- Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues
[作者:Beguin, C; Potuzak, J; Xu, W; Liu-Chen, LY; Streicher, JM; Groer, CE; Bohn, LM; Carlezon, WA; Cohen, BM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1023-1026 , 文章类型: Article,,卷期:2012年22-2]
- The kappa opioid receptor (KOPR) has been identified as a potential drug target to prevent or alter the course of mood, anxiety and addictive disorders or reduce response to stress. In a search for highly potent and sele...
- Synthesis, characterization and in vitro biological evaluation of some novel diarylsulfonylureas as potential cytotoxic and antimicrobial agents
[作者:Avupati, VR; Yejella, RP; Guntuku, G; Gunta, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1031-1035 , 文章类型: Article,,卷期:2012年22-2]
- A series of novel diarylsulfonylureas (1-28) have been synthesized and characterized by FTIR, H-1 NMR, C-13 NMR and LC mass spectral analysis. All the synthesized compounds were evaluated for their in vitro cytotoxicity ...
- Design and synthesis of novel photoaffinity probes for study of the target proteins of oleanolic acid
[作者:Zhang, LY; Zhang, YX; Dong, JZ; Liu, J; Zhang, LY; Sun, HB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1036-1039 , 文章类型: Article,,卷期:2012年22-2]
- To explore the molecular mechanisms of oleanolic acid, two novel photoaffinity probes were synthesized based on the structure-activity relationship reported previously. Their potency were evaluated in an enzyme inhibitio...
- Solid-state NMR analysis of calcium and D-mannose binding of BMY-28864, a water-soluble analogue of pradimicin A
[作者:Nakagawa, Y; Doi, T; Takegoshi, K; Igarashi, Y; Ito, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1040-1043 , 文章类型: Article,,卷期:2012年22-2]
- Pradimicin A (PRM-A) is a unique antibiotic with a lectin-like ability to recognize D-mannopyranosides (Man) in the presence of Ca2+ ion. BMY-28864 (1) is a water-soluble analogue of PRM-A, which has been extensively use...
- Development of a more highly selective M-1 antagonist from the continued optimization of the MLPCN Probe ML012
[作者:Melancon, BJ; Lamers, AP; Bridges, TM; Sulikowski, GA; Utley, TJ; Sheffler, DJ; Noetzel, MJ; Morrison, RD; Daniels, JS; Niswender, CM; Jones, CK; Conn, PJ; Lindsley, CW; Wood, MR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1044-1048 , 文章类型: Article,,卷期:2012年22-2]
- This Letter describes the continued optimization of an MLPCN probe molecule (ML012) through an iterative parallel synthesis approach. After exploring extensive modifications throughout the parent structure, we arrived at...
- Structure-based library design and the discovery of a potent and selective mast cell beta-tryptase inhibitor as an oral therapeutic agent
[作者:Liang, GY; Aldous, S; Merriman, G; Levell, J; Pribish, J; Cairns, J; Chen, X; Maignan, S; Mathieu, M; Tsay, J; Sides, K; Rebello, S; Whitely, B; Morize, I; Pauls, HW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1049-1054 , 文章类型: Article,,卷期:2012年22-2]
- A solid phase combinatorial library was designed based on X-ray structures and in-silico models to explore an inducible S4+ pocket, which is formed by a simple side-chain rotation of Tyr95. This inducible S4+ pocket is u...
- Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists
[作者:Nguyen, HN; Bregman, H; Buchanan, JL; Du, BF; Feric, E; Huang, LY; Li, XW; Ligutti, J; Liu, D; Malmberg, AB; Matson, DJ; McDermott, JS; Patel, VF; Wilenkin, B; Zou, AR; McDonough, SI; DiMauro, EF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1055-1060 , 文章类型: Article,,卷期:2012年22-2]
- Clinical genetic data have shown that the product of the SCN9A gene, voltage-gated sodium ion channel Nav1.7, is a key control point for pain perception and a possible target for a next generation of analgesics. Sodium c...
