- Towards novel S-DABOC inhibitors: Synthesis, biological investigation, and molecular modeling studies
[作者:Radi, M; Angeli, L; Franchi, L; Contemori, L; Maga, G; Samuele, A; Zanoli, S; Armand-Ugon, M; Gonzalez, E; Llano, A; Este, JA; Botta, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5777-5780 , 文章类型: Article,,卷期:2008年18-21]
- A small family of S-DABO cytosine analogs (S-DABOCs) has been synthesized and biologically evaluated as HIV-1 inhibitor both on wild type (wt) and drug-resistant mutants leading to the identification of an interesting co...
- The identification of neurotensin NTS1 receptor partial agonists through a ligand-based virtual screening approach
[作者:Fan, Y; Lai, MH; Sullivan, K; Popiolek, M; Andree, TH; Dollings, P; Pausch, MH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5789-5791 , 文章类型: Article,,卷期:2008年18-21]
- We identified small molecule NTS1R agonist compounds through virtual screening of the corporate database using a ROCS approach that searches multi-conformer representations efficiently. As a starting point for the ROCS s...
- Synthesis and biological evaluation of a novel decadentate ligand DEPA
[作者:Chong, HS; Lim, S; Baidoo, KE; Milenic, DE; Ma, X; Jia, F; Song, HA; Brechbiel, MW; Lewis, MR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5792-5795 , 文章类型: Article,,卷期:2008年18-21]
- An efficient and short synthetic route to a novel decadentate ligand 7-[2-(bis-carboxymethyl-amino)-ethyl]-4,10-bis-carboxymethyl-1,4,7,10-tetraaza-cyclododec-1-yl-acetic acid (DEPA) with both macrocyclic and acyclic bin...
- 2-Aryloxymethylmorpholine histamine H-3 antagonists
[作者:Letavic, MA; Keith, JM; Ly, KS; Bonaventure, P; Feinstein, MA; Lord, B; Miller, KL; Motley, ST; Nepomuceno, D; Sutton, SW; Carruthers, NI,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5796-5799 , 文章类型: Article,,卷期:2008年18-21]
- The synthesis and biological activity of a new series of 2-aryloxymethylmorpholine histamine H-3 antagonists is described. The new compounds are high affinity histamine H-3 ligands that penetrate the CNS and occupy the h...
- One-pot synthesis and antibacterial activities of pyrazolo[4 ',3 ':5,6]pyrido[2,3-d]pyrimidine-dione derivatives
[作者:Bazgir, A; Khanaposhtani, MM; Soorki, AA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5800-5803 , 文章类型: Article,,卷期:2008年18-21]
- A one-pot and efficient method for the synthesis of pyrazolo[4',3':5,6] pyrido[2,3-d]pyrimidine-dione derivatives by condensation reaction of barbituric acids, 1H-pyrazol-5-amines and aldehydes under solvent-free conditi...
- Piperidine dispiro-1,2,4-trioxane analogues
[作者:Sabbani, S; Stocks, PA; Ellis, GL; Davies, J; Hedenstrom, E; Ward, SA; O'Neill, PM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5804-5808 , 文章类型: Article,,卷期:2008年18-21]
- Dispiro N-Boc-protected 1,2,4-trioxane 2 was synthesised via Mo(acac)(2) catalysed perhydrolysis of N-Boc spirooxirane followed by condensation of the resulting beta-hydroperoxy alcohol 10 with 2-adamantanone. N-Boc 1,2,...
- Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: Optimization of the S3 ' pocket
[作者:Mazzola, RD; Zhu, ZN; Sinning, L; McKittrick, B; Lavey, B; Spitler, J; Kozlowski, J; Neng-Yang, S; Zhou, GW; Guo, ZY; Orth, P; Madison, V; Sun, J; Lundell, D; Niu, XD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5809-5814 , 文章类型: Article,,卷期:2008年18-21]
- A series of cyclopropyl hydroxamic acids were prepared. Many of the compounds displayed picomolar affinity for the TACE enzyme while maintaining good to excellent selectivity profiles versus MMP-1, - 2, - 3, - 7, - 14, a...
- Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists
[作者:Bongartz, JP; Buntinx, M; Coesemans, E; Hermans, B; Van Lommen, G; Van Wauwe, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5819-5823 , 文章类型: Article,,卷期:2008年18-21]
- The synthesis and evaluation of benzetimide derivatives showing potent CXCR3 antagonism are described. Optimization of the screening hits led to the identification of more potent CXCR3 antagonists devoid of anti-choliner...
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