- 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: A novel class of Pim kinase inhibitors with potent cell antiproliferative activity
[作者:Pierre, F; Stefan, E; Nedellec, AS; Chevrel, MC; Regan, CF; Siddiqui-Jain, A; Macalino, D; Streiner, N; Drygin, D; Haddach, M; O'Brien, SE; Anderes, K; Ryckman, DM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6687-6692 , 文章类型: Article,,卷期:2011年21-22]
- A novel class of pan-Pim kinase inhibitors was designed by modifying the CK2 inhibitor CX-4945. Introduction of a triazole or secondary amide functionality on the C-7 position and 2'-halogenoanilines on C-5 resulted in p...
- Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11 beta-hydroxydehydrogenase 1 (11 beta-HSD1)
[作者:Wu, SC; Yoon, D; Chin, J; van Kirk, K; Seethala, R; Golla, R; He, B; Harrity, T; Kunselman, LK; Morgan, NN; Ponticiello, RP; Taylor, JR; Zebo, R; Harper, TW; Li, WY; Wang, MM; Zhang, LS; Sleczka, BG; Nayeem, A; Sheriff, S; Camac, DM; Morin, PE; Everlof, JG; Li, YX; Ferraro, CA; Kieltyka, K; Shou, W; Vath, MB; Zvyaga, TA; Gordon, DA; Robl, JA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6693-6698 , 文章类型: Article,,卷期:2011年21-22]
- Derived from the HTS hit 1, a series of hydroxyisoquinolines was discovered as potent and selective 11 beta-HSD1 inhibitors with good cross species activity. Optimization of substituents at the 1 and 4 positions of the i...
- Design, synthesis, and SAR studies of novel polycyclic acids as potent and selective inhibitors of human 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD-1)
[作者:Ye, XY; Chen, SY; Nayeem, A; Golla, R; Seethala, R; Wang, MM; Harper, T; Sleczka, BG; Li, YX; He, B; Kirby, M; Gordon, DA; Robl, JA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6699-6704 , 文章类型: Article,,卷期:2011年21-22]
- Starting from high throughput screening hit 2-adamantyl acetic acid 3, a series of polycyclic acids have been designed and synthesized as novel, potent, and selective inhibitors of human 11 beta-HSD1. Structure-activity ...
- Identification of a novel RAMP-independent CGRP receptor antagonist
[作者:Zartman, CB; Bell, IM; Gallicchio, SN; Graham, SL; Kane, SA; Mallee, JJ; Rutledge, RZ; Salvatore, CA; Vacca, JP; Williams, TM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6705-6708 , 文章类型: Article,,卷期:2011年21-22]
- Identification of an HIV integrase inhibitor with micromolar affinity for the CGRP receptor led to the discovery of a series of structurally novel CGRP receptor antagonists. Optimization of this series produced compound ...
- A novel potential therapeutic avenue for autism: Design, synthesis and pharmacophore generation of SSRIs with dual action
[作者:Ghoneim, OM; Ibrahim, DA; El-Deeb, IM; Lee, SH; Booth, RG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6714-6723 , 文章类型: Article,,卷期:2011年21-22]
- Autism symptoms are currently modulated by Selective Serotonin Reuptake Inhibitors (SSRIs). SSRIs slow onset of action limits their efficiency. The established synergistic activity of SSRIs and 5HT(1B/1D) autoreceptors a...
- Rational design of 2-pyrrolinones as inhibitors of HIV-1 integrase
[作者:Ma, KQ; Wang, PH; Fu, W; Wan, XL; Zhou, L; Chu, Y; Ye, DY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6724-6727 , 文章类型: Article,,卷期:2011年21-22]
- HIV-1 integrase is an essential enzyme for viral replication and a validated target for the development of drugs against AIDS. With an aim to discover new potent inhibitors of HIV-1 integrase, we developed a pharmacophor...
- Synthesis and antibacterial activity of N(4)-mono alkyl derivatives of novel glycopeptide LYV07ww01
[作者:Shao, C; Zhou, WC; Zhang, SL; Wei, W; Ruan, LG; Jin, YP; Sun, XQ; Huang, YQ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6732-6738 , 文章类型: Article,,卷期:2011年21-22]
- Thirty-one N(4)-mono alkyl derivatives of novel glycopeptide LYV07ww01 were synthesized by the reductive alkylation and their in vitro antibacterial activity was tested. The benzyl derivatives showed potent activity, esp...
