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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64条记录   Synthesis and in vitro antimicrobial activities of new (cyano-NNO-azoxy) pyrazole derivatives [作者：Boschi, D; Guglielmo, S; Aiello, S; Morace, G; Borghi, E; Fruttero, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3431-3434 , 文章类型： Article，,卷期：2011年21-11] The antibacterial and antifungal activity of a series of products, in which the 1,5-dimethyl-4-(cyano-NNO-azoxy)pyrazol-3-yl and 1,3-dimethyl-4-(cyano-NNO-azoxy)pyrazol-5-yl moieties were linked to pyridine, pyrazole, is... Synthesis and biological evaluation of 3-alkyl-dihydrotetrabenazine derivatives as vesicular monoamine transporter-2 (VMAT2) ligands [作者：Zheng, PG; Lieberman, BP; Choi, SR; Ploessl, K; Kung, HF,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3435-3438 , 文章类型： Article，,卷期：2011年21-11] In the search of new probes for in vivo brain imaging of vesicular monoamine transporter type 2 (VMAT2), we have developed an efficient synthesis of a novel series of 3-alkyl-dihydrotetrabenazine (DTBZ) derivatives. The ... Synthesis and bioactivity of new Finasteride conjugate [作者：Zhao, S; Wu, JZ; Yang, LJ; Li, Z; Yu, DH; Li, JF; Yu, J; Liang, YT; Wang, ES; Fang, XX,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3439-3442 , 文章类型： Article，,卷期：2011年21-11] Finasteride is a synthetic 4-azasteroid compound that acts by inhibiting type II 5 alpha-reductase, the enzyme that converts the androgen testosterone to 5 alpha-dihydrotestosterone. It was approved by the US FDA for the... Synthesis and in vitro anti-HIV activity of N-1,3-benzo[d]thiazol-2-yl-2-(2-oxo-2H-chromen-4-yl)acetamide derivatives using MTT method [作者：Bhavsar, D; Trivedi, J; Parekh, S; Savant, M; Thakrar, S; Bavishi, A; Radadiya, A; Vala, H; Lunagariya, J; Parmar, M; Paresh, L; Loddo, R; Shah, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3443-3446 , 文章类型： Article，,卷期：2011年21-11] A series of novel N-1,3-benzo[d]thiazol-2-yl-2-(2-oxo-2H-chromen-4-yl)acetamide derivatives has been synthesized. All the newly synthesized compounds were evaluated for their anti-HIV activity using MTT method. Most of t... Synthesis and SAR study of tricyclic sulfones as gamma-secretase inhibitors: C-6 and C-8 positions [作者：Su, J; Tang, HQ; McKittrick, BA; Xu, R; Clader, JW; Greenlee, WJ; Hyde, L; Zhang, LL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3447-3451 , 文章类型： Article，,卷期：2011年21-11] SAR exploration at C-6 and C-8 positions of the tricyclic sulfone series was carried out. Several functional groups were found to be well tolerated at C-6 and C-8 positions. Selective combination of C-6 and C-8 modificat... 3-Amino-pyrazolo[3,4-d]pyrimidines as p38 alpha kinase inhibitors: Design and development to a highly selective lead [作者：Soth, M; Abbot, S; Abubakari, A; Arora, N; Arzeno, H; Billedeau, R; Dewdney, N; Durkin, K; Frauchiger, S; Ghate, M; Goldstein, DM; Hill, RJ; Kuglstatter, A; Li, FJ; Loe, B; McCaleb, K; McIntosh, J; Papp, E; Park, J; Stahl, M; Sung, ML; Suttman, R; Swinney, DC; Weller, P; Wong, B; Zecic, H; Gabriel, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3452-3456 , 文章类型： Article，,卷期：2011年21-11] Learnings from previous Roche p38-selective inhibitors were applied to a new fragment hit, which was optimized to a potent, exquisitely selective preclinical lead with a good pharmacokinetic profile. (C) 2011 Elsevier Lt... Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists [作者：Prat, M; Buil, MA; Fernandez, MD; Castro, J; Monleon, JM; Tort, L; Casals, G; Ferrer, M; Huerta, JM; Espinosa, S; Lopez, M; Segarra, V; Gavalda, A; Miralpeix, M; Ramos, I; Vilella, D; Gonzalez, M; Cordoba, M; Cardenas, A; Anton, F; Beleta, J; Ryder, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3457-3461 , 文章类型： Article，,卷期：2011年21-11] Novel quaternary ammonium derivatives of N,N-disubstituted (3R)-quinuclidinyl carbamates have been identified as potent M-3 muscarinic antagonists with long duration of action in an in vivo model of bronchoconstriction. ... A new iridoid and effect on the rat aortic vascular smooth muscle cell proliferation of isolated compounds from Buddleja officinalis [作者：Tai, BH; Nhiem, NX; Quang, TH; Nguyen, TTN; Tung, NH; Kim, Y; Lee, JJ; Myung, CS; Cuong, NM; Kim, YH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3462-3466 , 文章类型： Article，,卷期：2011年21-11] A new iridoid, named methylscutelloside (1) together with 19 known compounds belonging to the iridoids (2-4), monoterpenoids (5), flavonoids (6-8), triterpenoids (9-14), and phenylethanoids (15-20) were isolated from the... Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life [作者：Pike, KG; Allen, JV; Caulkett, PWR; Clarke, DS; Donald, CS; Fenwick, ML; Johnson, KM; Johnstone, C; McKerrecher, D; Rayner, JW; Walker, RP; Wilson, I,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3467-3470 , 文章类型： Article，,卷期：2011年21-11] The continued optimization of a series of glucokinase activators is described, including attempts to understand the interplay between molecular structure and the composite parameter of unbound clearance. These studies re... New indole amide derivatives as potent CRTH2 receptor antagonists [作者：Zaghdane, H; Boyd, M; Colucci, J; Simard, D; Berthelette, C; Leblanc, Y; Wang, ZY; Houle, R; Levesque, JF; Molinaro, C; Hamel, M; Stocco, R; Sawyer, N; Sillaots, S; Gervais, F; Gallant, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3471-3474 , 文章类型： Article，,卷期：2011年21-11] A new series of indole amide acting as hCRTH2 receptor ligands had been explored and are described herein. Several amide derivatives displaying low nanomolar activity in hCRTH2 binding and whole blood assays were identif... Synthesis and antidyslipidemic activity of chalcone fibrates [作者：Shukla, P; Srivastava, SP; Srivastava, R; Rawat, AK; Srivastava, AK; Pratap, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3475-3478 , 文章类型： Article，,卷期：2011年21-11] A series of chalcone based PPAR-alpha agonists were synthesized and evaluated for their antidyslipidemic activity in high fructose high fat fed dyslipidemic Syrian golden hamsters. Most of the compounds exhibited antidys... Design, synthesis, and biological activity of novel Magmas inhibitors [作者：Jubinsky, PT; Short, MK; Ghanem, M; Das, BC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3479-3482 , 文章类型： Article，,卷期：2011年21-11] Magmas (mitochondria associated, granulocyte-macrophage colony stimulating factor signaling molecule), is a highly conserved and essential gene, expressed in all cell types. We designed and synthesized several small mole... Anti-inflammatory activity of constituents from Glechoma hederacea var. longituba [作者：Kim, J; Song, S; Lee, I; Kim, Y; Yoo, I; Ryoo, I; Bae, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3483-3487 , 文章类型： Article，,卷期：2011年21-11] Rosmarinic acid, its analogues, and a phenolic compound were obtained from G. hederacea var. longituba. There were two new compounds, methyl isoferuloyl-7-(3,4-dihydroxyphenyl) lactate (1) and benzyl-4'-hydroxy-benzoyl-3... Non-oxime pyrazole based inhibitors of B-Raf kinase [作者：Newhouse, BJ; Hansen, JD; Grina, J; Welch, M; Topalov, G; Littman, N; Callejo, M; Martinson, M; Galbraith, S; Laird, ER; Brandhuber, BJ; Vigers, G; Morales, T; Woessner, R; Randolph, N; Lyssikatos, J; Olivero, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3488-3492 , 文章类型： Article，,卷期：2011年21-11] The synthesis and biological evaluation of non-oxime pyrazole based B-Raf inhibitors is reported. Several oxime replacements have been prepared and have shown excellent enzyme activity. Further optimization of fused pyra... Actin depolymerizing effect of trisoxazole-containing macrolides [作者：Chung, SC; Lee, SH; Jang, KH; Park, W; Jeon, JE; Oh, H; Shin, J; Oh, KB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3198-3201 , 文章类型： Article，,卷期：2011年21-11] Oxazole-containing macrolides (1-5) isolated from the marine sponge Chondrosia corticata were evaluated for their actin depolymerizing activities by monitoring fluorescent intensity of pyrene F-actin. These studies led t... 2-Arylmethylaminomethyl-5,6-dihydroxychromone derivatives with selective anti-HCV activity [作者：Park, HR; Park, KS; Chong, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3202-3205 , 文章类型： Article，,卷期：2011年21-11] Anti-HCV activity of aryl diketoacid (ADK) has been characterized by its two pharmacophoric elements, alpha,beta-diketo acid moiety and substituted aryl ring. In this study, as a part of our ongoing efforts to discover a...