- Potent triazolyl-proline-based inhibitors of HCVNS3 protease
[作者:Naud, J; Lemke, C; Goudreau, N; Beaulieu, E; White, PD; Llinas-Brunet, M; Forgione, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3400-3404 , 文章类型: Article,,卷期:2008年18-11]
- The design and synthesis of tripeptide-based inhibitors of the HCV NS3 protease containing a novel P2-triazole is described. Replacement of the P2 quinoline with a triazole moiety provided a versatile handle which could ...
- 4-methyl-5-phenyl triazoles as selective inhibitors of 11 beta-hydroxysteroid dehydrogenase type I
[作者:Zhu, YP; Olson, SH; Hermanowski-Vosatka, A; Mundt, S; Shah, K; Springer, M; Thieringer, R; Wright, S; Xiao, J; Zokian, H; Balkovec, JM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3405-3411 , 文章类型: Article,,卷期:2008年18-11]
- 4-Methyl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1). They were active in vitro and in an in vivo mouse pharmacodynamic (PD) model. The...
- Phenylcyclobutyl triazoles as selective inhibitors of 11 beta-hydroxysteroid dehydrogenase type I
[作者:Zhu, YP; Olson, SH; Graham, D; Patel, G; Hermanowski-Vosatka, A; Mundt, S; Shah, K; Springer, M; Thieringer, R; Wright, S; Xiao, JY; Zokian, H; Dragovic, J; Balkovec, JM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3412-3416 , 文章类型: Article,,卷期:2008年18-11]
- 3-(Phenylcyclobutyl)-1,2,4-triazoles were identified as selective inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1). These were active both in vitro and in an in vivo mouse pharmacodynamic (PD) mod...
- New anti-inflammatory ergostane-type ecdysteroids from the sclerotium of Polyporus umbellatus
[作者:Sun, Y; Yasukawa, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3417-3420 , 文章类型: Article,,卷期:2008年18-11]
- Bioassay-guided fractionation of the ethyl acetate extract from the sclerotium of Polyporus umbellatus resulted in the isolation of three new ergostane-type ecdysteroids, named polyporoid A (1), B (2), and C (3), togethe...
- Novel HCV NS5B polymerase inhibitors derived from 4-(1 ',1 '-dioxo-1 ',4 '-dihydro-1 'lambda(6)-benzo[1 ',2 ',4 ']thiadiazin-3 '-yl)-5-hydroxy-2H-pyridazin-3-ones: Part 4. Optimization of DMPK properties
[作者:Sergeeva, MV; Zhou, YF; Bartkowski, DM; Nolan, TG; Norris, DA; Okamoto, E; Kirkovsky, L; Kamran, R; LeBrun, LA; Tsan, M; Patel, R; Shah, AM; Lardy, M; Gobbi, A; Li, LS; Zhao, JJ; Bertolini, T; Stankovic, N; Sun, ZX; Murphy, DE; Webber, SE; Dragovich, PS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3421-3426 , 文章类型: Article,,卷期:2008年18-11]
- 5-Hydroxy-3(2H)-pyridazinone derivatives were investigated as potent inhibitors of genotype 1 HCV NS5B polymerase focusing on the optimization of their drug metabolism and pharmacokinetics (DMPK) profiles. This investiga...
- Design and synthesis of hydroxy-alkynoic acids and their methyl esters as novel activators of BK channels
[作者:Patil, S; Bukiya, AN; Li, W; Dopico, AM; Miller, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3427-3430 , 文章类型: Article,,卷期:2008年18-11]
- Physiological and pharmacological agents that activate large conductance, voltage-, and calcium- gated potassium (BK) channels located in the smooth muscle are effective vasodilators. Thus, activators of smooth muscle BK...
- Efficient synthesis and evaluation of bimodal ligand NETA
[作者:Chong, HS; Song, HA; Birch, N; Le, T; Lim, S; Ma, X,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3436-3439 , 文章类型: Article,,卷期:2008年18-11]
- The efficient and short synthetic route to the structurally novel bimodal ligand NETA for antibody-targeted radiation therapy (radioimmunotherapy, RIT) of cancer was developed. The structure of NETA was determined by X-r...
- Bis-tetrahydroisoquinoline derivatives: AG525E1, a new step in the search for non-quaternary non-peptidic small conductance Ca2+-activated K+ channel blockers
[作者:Graulich, A; Lamy, C; Alleva, L; Dilly, S; Chavatte, P; Wouters, J; Seutin, V; Liegeois, JF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3440-3445 , 文章类型: Article,,卷期:2008年18-11]
- So far, small conductance Ca2+-activated K+ channel (SK) blockers mostly consist of quaternary ammonium derivatives or peptides. Due to their physicochemical properties, these blockers are not suitable to study the physi...
