- Discovery of tricyclic 5,6-dihydro-1H-pyridin-2-ones as novel, potent, and orally bioavailable inhibitors of HCV NS5B polymerase
[作者:Ruebsam, F; Murphy, DE; Tran, CV; Li, LS; Zhao, JJ; Dragovich, PS; McGuire, HM; Xiang, AX; Sun, ZX; Ayida, BK; Blazel, JK; Kim, SH; Zhou, YF; Han, Q; Kissinger, CR; Webber, SE; Showalter, RE; Shah, AM; Tsan, M; Patel, RA; Thompson, PA; LeBrun, LA; Hou, HYJ; Kamran, R; Sergeeva, MV; Bartkowski, DM; Nolan, TG; Norris, DA; Khandurina, J; Brooks, J; Okamoto, E; Kirkovsky, L,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6404-6412 , 文章类型: Article,,卷期:2009年19-22]
- A novel series of non-nucleoside small molecules containing a tricyclic dihydropyridinone structural motif was identified as potent HCV NS5B polymerase inhibitors. Driven by structure-based design and building on our pre...
- Design and synthesis of a simplified inhibitor for XIAP-BIR3 domain
[作者:Crisostomo, FRP; Feng, YM; Zhu, XJ; Welsh, K; An, J; Reed, JC; Huang, ZW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6413-6418 , 文章类型: Article,,卷期:2009年19-22]
- Based on tetrapeptide AVPI, we were able to design and synthesize a new simplified scaffold to inhibit the BIR3 domain of the XIAP protein at low micromolar range. The uncomplicated synthesis and the binding activity of ...
- Discovery and optimization of CRTH2 and DP dual antagonists
[作者:Liu, JW; Fu, Z; Wang, YC; Schmitt, M; Huang, A; Marshall, D; Tonn, G; Seitz, L; Sullivan, T; Tang, HL; Collins, T; Medina, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6419-6423 , 文章类型: Article,,卷期:2009年19-22]
- A series of phenylacetic acid derivatives was discovered as CRTH2 antagonists. Modification of the series led to compounds that are also antagonists of DP. Since activation of CRTH2 and DP are believed to play key roles ...
- Synthesis and biological activity of novel oxazolidinones
[作者:Das, B; Rajarao, AVS; Rudra, S; Yadav, A; Ray, A; Pandya, M; Rattan, A; Mehta, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6424-6428 , 文章类型: Article,,卷期:2009年19-22]
- A number of 5-substituted derivatives of Ranbezolid, a novel oxazolidinone were synthesized. Antibacterial activity of the compounds against a number of sensitive and resistant bacteria showed promising results. (C) 2009...
- Systematic study on the broad nucleotide triphosphate specificity of the pyrophosphorylase domain of the N-acetylglucosamine-1-phosphate uridyltransferase from Escherichia coli K12
[作者:Fang, JQ; Guan, WY; Cai, L; Gu, GF; Liu, XW; Wang, PG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6429-6432 , 文章类型: Article,,卷期:2009年19-22]
- N-Acetylglucosamine-1-phosphate uridyltransferase (GlmU) from Escherichia coli K12 is a bifunctional enzyme that catalyzes both the acetyltransfer and uridyltransfer reactions in the prokaryotic UDP-GlcNAc biosynthetic p...
- Synthesis of modified homo-N-nucleosides from the reactions of mesityl nitrile oxide with 9-allylpurines and their influence on lipid peroxidation and thrombin inhibition
[作者:Thalassitis, A; Hadjipavlou-Litina, DJ; Litinas, KE; Miltiadou, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6433-6436 , 文章类型: Article,,卷期:2009年19-22]
- 9-(3-Mesityl-4,5-dihydroisoxazol-5-yl) homo-N-nucleosides were prepared from the 1,3-dipolar cyclo-addition reactions of mesityl nitrile oxide with 9-allyl derivatives of 6-chloropurine, 6-piperidinylpurine, 6-morpholiny...
- Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors
[作者:Cho, TP; Jun, F; Li, H; Zhe, X; Ling, C; Xu, Z; Lei, Z; Bing, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6437-6440 , 文章类型: Article,,卷期:2009年19-22]
- A series of novel pyrrolopyridazine derivatives have been discovered to be HER-2 inhibitors. These compounds selectively inhibited HER-2 kinase activity at low nanomolar concentrations. Compound 7d was identified as a po...
