- Synthesis and anti-HCV activity of 3 ',4 '-oxetane nucleosides
[作者:Chang, W; Du, JF; Rachakonda, S; Ross, BS; Convers-Reignier, S; Yau, WT; Pons, JF; Murakami, E; Bao, HY; Steuer, HM; Furman, PA; Otto, MJ; Sofia, MJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4539-4543 , 文章类型: Article,,卷期:2010年20-15]
- Hepatitis C virus afflicts approximately 180 million people worldwide and currently there are no direct acting antiviral agents available to treat this disease. Our first generation nucleoside HCV inhibitor, RG7128 has a...
- Celecoxib prodrugs possessing a diazen-1-ium-1,2-diolate nitric oxide donor moiety: Synthesis, biological evaluation and nitric oxide release studies
[作者:Abdellatif, KRA; Chowdhury, MA; Velazquez, CA; Huang, ZJ; Dong, Y; Das, D; Yu, G; Suresh, MR; Knaus, EE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4544-4549 , 文章类型: Article,,卷期:2010年20-15]
- A new class of anti-inflammatory (AI) cupferron prodrugs was synthesized wherein a diazen-1-ium-1,2-diolato ammonium salt, and its O-2-methyl and O-2-acetoxyethyl derivatives, nitric oxide (NO) donor moieties were attach...
- Discovery of novel sphingosine kinase-1 inhibitors. Part 2
[作者:Xiang, YB; Hirth, B; Kane, JL; Liao, JK; Noson, KD; Yee, C; Asmussen, G; Fitzgerald, M; Klaus, C; Booker, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4550-4554 , 文章类型: Article,,卷期:2010年20-15]
- Building on our initial work, we have identified additional novel inhibitors of sphingosine kinase-1 (SK1). These new analogs address the shortcomings found in our previously reported compounds. Inhibitors 51 and 54 demo...
- Synthesis and activity of polyacetylene substituted 2-hydroxy acids, esters, and amides against microbes of clinical importance
[作者:Kyi, S; Wongkattiya, N; Warden, AC; O'Shea, MS; Deighton, M; Macreadie, I; Graichen, FHM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4555-4557 , 文章类型: Article,,卷期:2010年20-15]
- A series of novel polyacetylene substituted 2-hydroxy acids and derivatives were prepared and characterized. Alkylation of butane-2,3-diacetal (BDA) protected glycolic acid with iodoalkyl substituted polyacetylene compou...
- beta-Secretase (BACE-1) inhibitory effect of biflavonoids
[作者:Sasaki, H; Miki, K; Kinoshita, K; Koyama, K; Juliawaty, LD; Achmad, SA; Hakim, EH; Kaneda, M; Takahashi, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4558-4560 , 文章类型: Article,,卷期:2010年20-15]
- Here, we describe amentoflavone-type biflavonoids, which were isolated from natural sources and were found to inhibit beta-secretase (BACE-1). The structure-activity relationship was studied, and compounds 1-8, 10, 17, a...
- Identification of novel alpha 7 nAChR positive allosteric modulators with the use of pharmacophore in silico screening methods
[作者:Capelli, AM; Castelletti, L; Salvagno, C; Oliosi, B; Di Lenarda, E; Virginio, C; Lightfoot, A; Kew, JNC; Teague, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4561-4565 , 文章类型: Article,,卷期:2010年20-15]
- The pharmacophore model of in house potent and selective alpha 7 nAChR positive allosteric modulators is reported. The model was used to fish out commercially-available compounds from corporate 3D databases. As a result,...
- A specific and direct comparison of the trifluoromethyl and pentafluoro sulfanyl groups on the selective dopamine D-3 antagonist 3-(3-{[4-methyl-5-(4-methyl-1,3-oxazol-5-yl)-4H-1,2,4-triazol-3-yl]thio}propyl)-1-phenyl-3-azabicyclo[3.1.0] hexane template
[作者:Micheli, F; Andreotti, D; Braggio, S; Checchia, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4566-4568 , 文章类型: Article,,卷期:2010年20-15]
- A direct and specific comparison of a trifluoromethyl group with the corresponding pentafluorosulfanyl group is made in terms of primary affinity and pharmacokinetic properties. (C) 2010 Elsevier Ltd. All rights reserved...
