- Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H-3 receptor inverse agonists
[作者:Mizutani, T; Nagase, T; Ito, S; Miyamoto, Y; Tanaka, T; Takenaga, N; Tokita, S; Sato, N,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6041-6045 , 文章类型: Article,,卷期:2008年18-23]
- Novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives were identified as potent human H-3 receptor inverse agonists. After systematic modi. cation of lead 5a, the potent and selective analog 5r was identified. ...
- Pterocarpans and flavanones from Sophora flavescens displaying potent neuraminidase inhibition
[作者:Ryu, YB; Curtis-Long, MJ; Kim, JH; Jeong, SH; Yang, MS; Lee, KW; Lee, WS; Park, KH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6046-6049 , 文章类型: Article,,卷期:2008年18-23]
- Pterocarpans (1-3) and flavanones (4-10) were isolated from Sophora flavescens and screened for their ability to inhibit neuraminidase (an enzyme crucial in the proliferation of the influenza virus). The majority of inhi...
- Pyrrospirones A and B, apoptosis inducers in HL-60 cells, from an endophytic fungus, Neonectria ramulariae Wollenw KS-246
[作者:Shiono, Y; Shimanuki, K; Hiramatsu, F; Koseki, T; Tetsuya, M; Fujisawa, N; Kimura, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6050-6053 , 文章类型: Article,,卷期:2008年18-23]
- Pyrrospirones A and B have been isolated from unpolished rice cultures of the endophytic fungus Neonectria ramulariae Wollenw KS-246. Their absolute stereostructures (1 and 2) were elucidated through spectroscopic method...
- Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors
[作者:Bannwart, LM; Carter, DS; Cai, HY; Choy, JC; Greenhouse, R; Jaime-Figueroa, S; Iyer, PS; Lin, CJ; Lee, EK; Lucas, MC; Lynch, SM; Madera, AM; Moore, A; Ozboya, K; Raptova, L; Roetz, R; Schoenfeld, RC; Stein, KA; Steiner, S; Villa, M; Weikert, RJ; Zhai, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6062-6066 , 文章类型: Article,,卷期:2008年18-23]
- A series of 3,3-disubstituted pyrrolidine monoamine triple reuptake inhibitors were discovered. Analogues with low nanomolar potency, good human in vitro microsomal stability and in vitro permeability, and low drug-drug ...
- Synthesis and characterization of novel natural product-Gd(III) MRI contrast agent conjugates
[作者:Efthimiadou, EK; Katsarou, ME; Fardis, M; Zikos, C; Pitsinos, EN; Kazantzis, A; Leondiadis, L; Sagnou, M; Vourloumis, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6058-6061 , 文章类型: Article,,卷期:2008年18-23]
- Several novel gadolinium chelates conjugated with paclitaxel, colchicine and thyroxine have been prepared as MRI contrast agents targeted to tubulin and thyroxine-binding globulin, respectively. (C) 2008 Elsevier Ltd. Al...
- Synthesis and activity of novel 1-or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors
[作者:Zhang, PW; Terefenko, EA; McComas, CC; Mahaney, PE; Vu, A; Trybulski, E; Koury, E; Johnston, G; Bray, J; Deecher, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6067-6070 , 文章类型: Article,,卷期:2008年18-23]
- A series of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors was discovered. Several compounds such as 15 and 20 showed good hNET potency. Compoun...
- Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): Structure-activity relationships and strategies for the elimination of reactive metabolite formation
[作者:Walker, DP; Bi, FC; Kalgutkar, AS; Bauman, JN; Zhao, SX; Soglia, JR; Aspnes, GE; Kung, DW; Klug-McLeod, J; Zawistoski, MP; McGlynn, MA; Oliver, R; Dunn, M; Li, JC; Richter, DT; Cooper, BA; Kath, JC; Hulford, CA; Autry, CL; Luzzio, MJ; Ung, EJ; Roberts, WG; Bonnette, PC; Buckbinder, L; Mistry, A; Griffor, MC; Han, S; Guzman-Perez, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6071-6077 , 文章类型: Article,,卷期:2008年18-23]
- The synthesis and SAR for a series of diaminopyrimidines as PYK2 inhibitors are described. Using a combination of library and traditional medicinal chemistry techniques, a FAK-selective chemical series was transformed in...
- Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors
[作者:Scarpelli, R; Di Marco, A; Ferrigno, F; Laufer, R; Marcucci, I; Muraglia, E; Ontoria, JM; Rowley, M; Serafini, S; Steinkuhler, C; Jones, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6078-6082 , 文章类型: Article,,卷期:2008年18-23]
- 5-(Trifluoroacetyl)thiophene-2-carboxamides were found to be potent and selective class II HDAC inhibitors. This paper describes their further development and the investigation on the cause for the lack of cell-based act...
- 2-Aminobenzimidazoles as potent ITK antagonists: trans-stilbene-like moieties targeting the kinase specificity pocket
[作者:Lo, HY; Bentzien, J; Fleck, RW; Pullen, SS; Khine, HH; Woska, JR; Kugler, SZ; Kashem, MA; Takahashi, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6218-6221 , 文章类型: Article,,卷期:2008年18-23]
- Based on the information from molecular modeling and X-ray crystal structures, the kinase specificity pocket of ITK could be occupied upon extension of the right-hand-side of the 2-benzimidazole core of the inhibitors. 2...
- Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists
[作者:Morales-Ramos, AI; Mecom, JS; Kiesow, TJ; Graybill, TL; Brown, GD; Aiyar, NV; Davenport, EA; Kallal, LA; Knapp-Reed, BA; Li, P; Londregan, AT; Morrow, DM; Senadhi, S; Thalji, RK; Zhao, S; Burns-Kurtis, CL; Marino, JP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6222-6226 , 文章类型: Article,,卷期:2008年18-23]
- High-throughput screening of the GSK compound collection against the P2Y1 receptor identified a novel series of tetrahydro-4-quinolinamine antagonists. Optimal substitution around the piperidine group was pivotal for ens...
- Synthetic chalcones as efficient inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatase PtpA
[作者:Chiaradia, LD; Mascarello, A; Purificacao, M; Vernal, J; Cordeiro, MNS; Zenteno, ME; Villarino, A; Nunes, RJ; Yunes, RA; Terenzi, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6227-6230 , 文章类型: Article,,卷期:2008年18-23]
- In the search for lead compounds for new drugs for tuberculosis, the activity of 38 synthetic chalcones were assayed for their potential inhibitory action towards a protein tyrosine phosphatase from Mycobacterium tubercu...
- Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK)
[作者:Farmer, LJ; Bemis, G; Britt, SD; Cochran, J; Connors, M; Harrington, EM; Hoock, T; Markland, W; Nanthakumar, S; Taslimi, P; Ter Haar, E; Wang, J; Zhaveri, D; Salituro, FG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6231-6235 , 文章类型: Article,,卷期:2008年18-23]
- A series of SYK inhibitors based on the phenylamino pyrimidine thiazole lead 4 were prepared and evaluated for biological activity. Lead optimization provided compounds with nanomolar K-i's against SYK and potent inhibit...
- Modifications of the isonipecotic acid fragment of SNS-032: Analogs with improved permeability and lower efflux ratio
[作者:Fan, JF; Fahr, B; Stockett, D; Chan, E; Cheeti, S; Serafimova, I; Lu, YF; Pham, P; Walker, DH; Hoch, U; Choong, IC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6236-6239 , 文章类型: Article,,卷期:2008年18-23]
- Modifications of the isonipecotic acid fragment of SNS-032 results in analogs which are more permeable and lower effluxed than SNS-032. The enantiomerically pure synthesis and the in vivo pro. le of analog 20 is describe...
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