- Synthesis of cinnamoyl ketoamides as hybrid structures of antioxidants and calpain inhibitors
[作者:Yoo, YJ; Nama, DH; Jung, SY; Jang, JW; Kim, HJ; Jin, C; Pae, AN; Lee, YS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2850-2854 , 文章类型: Article,,卷期:2011年21-10]
- The excessive calpain activation causes serious cellular damage or even cell death in neurological disorders such as stroke and Alzheimer's disease. Oxidative stress has also been implicated in the initiation or progress...
- Synthesis, structure-activity relationship of novel substituted 4H-chromen-1,2,3,4-tetrahydropyrimidine-5-carboxylates as potential anti-mycobacterial and anticancer agents
[作者:Raju, BC; Rao, RN; Suman, P; Yogeeswari, P; Sriram, D; Shaik, TB; Kalivendi, SV,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2855-2859 , 文章类型: Article,,卷期:2011年21-10]
- Series of 4H-chromen-1,2,3,4-tetrahydropyrimidine-5-carboxylate derivatives 7a-7zb, 8a-8d and 9a-9d were synthesized and screened for their in vitro anti-mycobacterial activity against Mycobacterium tuberculosis H(37)Rv ...
- Design of novel and potent cPLA(2)alpha inhibitors containing an alpha-methyl-2-ketothiazole as a metabolically stable serine trap
[作者:Mete, A; Andrews, G; Bernstein, M; Connolly, S; Hartopp, P; Jackson, CG; Lewis, R; Martin, I; Murray, D; Riley, R; Robinson, DH; Smith, GM; Wells, E; Withnall, WJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3128-3133 , 文章类型: Article,,卷期:2011年21-10]
- We report the design of novel, potent cPLA(2)alpha inhibitors that possess an alpha-methyl-2-ketothiazole that acts as a serine-reactive moiety. We describe the optimization of the series for potency and metabolic stabil...
- Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control
[作者:Semple, G; Ren, A; Fioravanti, B; Pereira, G; Calderon, I; Choi, K; Xiong, YF; Shin, YJ; Gharbaoui, T; Sage, CR; Morgan, M; Xing, C; Chu, ZL; Leonard, JN; Grottick, AJ; Al-Shamma, H; Liang, Y; Demarest, KT; Jones, RM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3134-3141 , 文章类型: Article,,卷期:2011年21-10]
- We herein outline the design of a new series of agonists of the pancreatic and GI-expressed orphan G-protein coupled receptor GPR119, a target that has been of significant recent interest in the field of metabolism, star...
- SAR studies on a series of N-benzyl-4-heteroaryl-1-(phenylsulfonyl)piperazine-2-carboxamides: Potent inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus
[作者:Gentles, RG; Ding, M; Zheng, XF; Chupak, L; Poss, MA; Beno, BR; Pelosi, L; Liu, MP; Lemm, J; Wang, YK; Roberts, S; Gao, M; Kadow, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3142-3147 , 文章类型: Article,,卷期:2011年21-10]
- Described herein is the initial optimization of (+/-) N-benzyl-4-heteroaryl-1-(phenylsulfonyl)piperazine-2-carboxamide (1), a hit discovered in a high throughput screen run against the NS5B polymerase enzyme of the hepat...
- Synthesis and in vitro antitubercular activity of ferrocene-based hydrazones
[作者:Mahajan, A; Kremer, L; Louw, S; Gueradel, Y; Chibale, K; Biot, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2866-2868 , 文章类型: Article,,卷期:2011年21-10]
- We report here the synthesis and in vitro antitubercular activity of a new series of ferrocenyl derivatives. The quinoline-ferrocene hybrid 5 exhibited significant activity (MIC = 2.5-5 mu g/ml) against Mycobacterium tub...
- The Synthesis and evaluation of a novel class of (E)-3-(1-cyclohexyl-1H-pyrazol-3-yl)-2-methylacrylic acid Hepatitis C virus polymerase NS5B inhibitors
[作者:Martin, SW; Glunz, P; Beno, BR; Bergstrom, C; Romine, JL; Priestley, ES; Newman, M; Gao, M; Roberts, S; Rigat, K; Fridell, R; Qiu, D; Knobloh, G; Wang, YK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2869-2872 , 文章类型: Article,,卷期:2011年21-10]
- Herein we report the identification and evaluation of a novel series of (E)-3-(1-cyclohexyl-1H-pyrazol-3-yl)-2-methylacrylic acid derivatives identified from a deannulation study performed on the reported benzimidazole N...