- Ceratinadins A-C, new bromotyrosine alkaloids from an Okinawan marine sponge Pseudoceratina sp.
[作者:Kon, Y; Kubota, T; Shibazaki, A; Gonoi, T; Kobayashi, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4569-4572 , 文章类型: Article,,卷期:2010年20-15]
- Three new bromotyrosine alkaloids, ceratinadins A-C (1-3), were isolated from an Okinawan marine sponge Pseudoceratina sp. and the structures of 1-3 were elucidated on the basis of spectroscopic data. Ceratinadin A (1) w...
- 5-Nitro-2-furoic acid hydrazones: Design, synthesis and in vitro antimycobacterial evaluation against log and starved phase cultures
[作者:Sriram, D; Yogeeswari, P; Vyas, DRK; Senthilkumar, P; Bhat, P; Srividya, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4313-4316 , 文章类型: Article,,卷期:2010年20-15]
- Various 5-nitro-2-furoic acid hydrazones were synthesized and evaluated for in vitro activities against log and starved phase culture of two mycobacterial species and Mycobacterium tuberculosis (MTB) isocitrate lyase (IC...
- Peptide deformylase inhibitors with retro-amide scaffold: Synthesis and structure-activity relationships
[作者:Lee, SK; Choi, KH; Lee, SJ; Suh, SW; Kim, BM; Lee, BJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4317-4319 , 文章类型: Article,,卷期:2010年20-15]
- Peptide deformylase (PDF) is a metalloprotease catalyzing the removal of a formyl group from newly synthesized proteins. Thus inhibition of PDF activity is considered to be one of the most effective antibiotic strategies...
- Rational design of a novel peripherally-restricted, orally active CB1 cannabinoid antagonist containing a 2,3-diarylpyrrole motif
[作者:Hortala, L; Rinaldi-Carmona, M; Congy, C; Boulu, L; Sadoun, F; Fabre, G; Finance, O; Barth, F,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4573-4577 , 文章类型: Article,,卷期:2010年20-15]
- A new series of 2,3-diarylpyrroles have been prepared and evaluated as CB1 antagonists. Modulation of the topological polar surface area allowed the identification of high affinity peripherally-restricted CB1 antagonists...
- Regioselective synthesis of folate receptor-targeted agents derived from epothilone analogs and folic acid
[作者:Vlahov, IR; Vite, GD; Kleindl, PJ; Wang, Y; Santhapuram, HKR; You, F; Howard, SJ; Kim, SH; Lee, FFY; Leamon, CP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4578-4581 , 文章类型: Article,,卷期:2010年20-15]
- Efficient regioselective syntheses of conjugates of folic acid and cytotoxic agents derived from natural epothilones are described. These folate receptor (FR) targeting compounds are water soluble and incorporate a hydro...
- A novel aryl-hydrazide from the marine lichen Lichina pygmaea: Isolation, synthesis of derivatives, and cytotoxicity assays
[作者:Roullier, C; Chollet-Krugler, M; van de Weghe, P; Devehat, FLL; Boustie, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4582-4586 , 文章类型: Article,,卷期:2010年20-15]
- A new aryl-hydrazide L-glutamic acid derivative, pygmeine (3), was isolated from a methanolic extract of Lichina pygmaea, a marine lichen. Synthetic derivatives obtained via a two-step coupling of L-glutamic acid with ph...
- Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: Potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties
[作者:Rheault, TR; Donaldson, KH; Badiang-Alberti, JG; Davis-Ward, RG; Andrews, CW; Bambal, R; Jackson, JR; Cheung, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4587-4592 , 文章类型: Article,,卷期:2010年20-15]
- Potent inhibitors of PLK1 with acceptable solubility, mouse iv clearance, and reduced CYP450 inhibition were identified. Drug-like properties were improved using a heteroaryl ring as a functional handle for manipulation ...
|