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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56条记录   Human kallikrein 6 inhibitors with a para-amidobenzylanmine P1 group identified through virtual screening [作者：Liang, GY; Chen, X; Aldous, S; Pu, SF; Mehdi, S; Powers, E; Xia, TH; Wang, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2450-2455 , 文章类型： Article，,卷期：2012年22-7] A series of hK6 inhibitors with a para-amidobenzylamine P1 group and a 2-hydroxybenzamide scaffold linker was discovered through virtual screening. The X-ray structure of hK6 complexed with compound 9b was determined to ... Discovery of thiadiazole amides as potent, S1P(3)-sparing agonists of sphingosine-1-phosphate 1 (S1P(1)) receptor [作者：Xu, H; Zhang, HB; Luan, LB; Xu, Y; Li, CY; Wang, YH; Han, FB; Yang, T; Ren, F; Xiang, JN; Elliott, JD; Zhao, YG; Guo, TB; Lu, HT; Zhang, W; Hirst, D; Lindon, M; Lin, XC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2456-2459 , 文章类型： Article，,卷期：2012年22-7] High-throughput screening of GSK compound collection led to the discovery of a novel series of thiadiazole amides as potent and S1P(3)-sparing sphingosine-1-phosphate 1 (S1P(1)) receptor agonists. Synthesis, structure an... Iodine-catalyzed condensation of isatin with indoles: A facile synthesis of di(indolyl)indolin-2-ones and evaluation of their cytotoxicity [作者：Reddy, BVS; Rajeswari, N; Sarangapani, M; Prashanthi, Y; Ganji, RJ; Addlagatta, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2460-2463 , 文章类型： Article，,卷期：2012年22-7] Isatin reacts smoothly with indoles in the presence of a catalytic amount of molecular iodine under mild conditions to afford a novel class of di(indolyl)indolin-2-one derivatives in good yields. These molecules are foun... An example of designed multiple ligands spanning protein classes: Dual MCH-1R antagonists/DPPIV inhibitors [作者：Gattrell, WT; Smith, CPS; Smith, AJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2464-2469 , 文章类型： Article，,卷期：2012年22-7] A ligand-based approach to identify potential starting points for a dual MCH-1R antagonist/DPPIV inhibitor medicinal chemistry program was undertaken. Potential ligand pairs were identified by analysis of MCH-1R and DPPI... Synthesis and properties of cationic 2 '-O-[N-(4-aminobutyl)carbamoyl] modified oligonucleotides [作者：Seio, K; Tokugawa, M; Kanamori, T; Tsunoda, H; Ohkubo, A; Sekine, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2470-2473 , 文章类型： Article，,卷期：2012年22-7] 2'-O-[N-(4-Aminobutylcarbamoyl)]uridine (U-abcm) was synthesized and incorporated into oligonucleotides. The oligonucleotides incorporating U-abcm formed more stable duplexes with their complementary and mismatched RNAs ... Scaffold hybridization in generation of indenoindolones as anticancer agents that induce apoptosis with cell cycle arrest at G2/M phase [作者：Kashyap, M; Das, D; Preet, R; Mohapatra, P; Satapathy, SR; Siddharth, S; Kundu, CN; Guchhait, SK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2474-2479 , 文章类型： Article，,卷期：2012年22-7] Scaffold hybridization of several natural and synthetic anticancer leads led to the consideration of indenoindolones as potential novel anticancer agents. A series of these compounds were prepared by a diversity-feasible... Design and synthesis of 4-alkynyl pyrazoles as inhibitors of PDE4: A practical access via Pd/C-Cu catalysis [作者：Gorja, DR; Kumar, KS; Kandale, A; Meda, CLT; Parsa, KVL; Mukkanti, K; Pal, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2480-2487 , 文章类型： Article，,卷期：2012年22-7] The design and synthesis of 4-alkynyl pyrazole derivatives has led to the identification of new class of PDE4 inhibitors. All these compounds were accessed for the first time via a facile Pd/C-CuI-PPh3 mediated C-C bond ... Synthesis and evaluation of ursolic acid derivatives as potent cytotoxic agents [作者：Bai, KK; Yu, Z; Chen, FL; Li, F; Li, WY; Guo, YH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2488-2493 , 文章类型： Article，,卷期：2012年22-7] Structural modification was performed at the C-3 and C-28 positions of ursolic acid (UA). Ten UA derivatives with distinct electrical property were synthesized. They could be divided into two groups according to their ch... N-Caffeoyl serotonin as selective COX-2 inhibitor [作者：Takahashi, T; Miyazawa, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2494-2496 , 文章类型： Article，,卷期：2012年22-7] The inhibitory effects of the synthetic serotonin analogues (1-8) on COX (1 and 2) were evaluated. Two serotonin derivatives (4 and 8) showed inhibitory effect of COX (1 and 2). Especially, 4 exhibited excellent inhibiti... Thiadiazoles as new inhibitors of diacylglycerol acyltransferase type 1 [作者：Mougenot, P; Namane, C; Fett, E; Camy, F; Dadji-Faihun, R; Langot, G; Monseau, C; Onofri, B; Pacquet, F; Pascal, C; Crespin, O; Ben-Hassine, M; Ragot, JL; Van-Pham, T; Philippo, C; Chatelain-Egger, F; Peron, P; Le Bail, JC; Guillot, E; Chamiot-Clerc, P; Chabanaud, MA; Pruniaux, MP; Schmidt, F; Venier, O; Nicolai, E; Viviani, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2497-2502 , 文章类型： Article，,卷期：2012年22-7] A novel class of DGAT1 inhibitors containing a thiadiazole core has been discovered. Chemical optimization lead to inhibitors of human DGAT1 with an appropriate ADME profile and that show in vivo activity in target tissu... Verrulactones A and B, new inhibitors of Staphylococcus aureus enoyl-ACP reductase produced by Penicillium verruculosum F375 [作者：Kim, N; Sohn, MJ; Kim, CJ; Kwon, HJ; Kim, WG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2503-2506 , 文章类型： Article，,卷期：2012年22-7] New dimeric compounds of alternariol class, verrulactones A and B, were isolated from a culture broth of the fungal strain Penicillium verruculosum F375 and their structure were established by various spectral analysis. ... Synthesis, resolution and anticonvulsant activity of chiral N-1 '-ethyl,N-3 '-(1-phenylethyl)-(R,S)-2 ' H,3H,5 ' H-spiro-(2-benzofuran-1,4 '-imidazolidine)-2 ',3,5 '- trione diastereomers [作者：Sadarangani, IR; Bhatia, S; Amarante, D; Lengyel, I; Stephani, RA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2507-2509 , 文章类型： Article，,卷期：2012年22-7] Four new N-1', N-3'-disubstituted-2'H, 3H, 5'H-spiro-(2-benzofuran-1,4'-imidazolidine)-2',3,5'-triones bearing a chiral N-3' substituent were synthesized, resolved and their anticonvulsant activity was obtained and deter... Novel, druglike 1,7-disubstituted 2,3,4,5-tetrahydro-1H-benzo[b]azepine-based selective inhibitors of human neuronal nitric oxide synthase (nNOS) [作者：Annedi, SC; Ramnauth, J; Cossette, M; Maddaford, SP; Dove, P; Rakhit, S; Andrews, JS; Porreca, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2510-2513 , 文章类型： Article，,卷期：2012年22-7] A novel class of 1,7-disubstituted 2,3,4,5-tetrahydro-1H-benzo[b]azepine derivatives was designed, synthesized and evaluated as human nitric oxide synthase (NOS) inhibitors. Structure-activity relationship studies based ... 3-Phenyl-5-isothiazole carboxamides with potent mGluR1 antagonist activity [作者：Fisher, MJ; Backer, RT; Barth, VN; Garbison, KE; Gruber, JM; Heinz, BA; Iyengar, S; Hollinshead, SP; Kingston, A; Kuklish, SL; Li, LL; Nisenbaum, ES; Peters, SC; Phebus, L; Simmons, RMA; van der Aar, E,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2514-2517 , 文章类型： Article，,卷期：2012年22-7] The disclosed 3-phenyl-5-isothiazole carboxamides are potent allosteric antagonists of mGluR1 with generally good selectivity relative to the related group 1 receptor mGluR5. Pharmacokinetic properties of a member of thi... Synthesis and biological properties of chemically modified siRNAs bearing 1-deoxy-D-ribofuranose in their 3 '-overhang region [作者：Taniho, K; Nakashima, R; Kandeel, M; Kitamura, Y; Kitade, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2518-2521 , 文章类型： Article，,卷期：2012年22-7] To elucidate the role of the sugar moiety in the two natural nucleotides of the 3'-overhang region of small interfering RNA (siRNA), we synthesized siRNAs that incorporated two abasic nucleosides, 1-deoxy-D-ribofuranose ... A novel 3,4-dihydropyrimidin-2(1H)-one: HIV-1 replication inhibitors with improved metabolic stability [作者：Kim, J; Ok, T; Park, C; So, W; Jo, M; Kim, Y; Seo, M; Lee, D; Jo, S; Ko, Y; Choi, I; Park, Y; Yoon, J; Ju, MK; Ahn, J; Kim, J; Han, SJ; Kim, TH; Cechetto, J; Namc, J; Liuzzi, M; Sommer, P; No, Z,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2522-2526 , 文章类型： Article，,卷期：2012年22-7] Following the previous SAR of a novel dihydropyrimidinone scaffold as HIV-1 replication inhibitors a detailed study directed towards optimizing the metabolic stability of the ester functional group in the dihydropyrimidi...