- Synthesis, structure-activity relationship and in vitro biological evaluation of N-arylethyl isoquinoline derivatives as Coxsackievirus B3 inhibitors
[作者:Wang, YX; Li, YH; Li, YH; Gao, RM; Wang, HQ; Liu, YX; Gao, LM; Lu, QN; Jiang, JD; Song, DQ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5787-5790 , 文章类型: Article,,卷期:2011年21-19]
- Currently, there is no approved antiviral drug for the infection caused by enteroviruses. A series of novel N-arylethyl isoquinoline derivatives defined with substituents on the ring A and C were designed, synthesized an...
- Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent gamma-secretase inhibitors
[作者:Aubele, DL; Truong, AP; Dressen, DB; Probst, GD; Bowers, S; Mattson, MN; Semko, CM; Sun, MH; Garofalo, AW; Konradi, AW; Sham, HL; Zmolek, W; Wong, K; Goldbach, E; Quinn, KP; Sauer, JM; Brigham, EF; Wallace, W; Nguyen, L; Bova, MP; Hemphill, SS; Basi, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5791-5794 , 文章类型: Article,,卷期:2011年21-19]
- The structure-activity relationship (SAR) of a novel, potent and metabolically stable series of sulfonamide-pyrazoles that attenuate beta-amyloid peptide synthesis via gamma-secretase inhibition is detailed herein. Sulfo...
- Synthesis of a series of gamma-amino alcohols comprising an N-methyl isoindoline moiety and their evaluation as NMDA receptor antagonists
[作者:Muller, A; Hofner, G; Renukappa-Gutke, T; Parsons, CG; Wanner, KT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5795-5799 , 文章类型: Article,,卷期:2011年21-19]
- We report a series of new stereoisomeric gamma-amino alcohols comprising an N-methyl isoindoline moiety as ligands for the ifenprodil binding site of the NMDA receptor. Among the four series of stereoisomers, 8a-c, 9a-c,...
- Synthesis and in vitro antiprotozoal activities of 5-phenyliminobenzo[a] phenoxazine derivatives
[作者:Shi, XL; Ge, JF; Liu, BQ; Kaiser, M; Wittlin, S; Brun, R; Ihara, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5804-5807 , 文章类型: Article,,卷期:2011年21-19]
- A series of 5-phenyliminobenzo[a]phenoxazine derivatives were synthesized. The in vitro antiprotozoal activities were evaluated against Plasmodium falciparum K1, Trypanosoma cruzi, Leishmania donovani and Trypanosoma bru...
- Exploration of pyridine containing heteroaryl analogs of biaryl ureas as DGAT1 inhibitors
[作者:Motiwala, H; Kandre, S; Birar, V; Kadam, KS; Rodge, A; Jadhav, RD; Reddy, MMK; Brahma, MK; Deshmukh, NJ; Dixit, A; Doshi, L; Gupte, A; Gangopadhyay, AK; Vishwakarma, RA; Srinivasan, S; Sharma, M; Nemmani, KVS; Sharma, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5812-5817 , 文章类型: Article,,卷期:2011年21-19]
- The diacylglycerol acyltransferase enzyme, DGAT1, presents itself as a potential target for obesity as this enzyme is dedicated to the final committed step in triglyceride biosynthesis. Biphenyl ureas, exemplified by com...
- Synthesis and evaluation of ferrocenoyl pentapeptide (Fc-KLVFF) as an inhibitor of Alzheimer's A beta(1-42) fibril formation in vitro
[作者:Wei, CW; Peng, Y; Zhang, L; Huang, QY; Cheng, M; Liu, YN; Li, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5818-5821 , 文章类型: Article,,卷期:2011年21-19]
- Aggregation and fibril formation of beta-amyloid peptides (A beta) is the key event in the pathogenesis of Alzheimer's disease. Many efforts have been made on the development of effective inhibitors to prevent A beta fib...
- Synthesis and acrosin inhibitory activities of substituted ethyl 5-(4-aminophenyl)-1H-pyrazole-3-carboxylate derivatives
[作者:Qi, JJ; Zhu, J; Liu, XF; Ding, LL; Zheng, CH; Han, GQ; Lv, JG; Zhou, YJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5822-5825 , 文章类型: Article,,卷期:2011年21-19]
- A series of novel ethyl 5-(4-aminophenyl)-1H-pyrazole-3-carboxylate derivatives were designed and synthesized and their in vitro acrosin inhibitory activities were evaluated. Most of the compounds exhibited acrosin inhib...
- Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma
[作者:Millan, DS; Ballard, SA; Chunn, S; Dybowski, JA; Fulton, CK; Glossop, PA; Guillabert, E; Hewson, CA; Jones, RM; Lamb, DJ; Napier, CM; Payne-Cook, TA; Renery, ER; Selby, MD; Tutt, MF; Yeadon, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5826-5830 , 文章类型: Article,,卷期:2011年21-19]
- In this Letter we present data for a novel series of ICS for the treatment of asthma. 'Inhalation by design' principles have been applied to a series of highly potent steroidal GR agonists, with a focus on optimising the...
- Anti-AIDS agents 87. New bio-isosteric dicamphanoyl-dihydropyranochromone (DCP) and dicamphanoyl-khellactone (DCK) analogues with potent anti-HIV activity
[作者:Liu, HS; Xu, SQ; Cheng, M; Chen, Y; Xia, P; Qian, KD; Xia, Y; Yang, ZY; Chen, CH; Morris-Natschke, SL; Lee, KH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5831-5834 , 文章类型: Article,,卷期:2011年21-19]
- Six 3'R,4'R-di-O-(S)-camphanoyl-2',2'-dimethyldihydropyrano[2,3-f] chromone (DCP) and two 3'R,4'R-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) derivatives were designed, synthesized, and evaluated for inhibition of HIV-...
- Solid-phase synthesis and pharmacological evaluation of novel nucleoside-tethered dinuclear platinum(II) complexes
[作者:D'Errico, S; Oliviero, G; Piccialli, V; Amato, J; Borbone, N; D'Atri, V; D'Alessio, F; Di Noto, R; Ruffo, F; Salvatore, F; Piccialli, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5835-5838 , 文章类型: Article,,卷期:2011年21-19]
- Three novel inosine-based dinuclear platinum complexes have been synthesized via a solid-phase strategy. In these compounds, the metal is linked both to the N-7 of the purine nucleus and to the terminal amine group of a ...
- Hydrazidomycins, cytotoxic alkylhydrazides from Streptomyces atratus
[作者:Ueberschaar, N; Ndejouong, BLT; Ding, L; Maier, A; Fiebig, HH; Hertweck, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5839-5841 , 文章类型: Article,,卷期:2011年21-19]
- Three unusual alkyhydrazide natural products, named hydrazidomycin A (1), B (2) and C (3), were isolated from the chloroform extract of a Streptomyces atratus culture, and their structures were elucidated by MS and NMR t...
- Synthesis and evaluation of compounds that induce readthrough of premature termination codons
[作者:Jung, ME; Ku, JM; Du, LT; Hu, HL; Gatti, RA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5842-5848 , 文章类型: Article,,卷期:2011年21-19]
- A structure-activity relationship (SAR) study was carried out to identify novel, small molecular weight compounds which induce readthrough of premature termination codons. In particular, analogs of RTC13, 1, were evaluat...
- Discovery of potent and novel S-nitrosoglutathione reductase inhibitors devoid of cytochrome P450 activities
[作者:Sun, XC; Qiu, J; Strong, SA; Green, LS; Wasley, JWF; Blonder, JP; Colagiovanni, DB; Mutka, SC; Stout, AM; Richards, JP; Rosenthal, GJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5849-5853 , 文章类型: Article,,卷期:2011年21-19]
- The pyrrole based N6022 was recently identified as a potent, selective, reversible, and efficacious S-nitrosoglutathione reductase (GSNOR) inhibitor and is currently undergoing clinical development for the treatment of a...
- Synthesis of a new trifluoromethylketone analogue of (L)-arginine and contrasting inhibitory activity against human arginase I and histone deacetylase 8
[作者:Ilies, M; Dowling, DP; Lombardi, PM; Christianson, DW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5854-5858 , 文章类型: Article,,卷期:2011年21-19]
- As part of our continuing search for new amino acid inhibitors of metalloenzymes, we now report the synthesis and biological evaluation of the trifluoromethylketone analogue of (L)-arginine, (S)-2-amino-8,8,8- trifluoro-...
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