- 7-Azaindole-3-acetic acid derivatives: Potent and selective CRTh2 receptor antagonists
[作者:Sandham, DA; Adcock, C; Bala, K; Barker, L; Brown, Z; Dubois, G; Budd, D; Cox, B; Fairhurst, RA; Furegati, M; Leblanc, C; Manini, J; Profit, R; Reilly, J; Stringer, R; Schmidt, A; Turner, KL; Watson, SJ; Willis, J; Williams, G; Wilson, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4794-4798 , 文章类型: Article,,卷期:2009年19-16]
- High throughput screening identified a 7-azaindole-3-acetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a highly selective compound with good functional potency for i...
- Dopamine D-3 receptor antagonists: The quest for a potentially selective PET ligand. Part one: Lead identification
[作者:Holmes, IP; Micheli, F; Gaines, S; Lorthioir, O; Watson, SP; Di Fabio, R; Gentile, G; Heidbreder, C; Savoia, C; Worby, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4799-4801 , 文章类型: Article,,卷期:2009年19-16]
- The synthesis and SAR of a new series of potent and selective dopamine D-3 receptor antagonists is reported. (C) 2009 Elsevier Ltd. All rights reserved.
- Carbonic anhydrase inhibitors. Inhibition of the beta-class enzyme from the pathogenic yeast Candida glabrata with anions
[作者:Innocenti, A; Leewattanapasuk, W; Muhlschlegel, FA; Mastrolorenzo, A; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4802-4805 , 文章类型: Article,,卷期:2009年19-16]
- A beta-carbonic anhydrase (CA, EC 4.2.1.1), the protein encoded by the NCE103 gene of Candida glabrata which also present in Candida albicans and Saccharomyces cerevisiae, was cloned, purified, characterized kinetically ...
- Structural and theoretical studies of [6-bromo-1-(4-fluorophenylmethyl)-4(1H)-quinolinon-3-yl)]-4-hydroxy-2-oxo-3-butenoic acid as HIV-1 integrase inhibitor
[作者:Vandurm, P; Cauvin, C; Guiguen, A; Georges, B; Le Van, K; Martinelli, V; Cardona, C; Mbemba, G; Mouscadet, JF; Hevesi, L; Van Lint, C; Wouters, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4806-4809 , 文章类型: Article,,卷期:2009年19-16]
- Ethyl [6-bromo-1-(4-fluorophenylmethyl)-4(1H)-quinolinon-3-yl]-4-hydroxy-2-oxo-3-butenoate 1 and [6-bromo-1-(4-fluorophenylmethyl)-4(1H)-quinolinon-3-yl)]-4-hydroxy-2-oxo-3-buteno c acid 2 were synthesized as potential H...
- Tricyclic indole and dihydroindole derivatives as new inhibitors of soluble guanylate cyclase
[作者:Spyridonidou, K; Fousteris, M; Antonia, M; Chatzianastasiou, A; Papapetropoulos, A; Nikolaropoulos, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4810-4813 , 文章类型: Article,,卷期:2009年19-16]
- The synthesis of new tricyclic fused indole and dihydroindole derivatives and preliminary results from their in vitro inhibitory activity against soluble guanylate cyclase (sGC) are presented. (C) 2009 Elsevier Ltd. All ...
- Esters of betulin and betulinic acid with amino acids have improved water solubility and are selectively cytotoxic toward cancer cells
[作者:Drag-Zalesinska, M; Kulbacka, J; Saczko, J; Wysocka, T; Zabel, M; Surowiak, P; Drag, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4814-4817 , 文章类型: Article,,卷期:2009年19-16]
- Betulin and betulinic acid are naturally occurring pentacyclic triterpenes showing cytotoxicity towards a number of cancer cell lines. Unfortunately they are practically insoluble in aqueous media and therefore their ove...
- From lead to preclinical candidate: Optimization of beta-homophenylalanine based inhibitors of dipeptidyl peptidase IV
[作者:Nordhoff, S; Lopez-Canet, M; Hoffmann-Enger, B; Bulat, S; Cerezo-Galvez, S; Hill, O; Rosenbaum, C; Rummey, C; Thiemann, M; Matassa, VG; Edwards, PJ; Feurer, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4818-4823 , 文章类型: Article,,卷期:2009年19-16]
- A series of highly potent and selective inhibitors of DPP-4 was optimized for ADMET properties. The effort resulted in the discovery of inhibitor 1g, that exhibits excellent efficacy in an oral glucose tolerance test and...