- Rapid access towards follow-up NOP receptor agonists using a knowledge based approach
[作者:Palin, R; Clark, JK; Evans, L; Feilden, H; Fletcher, D; Hamilton, NM; Houghton, AK; Jones, PS; McArthur, D; Montgomery, B; Ratcliffe, PD; Smith, ARC; Sutherland, A; Weston, MA; Wishart, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6441-6446 , 文章类型: Article,,卷期:2009年19-22]
- A knowledge based approach has been adopted to identify novel NOP receptor agonists with simplified hydrophobes. Substitution of the benzimidazol-2-one piperidine motif with a range of hydrophobic groups and pharmacophor...
- Pyranocoumarins: A new class of anti-hyperglycemic and anti-dyslipidemic agents
[作者:Kumar, A; Maurya, RA; Sharma, S; Ahmad, P; Singh, AB; Bhatia, G; Srivastava, AK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6447-6451 , 文章类型: Article,,卷期:2009年19-22]
- A series of pyranocoumarin derivatives were synthesized and evaluated in vivo for their anti-hyperglycemic as well as anti-dyslipidemic activities. Compounds 7a, 7c, 8a, 8b, 8c, 8e and 8f have shown promising anti-hyperg...
- The discovery and optimisation of benzazepine sulfonamide and sulfones as potent agonists of the motilin receptor
[作者:Bailey, JM; Scott, JS; Basilla, JB; Bolton, VJ; Boyfield, I; Evans, DG; Fleury, E; Heightman, TD; Jarvie, EM; Lawless, K; Matthews, KL; McKay, F; Mok, H; Muir, A; Orlek, BS; Sanger, GJ; Stemp, G; Stevens, AJ; Thompson, M; Ward, J; Vaidya, K; Westaway, SM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3452-6458 , 文章类型: Article,,卷期:2009年19-22]
- Optimisation of a series of benzazepine sulfonamide hit compounds identified from high throughput screening led to the discovery of a new series of tractable, potent motilin receptor agonists. (C) 2009 Elsevier Ltd. All ...
- Synthesis and antitumor activities of 3-modified 2-methoxyestradiol analogs
[作者:Suwandi, LS; Agoston, GE; Shah, JH; Hanson, AD; Zhan, XGH; LaVallee, TM; Treston, AM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6459-6462 , 文章类型: Article,,卷期:2009年19-22]
- The syntheses of 2-methoxyestradiol analogs with modifications at the 3-position are described. The analogs were assessed for their antiproliferative, antiangiogenic, and estrogenic activities. Several lead substituents ...
- Synthesis of a novel C2/C2 '-aryl-substituted pyrrolo[2,1-c][1,4]benzodiazepine dimer prodrug with improved water solubility and reduced DNA reaction rate
[作者:Howard, PW; Chen, ZZ; Gregson, SJ; Masterson, LA; Tiberghien, AC; Cooper, N; Fang, M; Coffils, MJ; Klee, S; Hartley, JA; Thurston, DE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6463-6466 , 文章类型: Article,,卷期:2009年19-22]
- A prodrug form (17) of a novel C2/C2'-aryl-substituted pyrrolobenzodiazepine (PBD) dimer (16) has been synthesized by introducing sodium bisulfite groups to the C11/C11'-positions of the parent bis-imine. The prodrug for...
- Scaffold-based design and synthesis of potent N-type calcium channel blockers
[作者:Zamponi, GW; Feng, ZP; Zhang, LY; Pajouhesh, H; Ding, YB; Belardetti, F; Pajouhesh, H; Dolphin, D; Mitscher, LA; Snutch, TP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6467-6472 , 文章类型: Article,,卷期:2009年19-22]
- The therapeutic agents flunarizine and lomerizine exhibit inhibitory activities against a variety of ion channels and neurotransmitter receptors. We have optimized their scaffolds to obtain more selective N-type calcium ...
- Solid-phase synthesis of a library based on biphenyl-containing trypsin-like serine protease inhibitors
[作者:Shi, SH; Zhu, SR; Gerritz, SW; Rachwal, B; Ruan, ZM; Hutchins, R; Kakarla, R; Sofia, MJ; Sutton, J; Cheney, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6477-6480 , 文章类型: Article,,卷期:2009年19-22]
- The solid-phase synthesis of a library based on an unusual biphenyl-containing trypsin-like serine protease inhibitor is described. Key to this effort was the synthesis of a highly functionalized aryl boronic acid reagen...
- Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C (vol 19, pg 5392, 2009)
[作者:Guay, D; Beaulieu, C; Reddy, TJ; Zamboni, R; Methot, N; Rubin, J; Ethier, D; Percival, MD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6481-6481 , 文章类型: Correction,,卷期:2009年19-22]
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