- Identification of iminooxothiazolidines as secreted frizzled related protein-1 inhibitors
[作者:Shi, MX; Stauffer, B; Bhat, R; Billiard, J; Ponce-De-Leon, H; Seestaller-Wehr, L; Fukayama, S; Mangine, A; Moran, R; Krishnamurthy, G; Bodine, P; Gopalsamy, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6337-6339 , 文章类型: Article,,卷期:2009年19-22]
- Secreted frizzled related protein-1 (sFRP-1) inhibitors have the potential to be used for the treatment of osteoporosis or other bone related disorders, since the level of sFRP-1 affects osteoblast apoptosis and prolifer...
- The design of potent and selective inhibitors of DPP-4: Optimization of ADME properties by amide replacements
[作者:Nordhoff, S; Bulat, S; Cerezo-Galvez, S; Hill, O; Hoffmann-Enger, B; Lopez-Canet, M; Rosenbaum, C; Rummey, C; Thiemann, M; Matassa, VG; Edwards, PJ; Feurer, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6340-6345 , 文章类型: Article,,卷期:2009年19-22]
- For a series of beta-homophenylalanine based inhibitors of dipeptidyl peptidase IV ADME properties were improved by the incorporation of amide replacements. These efforts led to a novel series of potent and selective inh...
- Synthesis and biological activity of dialkylphosphocholines
[作者:Lukac, M; Mrva, M; Fischer-Fodor, E; Lacko, I; Bukovsky, M; Miklasova, N; Ondriska, F; Devinsky, F,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6346-6349 , 文章类型: Article,,卷期:2009年19-22]
- A series of dialkylphosphocholines were prepared and evaluated for their biological activity. The antiprotozoal activity was determined against Acanthamoeba lugdunensis. Compound 15 exhibited excellent trophocidal activi...
- Inhibitors of bacterial N-succinyl-L,L-diaminopimelic acid desuccinylase (DapE) and demonstration of in vitro antimicrobial activity
[作者:Gillner, D; Armoush, N; Holz, RC; Becker, DP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6350-6352 , 文章类型: Article,,卷期:2009年19-22]
- The dapE-encoded N-succinyl-L,L-diaminopimelic acid desuccinylase (DapE) is a critical bacterial enzyme for the construction of the bacterial cell wall. A screen biased toward compounds containing zinc-binding groups (ZB...
- Design of novel alpha 7-subtype-preferring nicotinic acetylcholine receptor agonists: Application of docking and MM-PBSA computational approaches, synthetic and pharmacological studies
[作者:Grazioso, G; Pome, DY; Matera, C; Frigerio, F; Pucci, L; Gotti, C; Dallanoce, C; De Amici, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6353-6357 , 文章类型: Article,,卷期:2009年19-22]
- In the search for nicotinic acetylcholine receptor (nAChRs) agonists with a selective affinity for the homomeric alpha 7 channels, we carried out the virtual screening of a test set of potential nicotinic ligands, and ad...
- Histone deacetylase and microtubules as targets for the synthesis of releasable conjugate compounds
[作者:Passarella, D; Comi, D; Vanossi, A; Paganini, G; Colombo, F; Ferrante, L; Zuco, V; Danieli, B; Zunino, F,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6358-6363 , 文章类型: Article,,卷期:2009年19-22]
- Design and synthesis of an HDAC inhibitor and its merger with three tubulin binders to create releasable conjugate compounds is described. The biological evaluation includes: (a) in vitro reactivity with glutathione, (b)...
- Design, synthesis and bioevaluation of novel maleamic amino acid ester conjugates of 3,5-bisarylmethylene-4-piperidones as cytostatic agents
[作者:Youssef, D; Potter, E; Jha, M; De Clercq, E; Balzarini, J; Stables, JP; Jha, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6364-6367 , 文章类型: Article,,卷期:2009年19-22]
- A novel series of maleamic amino acid ester conjugates of 3,5-bisarylmethylene-4-piperidones were prepared to investigate the efficacy of micronutrient conjugation in enhancing cytotoxic potency by improving selectivity ...
- Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: Development of novel spiropiperidines
[作者:Burgey, CS; Potteiger, CM; Deng, JZ; Mosser, SD; Salvatore, CA; Yu, S; Roller, S; Kane, SA; Vacca, JP; Williams, TM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6368-6372 , 文章类型: Article,,卷期:2009年19-22]
- Several novel spiropiperidine-based CGRP receptor antagonists have been developed that maintain good potency and have reduced potential for metabolism. (C) 2009 Elsevier Ltd. All rights reserved.
- Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: Discovery of CCKR1 selectivity in a previously CCKR2-selective lead series
[作者:Pippel, M; Allison, BD; Phuong, VK; Li, L; Morton, MF; Prendergast, C; Wu, XD; Shankley, NP; Rabinowitz, MH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6373-6375 , 文章类型: Article,,卷期:2009年19-22]
- A series of CCK2R-selective anthranilic amides is shown to derive CCK1R affinity via selective substitution of the amide side chain. Thus, extending the length of the original benzamide side chain by a single methylene u...
- Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists II: Tuning of receptor selectivity and in vivo efficacy
[作者:Pippel, M; Boyce, K; Venkatesan, H; Phuong, VK; Yan, W; Barrett, TD; Lagaud, G; Li, L; Morton, MF; Prendergast, C; Wu, XD; Shankley, NP; Rabinowitz, MH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6376-6378 , 文章类型: Article,,卷期:2009年19-22]
- In the previous article we demonstrated how certain CCK2R-selective anthranilic amides could be structurally modified to afford high-affinity, selective CCK1R activity. We now describe our efforts at modulating and optim...
- Identification of the amino acid-AZT-phosphoramidase by affinity T7 phage display selection
[作者:Cheng, JL; Zhou, X; Chou, TF; Ghosh, B; Liu, BL; Wagner, CR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6379-6381 , 文章类型: Article,,卷期:2009年19-22]
- A CEM cell cDNA T7 phage display library was prepared and used to screen for activating enzymes of phosphoramidate prodrugs of AZT monophosphate. Although, inefficient compared to ribonucleotide based phosphoramidates, h...
- Antioxidant reactivity toward nitroxide probes anchored into human serum albumin. A new model for studying antioxidant repairing capacity of protein radicals
[作者:Aspee, A; Orrego, A; Alarcon, E; Lopez-Alarcon, C; Poblete, H; Gonzalez-Nilo, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6382-6385 , 文章类型: Article,,卷期:2009年19-22]
- A new strategy to evaluate accessibility of antioxidants to radical proteins has been developed using nitroxide prefluorescent probes anchored into human serum albumin (HSA). Binding association constants for the nitroxi...
- Design and synthesis of cell potent BACE-1 inhibitors: Structure-activity relationship of P1 ' substituents
[作者:Sealy, JM; Truong, AP; Tso, L; Probst, GD; Aquino, J; Hom, RK; Jagodzinska, BM; Dressen, D; Wone, DWG; Brogley, L; John, V; Tung, JS; Pleiss, MA; Tucker, JA; Konradi, AW; Dappen, MS; Toth, G; Pan, H; Ruslim, L; Miller, J; Bova, MP; Sinha, S; Quinn, KP; Sauer, JM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6386-6391 , 文章类型: Article,,卷期:2009年19-22]
- Using structure-guided design, hydroxyethylamine BACE-1 inhibitors were optimized to nanomolar A beta cellular inhibition with selectivity against cathepsin-D. X-ray crystallography illuminated the S1' residues critical ...
- Pyrene-labeled deoxyguanosine as a fluorescence sensor to discriminate single and double stranded DNA structures: Design of ends free molecular beacons
[作者:Matsumoto, K; Shinohara, Y; Bag, SS; Takeuchi, Y; Morii, T; Saito, Y; Saito, I,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6392-6395 , 文章类型: Article,,卷期:2009年19-22]
- A novel fluorescent DNA probe containing pyrene-labeled C8 alkylamino-substituted 2'-deoxyguanosine was designed in order to discriminate single stranded and double stranded regions in DNA. This fluorescent sensor was us...
- Stereoselective total synthesis of a potent natural antifungal compound (6S)-5,6,dihydro-6-[(2R)-2-hydroxy-6-phenyl hexyl]-2H-pyran-2-one
[作者:Das, B; Laxminarayana, K; Krishnaiah, M; Kumar, DN,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6396-6398 , 文章类型: Article,,卷期:2009年19-22]
- A practical stereoselective synthesis of (6S)-5,6,dihydro-6-[(2R)-2-hydroxy-6-phenyl hexyl]-2H-pyran-2-one (1), a potent natural antifungal compound, is described. The sequence involves diastereoselective iodine-induced ...
- Imidazopyridine-5,6,7,8-tetrahydro-8-quinolinamine derivatives with potent activity against HIV-1
[作者:Gudmundsson, KS; Boggs, SD; Catalano, JG; Svolto, A; Spaltenstein, A; Thomson, M; Wheelan, P; Jenkinson, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6399-6403 , 文章类型: Article,,卷期:2009年19-22]
- Synthesis of several novel imidazopyridine-5,6,7,8-tetrahydro-8-quinolinamine derivatives with potent activity against HIV are described. Synthetic approaches allowing for variation of the substitution pattern are outlin...
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