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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   Anti-inflammatory and PPAR transactivational effects of secondary metabolites from the roots of Asarum sieboldii [作者：Quang, TH; Ngan, NTT; Van Minh, C; Van Kiem, P; Tai, BH; Thao, NP; Song, SB; Kim, YH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2527-2533 , 文章类型： Article，,卷期：2012年22-7] Phytochemical study on the roots of Asarum sieboldii resulted in the isolation of one new compound, (1R,2S,5R,6R)-5'-O-methylpluviatilol (1) and 12 known compounds (2-13). Their structures were determined by extensive sp... Oroxylin A analogs exhibited strong inhibitory activities against iNOS-mediated nitric oxide (NO) production [作者：Pham, TAN; Che, H; Phan, PTT; Lee, JW; Kim, SS; Park, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2534-2535 , 文章类型： Article，,卷期：2012年22-7] A number of oroxylin A analogs were prepared and evaluated for their inhibitory activities against iNOS-mediated nitric oxide (NO) production from LPS-stimulated BV2 cells. The analogs were synthesized from purchased 2'-... Structure based design of an in vivo active hydroxamic acid inhibitor of P. aeruginosa LpxC [作者：Warmus, JS; Quinn, CL; Taylor, C; Murphy, ST; Johnson, TA; Limberakis, C; Ortwine, D; Bronstein, J; Pagano, P; Knafels, JD; Lightle, S; Mochalkin, I; Brideau, R; Podoll, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2536-2543 , 文章类型： Article，,卷期：2012年22-7] Lipid A is an essential component of the Gram negative outer membrane, which protects the bacterium from attack of many antibiotics. The Lipid A biosynthesis pathway is essential for Gram negative bacterial growth and is... Discovery of nor-seco himbacine analogs as thrombin receptor antagonists [作者：Chelliah, MV; Chackalamannil, S; Xia, Y; Eagen, K; Greenlee, WJ; Ahn, HS; Agans-Fantuzzi, J; Boykow, G; Hsieh, YS; Bryant, M; Chan, TM; Chintala, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2544-2549 , 文章类型： Article，,卷期：2012年22-7] Discovery of a novel nor-seco himbacine analog as potent thrombin receptor (PAR-1) antagonist is described. Despite low plasma level, these new analogs showed excellent ex vivo efficacy in the monkey platelet aggregation... Discovery of novel aminoquinazolin-7-yl 6,7-dihydro-indol-4-ones as potent, selective inhibitors of heat shock protein 90 [作者：Huang, KH; Barta, TE; Rice, JW; Smith, ED; Ommen, AJ; Ma, W; Veal, JM; Fadden, RP; Barabasz, AF; Foley, BE; Hughes, PF; Hanson, GJ; Markworth, CJ; Silinski, M; Partridge, JM; Steed, PM; Hall, SE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2550-2554 , 文章类型： Article，,卷期：2012年22-7] A novel class of Hsp90 inhibitors, structurally distinct from previously reported scaffolds, was developed from rational design and optimization of a compound library screen hit. These aminoquinazoline derivatives, repre... Penicillin inhibitors of purple acid phosphatase [作者：Faridoon; Hussein, WM; Islam, NU; Guddat, LW; Schenk, G; McGeary, RP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2555-2559 , 文章类型： Article，,卷期：2012年22-7] Purple acid phosphatases (PAPs) are binuclear metallohydrolases that have a multitude of biological functions and are found in fungi, bacteria, plants and animals. In mammals, PAP activity is linked with bone resorption ... Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT2C agonists [作者：Conway, RJ; Valant, C; Christopoulos, A; Robertson, AD; Ben Capuano; Crosby, IT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2560-2564 , 文章类型： Article，,卷期：2012年22-7] A series of substituted 4-arylpiperidines and a smaller family of 4-aryl-1,2,3,6-tetrahydropyridines were synthesized and their biological activity at the 5-HT2C receptor studied to determine whether either series showed... Discovery of P2X3 selective antagonists for the treatment of chronic pain [作者：Cantin, LD; Bayrakdarian, M; Buon, C; Grazzini, E; Hua, YJ; Labrecque, J; Leung, C; Luo, XH; Martino, G; Pare, M; Payza, K; Popovic, N; Projean, D; Santhakumar, V; Walpole, C; Yu, XH; Tomaszewski, MJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2565-2571 , 文章类型： Article，,卷期：2012年22-7] Purinergic receptor P2X3 has been linked to analgesia in a number of pre-clinical models of pain, and is expressed in the human pain perception pathway. Only few P2X3-selective antagonists have been reported to date. Thi... Design of oxobenzimidazoles and oxindoles as novel androgen receptor antagonists [作者：Guo, CX; Pairish, M; Linton, A; Kephart, S; Ornelas, M; Nagata, A; Burke, B; Dong, LM; Engebretsen, J; Fanjul, AN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2572-2578 , 文章类型： Article，,卷期：2012年22-7] Oxobenzimidazoles (e.g., 1), a novel series of androgen receptor (AR) antagonists, were discovered through de novo design guided by structure-based drug design. The compounds in this series were reasonably permeable and ... Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. Part 1. Sildenafil analogs [作者：Wang, C; Ashton, TD; Gustafson, A; Bland, ND; Ochiana, SO; Campbell, RK; Pollastri, MP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2579-2581 , 文章类型： Article，,卷期：2012年22-7] Parasitic diseases, such as African sleeping sickness, have a significant impact on the health and wellbeing in the poorest regions of the world. Pragmatic drug discovery efforts are needed to find new therapeutic agents... Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. Part 2. Tadalafil analogs [作者：Ochiana, SO; Gustafson, A; Bland, ND; Wang, C; Russo, MJ; Campbell, RK; Pollastri, MP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2582-2584 , 文章类型： Article，,卷期：2012年22-7] In this Letter we describe our ongoing target repurposing efforts focused on discovery of inhibitors of the essential trypanosomal phosphodiesterase TbrPDEB1. This enzyme has been implicated in virulence of Trypanosoma b... The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia [作者：Ho, GD; Seganish, WM; Bercovici, A; Tulshian, D; Greenlee, WJ; Van Rijn, R; Hruza, A; Xiao, L; Rindgen, D; Mullins, D; Guzzi, M; Zhang, XP; Bleickardt, C; Hodgson, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2585-2589 , 文章类型： Article，,卷期：2012年22-7] The identification of potent and orally active dihydroimidazoisoquinolines as PDE 10A inhibitors is reported. The SAR development led to the discovery of compound 35 as a potent, selective, and orally active PDE10A inhib... Synthesis and comparative evaluation of 4-oxa- and 4-aza-podophyllotoxins as antiproliferative microtubule destabilizing agents [作者：Chernysheva, NB; Tsyganov, DV; Philchenkov, AA; Zavelevich, MP; Kiselyov, AS; Semenov, RV; Semenova, MN; Semenov, VV,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2590-2593 , 文章类型： Article，,卷期：2012年22-7] A series of novel 4-oxa-podophyllotoxin derivatives 7 featuring the intact lactone ring D and various substituents in rings B and E has been synthesized and evaluated in a phenotypic sea urchin embryo assay along with th... Discovery of oxazole-based PDE4 inhibitors with picomolar potency [作者：Kuang, R; Shue, HJ; Xiao, L; Blythin, DJ; Shih, NY; Chen, X; Gu, D; Schwerdt, J; Lin, L; Ting, PC; Cao, JH; Aslanian, R; Piwinski, JJ; Prelusky, D; Wu, P; Zhang, J; Zhang, X; Celly, CS; Billah, M; Wang, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2594-2597 , 文章类型： Article，,卷期：2012年22-7] Optimization of oxazole-based PDE4 inhibitors has led to the discovery of a series of quinolyl oxazoles, with 4-benzylcarboxamide and 5-alpha-aminoethyl groups which exhibit picomolar potency against PDE4. Selectivity pr... Stereoselective synthesis of bio-hybrid amphiphiles of coumarin derivatives by Ugi-Mannich triazole randomization using copper catalyzed alkyne azide click chemistry [作者：Pramitha, P; Bahulayan, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2598-2603 , 文章类型： Article，,卷期：2012年22-7] An efficient synthesis of ester-triazole-amide amphiphiles of coumarin derivatives by triazole randomization based on click approach is described. Twenty-five small peptide azides were synthesized using Ugi or alternate ... Synthesis and evaluation of 2-amido-3-carboxamide thiophene CB2 receptor agonists for pain management [作者：Nelson, DW; Frost, JM; Tietje, KR; Florjancic, AS; Ryther, K; Carroll, WA; Dart, MJ; Daza, AV; Hooker, BA; Grayson, GK; Fan, YH; Garrison, TR; El-Kouhen, OF; Yao, B; Pai, M; Chandran, P; Zhu, C; Hsieh, GC; Meyer, MD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2604-2608 , 文章类型： Article，,卷期：2012年22-7] SAR studies on a series of thiophene amide derivatives provided CB2 receptor agonists. The activity of the compounds was characterized by radioligand binding determination, multiple functional assays, ADME, and pharmacok...