- Discovery, synthesis and SAR analysis of novel selective small molecule S1P(4)-R agonists based on a (2Z,5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype
[作者:Urbano, M; Guerrero, M; Velaparthi, S; Crisp, M; Chase, P; Hodder, P; Schaeffer, MT; Brown, S; Rosen, H; Roberts, E,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6739-6745 , 文章类型: Article,,卷期:2011年21-22]
- High affinity and selective S1P(4) receptor (S1P(4)-R) small molecule agonists may be important proof-of-principle tools used to clarify the receptor biological function and effects to assess the therapeutic potential of...
- Effect of the leukotriene A(4) hydrolase aminopeptidase augmentor 4-methoxydiphenylmethane in a pre-clinical model of pulmonary emphysema
[作者:De Oliveira, EO; Wang, K; Kong, HS; Kim, S; Miessau, M; Snelgrove, RJ; Shim, YM; Paige, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6746-6750 , 文章类型: Article,,卷期:2011年21-22]
- The leukotriene A(4) hydrolase enzyme is a dual functioning enzyme with the following two catalytic activities: an epoxide hydrolase function that transforms the lipid metabolite leukotriene A(4) to leukotriene B(4) and ...
- Designing 2-aminoimidazole alkaloids analogs with anti-biofilm activities: Structure-activities relationships of polysubstituted triazoles
[作者:Linares, D; Bottzeck, O; Pereira, O; Praud-Tabaries, A; Blache, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6751-6755 , 文章类型: Article,,卷期:2011年21-22]
- In order to discover novel probes that may help in the investigation and the control of bacterial biofilms, we have designed a library of triazole-based analogs of 2-aminoimidazole marine alkaloids: naamine A and isonaam...
- Synthesis and radioligand binding studies of bis-(8-isopropyl-isoquinolinium) derivatives as ligands for apamin-sensitive sites on cloned SK2 and SK3 channels
[作者:Badarau, E; Dilly, S; Dufour, F; Poncin, S; Seutin, V; Liegeois, JF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6756-6759 , 文章类型: Article,,卷期:2011年21-22]
- A structure-activity relationship study of N-methyl-laudanosine, a SK channel blocker, has indicated that the 6,7-dimethoxy group could be successfully replaced by a hydrophobic moiety such as an isopropyl substituent in...
- Synthesis and preliminary evaluation of amiloride analogs as inhibitors of the urokinase-type plasminogen activator (uPA)
[作者:Matthews, H; Ranson, M; Tyndall, JDA; Kelso, MJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6760-6766 , 文章类型: Article,,卷期:2011年21-22]
- A known side-activity of the oral potassium-sparing diuretic drug amiloride is inhibition of the enzyme urokinase-type plasminogen activator (uPA, K(i) = 7 mu M), a promising anticancer target. Several studies have demon...
- 4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors
[作者:Rossi, C; Fincham, CI; D'Andrea, P; Porcelloni, M; Ettorre, A; Mauro, S; Bigioni, M; Binaschi, M; Maggi, CA; Nardelli, F; Parlani, M; Fattori, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6767-6769 , 文章类型: Article,,卷期:2011年21-22]
- A series of N-substituted 4-alkylpiperidine hydroxamic acids, corresponding to the basic structure of histone deacetylase (HDAC) inhibitors (zinc binding moiety-linker-capping group) has been previously reported by our g...
- Synthesis and anti-HIV-1 activity of 4-substituted-7-(2 '-deoxy-2 '-fluoro-4 '-azido-beta-D-ribofuranosyl) pyrrolo[2,3-d] pyrimidine analogues
[作者:Guo, XH; Li, YJ; Tao, L; Wang, Q; Wang, SY; Hu, WD; Pan, ZL; Yang, QH; Cui, YM; Ge, ZP; Dong, LH; Yu, XJ; An, HY; Song, CJ; Chang, JB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6770-6772 , 文章类型: Article,,卷期:2011年21-22]
- Three novel 4-subsituted-7-(2'-deoxy-2'-fluoro-4'-azido-beta-D-ribofuranosyl)pyrrolo[2,3-d] pyrimidine analogues were designed, synthesized, and tested for their anti-HIV-1 activity. Initial biological studies indicated ...
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