyme crucial in the proliferation of the influenza virus). The majority of inhi... Pyrrospirones A and B, apoptosis inducers in HL-60 cells, from an endophytic fungus, Neonectria ramulariae Wollenw KS-246 [作者：Shiono, Y; Shimanuki, K; Hiramatsu, F; Koseki, T; Tetsuya, M; Fujisawa, N; Kimura, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6050-6053 , 文章类型： Article，,卷期：2008年18-23] Pyrrospirones A and B have been isolated from unpolished rice cultures of the endophytic fungus Neonectria ramulariae Wollenw KS-246. Their absolute stereostructures (1 and 2) were elucidated through spectroscopic method... Synthesis and preliminary pharmacological evaluation of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides as novel atypical antipsychotic agents [作者：Sekhar, KVGC; Rao, VS; Vyas, DRK; Kumar, MMK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6054-6057 , 文章类型： Article，,卷期：2008年18-23] A series of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides were synthesized in an effort to prepare novel atypical antipsychotic agents. The compounds were synthesized by either microwave irr... Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors [作者：Bannwart, LM; Carter, DS; Cai, HY; Choy, JC; Greenhouse, R; Jaime-Figueroa, S; Iyer, PS; Lin, CJ; Lee, EK; Lucas, MC; Lynch, SM; Madera, AM; Moore, A; Ozboya, K; Raptova, L; Roetz, R; Schoenfeld, RC; Stein, KA; Steiner, S; Villa, M; Weikert, RJ; Zhai, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6062-6066 , 文章类型： Article，,卷期：2008年18-23] A series of 3,3-disubstituted pyrrolidine monoamine triple reuptake inhibitors were discovered. Analogues with low nanomolar potency, good human in vitro microsomal stability and in vitro permeability, and low drug-drug ... Synthesis and characterization of novel natural product-Gd(III) MRI contrast agent conjugates [作者：Efthimiadou, EK; Katsarou, ME; Fardis, M; Zikos, C; Pitsinos, EN; Kazantzis, A; Leondiadis, L; Sagnou, M; Vourloumis, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6058-6061 , 文章类型： Article，,卷期：2008年18-23] Several novel gadolinium chelates conjugated with paclitaxel, colchicine and thyroxine have been prepared as MRI contrast agents targeted to tubulin and thyroxine-binding globulin, respectively. (C) 2008 Elsevier Ltd. Al... Synthesis and activity of novel 1-or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors [作者：Zhang, PW; Terefenko, EA; McComas, CC; Mahaney, PE; Vu, A; Trybulski, E; Koury, E; Johnston, G; Bray, J; Deecher, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6067-6070 , 文章类型： Article，,卷期：2008年18-23] A series of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors was discovered. Several compounds such as 15 and 20 showed good hNET potency. Compoun... Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): Structure-activity relationships and strategies for the elimination of reactive metabolite formation [作者：Walker, DP; Bi, FC; Kalgutkar, AS; Bauman, JN; Zhao, SX; Soglia, JR; Aspnes, GE; Kung, DW; Klug-McLeod, J; Zawistoski, MP; McGlynn, MA; Oliver, R; Dunn, M; Li, JC; Richter, DT; Cooper, BA; Kath, JC; Hulford, CA; Autry, CL; Luzzio, MJ; Ung, EJ; Roberts, WG; Bonnette, PC; Buckbinder, L; Mistry, A; Griffor, MC; Han, S; Guzman-Perez, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6071-6077 , 文章类型： Article，,卷期：2008年18-23] The synthesis and SAR for a series of diaminopyrimidines as PYK2 inhibitors are described. Using a combination of library and traditional medicinal chemistry techniques, a FAK-selective chemical series was transformed in... Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors [作者：Scarpelli, R; Di Marco, A; Ferrigno, F; Laufer, R; Marcucci, I; Muraglia, E; Ontoria, JM; Rowley, M; Serafini, S; Steinkuhler, C; Jones, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6078-6082 , 文章类型： Article，,卷期：2008年18-23] 5-(Trifluoroacetyl)thiophene-2-carboxamides were found to be potent and selective class II HDAC inhibitors. This paper describes their further development and the investigation on the cause for the lack of cell-based act... 2-Aminobenzimidazoles as potent ITK antagonists: trans-stilbene-like moieties targeting the kinase specificity pocket [作者：Lo, HY; Bentzien, J; Fleck, RW; Pullen, SS; Khine, HH; Woska, JR; Kugler, SZ; Kashem, MA; Takahashi, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6218-6221 , 文章类型： Article，,卷期：2008年18-23] Based on the information from molecular modeling and X-ray crystal structures, the kinase specificity pocket of ITK could be occupied upon extension of the right-hand-side of the 2-benzimidazole core of the inhibitors. 2... Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists [作者：Morales-Ramos, AI; Mecom, JS; Kiesow, TJ; Graybill, TL; Brown, GD; Aiyar, NV; Davenport, EA; Kallal, LA; Knapp-Reed, BA; Li, P; Londregan, AT; Morrow, DM; Senadhi, S; Thalji, RK; Zhao, S; Burns-Kurtis, CL; Marino, JP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6222-6226 , 文章类型： Article，,卷期：2008年18-23] High-throughput screening of the GSK compound collection against the P2Y1 receptor identified a novel series of tetrahydro-4-quinolinamine antagonists. Optimal substitution around the piperidine group was pivotal for ens... Synthetic chalcones as efficient inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatase PtpA [作者：Chiaradia, LD; Mascarello, A; Purificacao, M; Vernal, J; Cordeiro, MNS; Zenteno, ME; Villarino, A; Nunes, RJ; Yunes, RA; Terenzi, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6227-6230 , 文章类型： Article，,卷期：2008年18-23] In the search for lead compounds for new drugs for tuberculosis, the activity of 38 synthetic chalcones were assayed for their potential inhibitory action towards a protein tyrosine phosphatase from Mycobacterium tubercu... Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK) [作者：Farmer, LJ; Bemis, G; Britt, SD; Cochran, J; Connors, M; Harrington, EM; Hoock, T; Markland, W; Nanthakumar, S; Taslimi, P; Ter Haar, E; Wang, J; Zhaveri, D; Salituro, FG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6231-6235 , 文章类型： Article，,卷期：2008年18-23] A series of SYK inhibitors based on the phenylamino pyrimidine thiazole lead 4 were prepared and evaluated for biological activity. Lead optimization provided compounds with nanomolar K-i's against SYK and potent inhibit... Modifications of the isonipecotic acid fragment of SNS-032: Analogs with improved permeability and lower efflux ratio [作者：Fan, JF; Fahr, B; Stockett, D; Chan, E; Cheeti, S; Serafimova, I; Lu, YF; Pham, P; Walker, DH; Hoch, U; Choong, IC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6236-6239 , 文章类型： Article，,卷期：2008年18-23] Modifications of the isonipecotic acid fragment of SNS-032 results in analogs which are more permeable and lower effluxed than SNS-032. The enantiomerically pure synthesis and the in vivo pro. le of analog 20 is describe...