- 6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha(1A) adrenoceptor partial agonists
[作者:Roberts, LR; Fish, PV; Storer, RI; Whitlock, GA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3113-3117 , 文章类型: Article,,卷期:2009年19-11]
- Novel pyrroloimidazoles have been identified as potent partial agonists of the alpha(1A) adrenergic receptor, with good selectivity over the alpha(1B), alpha(1D) and alpha(2A) receptor subtypes. Pyrimidine 19 possessed a...
- Potent and selective alpha(1A) adrenoceptor partial agonists-Novel imidazole frameworks
[作者:Whitlock, GA; Brennan, PE; Roberts, LR; Stobie, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3118-3121 , 文章类型: Article,,卷期:2009年19-11]
- Novel imidazole frameworks have been identified as potent partial agonists of the alpha(1A) adrenergic receptor, with good selectivity over the alpha(1B), alpha(1D) and alpha(2A) receptor sub-types. Nitrile 28 possessed ...
- The application of the phosphoramidate ProTide approach confers micromolar potency against Hepatitis C virus on inactive agent 4 '-azidoinosine: Kinase bypass on a dual base/sugar modified nucleoside
[作者:McGuigan, C; Daverio, F; Najera, I; Martin, JA; Klumpp, K; Smith, DB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3122-3124 , 文章类型: Article,,卷期:2009年19-11]
- Novel phosphoramidate ProTides derived from 4'-azidoinosine have been prepared and evaluated in the replicon assay against hepatitis C Virus (HCV). The parent nucleoside analogue is inactive in this assay, while the ProT...
- Synthesis of yashabushidiol and its analogues and their cytotoxic activity against cancer cell lines
[作者:Narasimhulu, M; Reddy, TS; Mahesh, KC; Krishna, AS; Rao, JV; Venkateswarlu, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3125-3127 , 文章类型: Article,,卷期:2009年19-11]
- A total synthesis of yashabushidiol (1a), a linear diarylheptanoid having 1,3-diol system and its analogues has been achieved by alkynylation of 3-hydroxy-5-phenyl pentanal with substituted phenyl acetylenes. All the com...
- Chloro-oxime derivatives as novel small molecule chaperone amplifiers
[作者:Zhou, YF; Vu, K; Chen, YS; Pham, J; Brady, T; Liu, G; Chen, JH; Nam, J; Reddy, PSMM; Au, QY; Yoon, IS; Tremblay, MH; Yip, G; Cher, C; Zhang, B; Barber, JR; Ng, SC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3128-3135 , 文章类型: Article,,卷期:2009年19-11]
- Chloro-oxime derivatives were investigated as novel small molecule chaperone amplifiers. Lead optimization led to the discovery of compounds that displayed potent HSF1 activation activity, significant cytoprotection in M...
- Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase
[作者:Patnaik, S; Stevens, KL; Gerding, R; Deanda, F; Shotwell, JB; Tang, J; Hamajima, T; Nakamura, H; Leesnitzer, MA; Hassell, AM; Shewchuck, LM; Kumar, R; Lei, HS; Chamberlain, SD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3136-3140 , 文章类型: Article,,卷期:2009年19-11]
- Exploration of the SAR around a series of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines led to the discovery of novel pyrrolopyridine inhibitors of the IGF-1R tyrosine kinase. Several compounds demonstrated nanomolar pote...
- NO donors. Part 18: Bioactive metabolites of GTN and PETN-Synthesis and vasorelaxant properties
[作者:Lange, K; Koenig, A; Roegler, C; Seeling, A; Lehmann, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3141-3144 , 文章类型: Article,,卷期:2009年19-11]
- The vasodilators glyceryl trinitrate (GTN) and pentaerythrityl tetranitrate (PETN) are supposed to be degraded in vivo to the lower nitrates PETriN, PEDN, PEMN, 1,2-GDN, 1,3-GDN, 1-GMN, and 2-GMN. We synthesized these bi...
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