- Discovery of dehydro-oxopiperazine acetamides as novel bradykinin B1 receptor antagonists with enhanced in vitro potency
[作者:Qian, WY; Chen, JJ; Human, J; Aya, T; Zhu, JW; Biswas, K; Peterkin, T; Hungate, RW; Arik, L; Johnson, E; Kumar, G; Joseph, S; Jona, J; Guo, HX; Wu, ZF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1061-1067 , 文章类型: Article,,卷期:2012年22-2]
- In a series of bradykinin B1 antagonists, we discovered that replacement of oxopiperazine acetamides with dehydro-oxopiperazine acetamides provided compounds with enhanced activity against the B1 receptor. The synthesis ...
- Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors
[作者:Rao, AU; Xiao, D; Huang, XH; Zhou, W; Fossetta, J; Lundell, D; Tian, F; Trivedi, P; Aslanian, R; Palani, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1068-1072 , 文章类型: Article,,卷期:2012年22-2]
- Facile synthesis of two new series of tetracyclic azepine and oxazocine analogs is described. These analogs were evaluated for their potential as MAPKAP-K2 (MK2) inhibitors and several were found to be potent at inhibiti...
- Synthesis and structure-activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H-3 receptor inverse agonists
[作者:Tao, M; Aimone, LD; Gruner, JA; Mathiasen, JR; Huang, ZQ; Lyons, J; Raddatz, R; Hudkins, RL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1073-1077 , 文章类型: Article,,卷期:2012年22-2]
- Optimization of the R-2 and R-6 positions of (5-{4-[3-(R)-2-methylpyrrolin-1-yl-propoxylphenyl)-2H-pyridazin-3-one) 2a with constrained phenoxypiperidines led to the identification of 5-[4-(cyclobutyl-piperidin-4-yloxy)-...
- Structural modification of ginsenoside Rh-2 by fatty acid esterification and its detoxification property in antitumor
[作者:Wei, GQ; Zheng, YN; Li, W; Liu, WC; Lin, T; Zhang, WY; Chen, HF; Zeng, JZ; Zhang, XK; Chen, QC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1082-1085 , 文章类型: Article,,卷期:2012年22-2]
- Ginsenoside Rh-2, one of the most important ginsenosides with anticancer properties in red ginseng, has been developed as principal antitumor ingredient for clinical use. However, the cytotoxicity test in human hepatocyt...
- Steroidal C-21 heteroaryl thioethers (Part 2): Discovery of orally bioavailable selective glucocorticoid receptor modulators (dissociated steroids)
[作者:Biju, P; McCormick, K; Aslanian, R; Berlin, M; Solomon, D; Wang, HW; Lee, YJ; Bitar, R; Prelusky, D; Mcleod, R; Jia, YL; Fernandez, X; Eckel, S; House, A; Lieber, G; Jimenez, J; Kelly, G; Chapman, R; Phillips, J; Anthes, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1086-1090 , 文章类型: Article,,卷期:2012年22-2]
- The prednisolone C-21 heteroaryl thioethers have been synthesized and evaluated in cell based transrepression and transactivation assays. Most of the compounds demonstrated weak transactivational activity in both human a...
- Antimycobacterial activities of 5-alkyl (or halo)-3 '-substituted pyrimidine nucleoside analogs
[作者:Srivastav, NC; Shakya, N; Bhavanam, S; Agrawal, A; Tse, C; Desroches, N; Kunimoto, DY; Kumar, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1091-1094 , 文章类型: Article,,卷期:2012年22-2]
- Several 5-alkyl (or halo)-3'-azido (amino or halo) analogs of pyrimidine nucleosides have been synthesized and evaluated against Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium. Among these compou...
- Novel, potent and orally bioavailable indolizidinone-derived inhibitors of the hepatitis C virus NS3 protease
[作者:Clarke, MO; Byun, D; Chen, XW; Doerffler, E; Leavitt, SA; Sheng, XC; Yang, CY; Kim, CU,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1095-1098 , 文章类型: Article,,卷期:2012年22-2]
- A novel, potent, and orally bioavailable class of product-like inhibitors of the HCV NS3 protease was discovered by constraining the P2-P3 amide bond and the P3 hydrocarbon substituent to the proteasebound conformation. ...
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