- Discovery of a novel series of nonacidic benzofuran EP(1) receptor antagonists
[作者:Allan, AC; Billinton, A; Brown, SH; Chowdhury, A; Eatherton, AJ; Fieldhouse, C; Giblin, GMP; Goldsmith, P; Hall, A; Hurst, DN; Naylor, A; Rawlings, DA; Sime, M; Scoccitti, T; Theobald, PJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4343-4348 , 文章类型: Article,,卷期:2011年21-14]
- We describe the discovery and optimization of a novel series of benzofuran EP(1) antagonists, leading to the identification of 26d, a novel nonacidic EP(1) antagonist which demonstrated efficacy in preclinical models of ...
- Exploration of antimicrobial and antioxidant potential of newly synthesized 2,3-disubstituted quinazoline-4(3H)-ones
[作者:Kumar, A; Sharma, P; Kumari, P; Kalal, BL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4353-4357 , 文章类型: Article,,卷期:2011年21-14]
- A series of 2-(chloromethyl)-3-(4-methyl-6-oxo-5-[(E)-phenyldiazenyl]-2-thioxo-5,6-dihydropyrimidine-1(2H)-yl)quinazoline-4(3H)-ones 9a-j was synthesized by treating 2-(chloroacetyl) amino benzoic acid with 3-amino-6-met...
- Use of the hydantoin isostere to produce inhibitors showing selectivity toward the vesicular glutamate transporter versus the obligate exchange transporter system x(c)(-)
[作者:Ahmed, SK; Etoga, JLG; Patel, SA; Bridges, RJ; Thompson, CM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4358-4362 , 文章类型: Article,,卷期:2011年21-14]
- Evidence was acquired prior to suggest that the vesicular glutamate transporter (VGLUT) but not other glutamate transporters were inhibited by structures containing a weakly basic a-amino group. To test this hypothesis, ...
- Thiophenyl oxime-derived phosphonates as nano-molar class C beta-lactamase inhibitors reducing MIC of imipenem against Pseudomonas aeruginosa and Acinetobacter baumannii
[作者:Tan, Q; Ogawa, AM; Raghoobar, SL; Wisniewski, D; Colwell, L; Park, YW; Young, K; Hermes, JD; DiNinno, FP; Hammonda, ML,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4363-4365 , 文章类型: Article,,卷期:2011年21-14]
- The preparation and characterization of a series of thiophenyl oxime phosphonate beta-lactamase inhibitors is described. A number of these analogs were potent and selective inhibitors of class C beta-lactamases from Pseu...
- Applying the pro-drug approach to afford highly bioavailable antagonists of P2Y(14)
[作者:Robichaud, J; Fournier, JF; Gagne, S; Gauthier, JY; Hamel, M; Han, YX; Henault, M; Kargman, S; Levesque, JF; Mamane, Y; Mancini, J; Morin, N; Mulrooney, E; Wu, J; Black, WC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4366-4368 , 文章类型: Article,,卷期:2011年21-14]
- Our series of competitive antagonists against the G-protein coupled receptor P2Y(14) were found to be highly shifted in the presence of serum (>99% protein bound). A binding assay using 2% human serum albumin (HSA) was d...
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