- A novel series of piperazinyl-pyridine ureas as antagonists of the purinergic P2Y(12) receptor
[作者:Bach, P; Bostrom, J; Brickmann, K; van Giezen, JJJ; Hovland, R; Petersson, AU; Ray, A; Zetterberg, F,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2877-2881 , 文章类型: Article,,卷期:2011年21-10]
- A novel series of P2Y(12) antagonists for development of drugs within the antiplatelet area is presented. The synthesis of the piperazinyl-pyridine urea derivatives and their structure-activity relationships (SAR) are de...
- Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk)
[作者:Rosenthal, AS; Tanega, C; Shen, M; Mott, BT; Bougie, JM; Nguyen, DT; Misteli, T; Auld, DS; Maloney, DJ; Thomas, CJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3152-3158 , 文章类型: Article,,卷期:2011年21-10]
- Continued examination of substituted 6-arylquinazolin-4-amines as Clk4 inhibitors resulted in selective inhibitors of Clk1, Clk4, Dyrk1A and Dyrk1B. Several of the most potent inhibitors were validated as being highly se...
- Biological evaluation of 3 '-O-alkylated analogs of salacinol, the role of hydrophobic alkyl group at 3 ' position in the side chain on the alpha-glucosidase inhibitory activity
[作者:Tanabe, G; Otani, T; Cong, WY; Minematsu, T; Ninomiya, K; Yoshikawa, M; Muraoka, O,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3159-3162 , 文章类型: Article,,卷期:2011年21-10]
- Four analogs with 3'-O-alkyl groups (9a: CH3, 9b: C2H5, 9c: C13H27 or 9d: CH2Ph) instead of the 3'-O-sulfate anion in salacinol (1), a naturally occurring potent alpha-glucosidase inhibitor, were synthesized by the coupl...
- The discovery of novel 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamides as vasopressin V-1A receptor antagonists
[作者:Napier, S; Wishart, G; Arbuckle, W; Baker, J; Barn, D; Bingham, M; Brown, A; Byford, A; Claxton, C; Craighead, M; Buchanan, K; Fielding, L; Gibson, L; Goodwin, R; Goutcher, S; Irving, N; MacSweeney, C; Milne, R; Mort, C; Presland, J; Sloan, H; Thomson, F; Turnbull, Z; Young, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3163-3167 , 文章类型: Article,,卷期:2011年21-10]
- The discovery of a novel series of 8-azabicyclo[3.2.1] octan-3-yl)-3-(4-chlorophenyl) propanamide antagonists of the vasopressin V-1A receptor is disclosed. Compounds 47 and 48 were found to be high affinity, selective v...
- Synthesis of benzologues of Nitazoxanide and Tizoxanide: A comparative study of their in vitro broad-spectrum antiprotozoal activity
[作者:Navarrete-Vazquez, G; Chavez-Silva, F; Argotte-Ramos, R; Rodriguez-Gutierrez, MD; Chan-Bacab, MJ; Cedillo-Rivera, R; Moo-Puc, R; Hernandez-Nunez, E,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3168-3171 , 文章类型: Article,,卷期:2011年21-10]
- We have synthesized two new benzologues of Nitazoxanide (NIT) and Tizoxanide (TIZ), using a short synthetic route. Both compounds were tested in vitro against six protozoa (Giardia intestinalis, Trichomonas vaginalis, En...
- Antiplasmodial and antitumor activity of dihydroartemisinin analogs derived via the aza-Michael addition reaction
[作者:Feng, TS; Guantai, EM; Nell, MJ; van Rensburg, CEJ; Hoppe, HC; Chibale, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2882-2886 , 文章类型: Article,,卷期:2011年21-10]
- A series of dihydroartemisinin derivatives were synthesized via an aza-Michael addition reaction to a dihydroartemisinin-based acrylate and were evaluated for antiplasmodial and antitumor activity. The target compounds s...
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