- Sulfonamides with the N-alkyl-N '-dialkylguanidine moiety as 5-HT7 receptor ligands
[作者:Zajdel, P; Subra, G; Verdie, P; Gabzdyl, E; Bojarski, AJ; Duszynska, B; Martinez, J; Pawlowski, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4827-4831 , 文章类型: Article,,卷期:2009年19-16]
- A series of arylsulfonamides containing guanidine incorporated in the structure of secondary amines (piperidine, piperazine) was synthesized on SynPhase Lanterns and evaluated for 5-HT1A, 5-HT2A, and 5-HT7 receptors. The...
- Novel inhibitors of the alpha v beta 3 integrin-lead identification strategy
[作者:Elliot, D; Henshaw, E; MacFaul, PA; Morley, AD; Newham, P; Oldham, K; Page, K; Rankine, N; Sharpe, P; Ting, A; Wood, CM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4832-4835 , 文章类型: Article,,卷期:2009年19-16]
- A novel approach to inhibition of the alpha v beta 3 integrin is described, which uses compounds designed to generate nM potency without using the arginine binding site. (C) 2009 Elsevier Ltd. All rights reserved.
- Functionalization of the A ring of pyridoacridine as a route toward greater structural diversity. Synthesis of an octacyclic analogue of eilatin
[作者:Bouffier, L; Dinica, R; Debray, J; Dumy, P; Demeunynck, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4836-4838 , 文章类型: Article,,卷期:2009年19-16]
- In an effort to increase the structural diversity of pyrido[4,3,2-kl] acridines, compounds containing amino substituents on the A ring were synthesized. The key-reactions involve regioselective electrophilic aromatic sub...
- Identification of new Hsp90 inhibitors by structure-based virtual screening
[作者:Hong, TJ; Park, H; Kim, YJ; Jeong, JH; Hahn, JS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4839-4842 , 文章类型: Article,,卷期:2009年19-16]
- Structure-based virtual screening identified pyrimidine-2,4,6-trione and 4H-1,2,4-triazole-3-thiol as novel scaffolds of Hsp90 ATPase inhibitors. Their binding modes in the ATP-binding pocket of Hsp90 were analyzed using...
- Synthesis, radiolabeling and preliminary in vivo evaluation of [F-18]FE-PE2I, a new probe for the dopamine transporter
[作者:Schou, M; Steiger, C; Varrone, A; Guilloteau, D; Halldin, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4843-4845 , 文章类型: Article,,卷期:2009年19-16]
- A new dopamine transporter (DAT) ligand, (E)-N-(3-iodoprop-2-enyl)-2 beta-carbofluoroethoxy-3 beta-(4'-methyl- phenyl) nortropane (FE-PE2I, 6), derived from PE2I (1), was prepared and found to be a potent inhibitor of ro...
- Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists
[作者:Biggadike, K; Caivano, M; Clackers, M; Coe, DM; Hardy, GW; Humphreys, D; Jones, HT; House, D; Miles-Williams, A; Skone, PA; Uings, I; Weller, V; Mclay, IM; Macdonald, SJF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4846-4850 , 文章类型: Article,,卷期:2009年19-16]
- Starting from a non-steroidal glucocorticoid agonist aryl pyrazole derivative, the NF kappa B agonist activity was optimised in an iterative process from pIC(50) 7.5 (for 7), to pIC(50) 10.1 (for 38E1). An explanation fo...
- In vivo targeting of tumor-associated carbonic anhydrases using acetazolamide derivatives
[作者:Ahlskog, JKJ; Dumelin, CE; Trussel, S; Marlind, J; Neri, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4851-4856 , 文章类型: Article,,卷期:2009年19-16]
- We describe the synthesis and characterization of two acetazolamide derivatives containing either a charged fluorophore or an albumin-binding moiety, which restrict binding to carbonic anhydrase IX and XII present on tum...
- Respiratory syncytial virus fusion inhibitors. Part 7: Structure-activity relationships associated with a series of isatin oximes that demonstrate antiviral activity in vivo
[作者:Sin, N; Venables, BL; Combrink, KD; Gulgeze, HB; Yu, KL; Civiello, RL; Thuring, J; Wang, XA; Yang, Z; Zadjura, L; Marino, A; Kadow, KF; Cianci, CW; Clarke, J; Genovesi, EV; Medina, I; Lamb, L; Krystal, M; Meanwell, NA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4857-4862 , 文章类型: Article,,卷期:2009年19-16]
- A series of bezimidazole-isatin oximes were prepared and profiled as inhibitors of respiratory syncytial virus (RSV) replication in cell culture. Structure-activity relationship studies were directed toward optimization ...
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