- Novel HCV NS5B polymerase inhibitors derived from 4-(1 ',1 '-dioxo-1 ',4 '-dihydro-1 'lambda(6)-benzo[1 ',2 ',4 '] thiadiazin-3 '-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 3: Further optimization of the 2-, 6-, and 7 '-substituents and initial pharmacokinetic assessments
[作者:Li, LS; Zhou, YF; Murphy, DE; Stankovic, N; Zhao, JJ; Dragovich, PS; Bertolini, T; Sun, ZX; Ayida, B; Tran, CV; Ruebsam, F; Webber, SE; Shah, AM; Tsan, M; Showalter, RE; Patel, R; LeBrun, LA; Bartkowski, DM; Nolan, TG; Norris, DA; Kamran, R; Brooks, J; Sergeeva, MV; Kirkovsky, L; Zhao, Q; Kissinger, CR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3446-3455 , 文章类型: Article,,卷期:2008年18-11]
- 5-Hydroxy-3(2H)-pyridazinone derivatives were investigated as inhibitors of genotype 1 HCV NS5B polymerase. Lead optimization led to the discovery of compound 3a, which displayed potent inhibitory activities in biochemic...
- 2-trifluoroacetylthiophenes, a novel series of potent and selective class II histone deacetylase inhibitors
[作者:Jones, P; Bottomley, MJ; Carfi, A; Cecchetti, O; Ferrigno, F; Lo Surdo, P; Ontoria, JM; Rowley, M; Scarpelli, R; Schultz-Fademrecht, C; Steinkuhler, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3456-3461 , 文章类型: Article,,卷期:2008年18-11]
- The identification of class II HDAC inhibitors has been hampered by lack of efficient enzyme assays, in the preceding paper two assays have been developed to improve the efficiency of these enzymes: mutating an active si...
- Design, synthesis and in vitro antiprotozoal activity of benzimidazole-pentamidine hybrids
[作者:Torres-Gomez, H; Hernandez-Nunez, E; Leon-Rivera, I; Guerrero-Alvarez, J; Cedillo-Rivera, R; Moo-Puc, R; Argotte-Ramos, R; Rodriguez-Gutierrez, MD; Chan-Bacab, MJ; Navarrete-Vazquez, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3147-3151 , 文章类型: Article,,卷期:2008年18-11]
- A series of ten novel hybrids from benzimidazole and pentamidine were prepared using a short synthetic route. Each compound was tested in vitro against the protozoa Trichomonas vaginalis, Giardia lamblia, Entamoeba histo...
- 3,5-dihydro-imidazo[4,5-d]pyridazin-4-ones: A class of potent DPP-4 inhibitors
[作者:Eckhardt, M; Hauel, N; Himmelsbach, F; Langkopf, E; Nar, H; Mark, M; Tadayyon, M; Thomas, L; Guth, B; Lotz, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3158-3162 , 文章类型: Article,,卷期:2008年18-11]
- Systematic variations of the xanthine scaffold in close analogs of development compound BI 1356 led to the class of 3,5-dihydro-imidazo[4,5-d]pyridazin-4-ones which provided, after substituent screening, a series of high...
- Tetrahydro anthranilic acid as a surrogate for anthranilic acid: Application to the discovery of potent niacin receptor agonists
[作者:Raghavan, S; Tria, GS; Shen, HC; Ding, FX; Taggart, AK; Ren, N; Wilsie, LC; Krsmanovic, ML; Holt, TG; Wolff, MS; Waters, MG; Hammond, ML; Tata, JR; Colletti, SL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3163-3167 , 文章类型: Article,,卷期:2008年18-11]
- The design, synthesis, and biological activity of a series of cycloalkene acid-based niacin receptor agonists are described. This led to the discovery that tetrahydro anthranilic acid is an excellent surrogate for anthra...
- Pyridine amides as potent and selective inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1
[作者:Wang, HX; Ruan, ZM; Li, JJ; Simpkins, LM; Smirk, RA; Wu, SC; Hutchins, RD; Nirschl, DS; Van Kirk, K; Cooper, CB; Sutton, JC; Ma, ZP; Golla, R; Seethala, R; Salyan, MEK; Nayeem, A; Krystek, SR; Sheriff, S; Camac, DM; Morin, PE; Carpenter, B; Robl, JA; Zahler, R; Gordon, DA; Hamann, LG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3168-3172 , 文章类型: Article,,卷期:2008年18-11]
- Several series of pyridine amides were identified as selective and potent 11 beta-HSD1 inhibitors. The most potent inhibitors feature 2,6- or 3,5-disubstitution on the pyridine core. Various linkers (CH2SO2, CH2S, CH2O, ...
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