- Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors
[作者:Heim-Riether, A; Taylor, SJ; Liang, S; Gao, DA; Xiong, ZM; August, EM; Collins, BK; Farmer, BT; Haverty, K; Hill-Drzewi, M; Junker, HD; Margarit, SM; Moss, N; Neumann, T; Proudfoot, JR; Keenan, LS; Sekul, R; Zhang, Q; Li, J; Farrow, NA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5321-5324 , 文章类型: Article,,卷期:2009年19-18]
- Discovery and optimization of potency and selectivity of a non-Zn-chelating MMP-13 inhibitor with the aid of protein co-crystal structural information is reported. This inhibitor was observed to have a binding mode disti...
- Synthesis of novel pyrazole carboxamide derivatives and discovery of modulators for apoptosis or autophagy in A549 lung cancer cells
[作者:Ding, XL; Zhang, HY; Qi, L; Zhao, BX; Lian, S; Lv, HS; Miao, JY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5325-5328 , 文章类型: Article,,卷期:2009年19-18]
- A series of novel 3-aryl-1-arylmethyl-1H-pyrazole-5-carboxamide derivatives 3a-1, were synthesized by the reaction of 3-aryl-1-arylmethyl-1H-pyrazole-5-carbonyl chloride with substituted amine in excellent yields. The co...
- Discovery of a novel class of isoxazoline voltage gated sodium channel blockers
[作者:Shao, PP; Ye, F; Weber, AE; Li, XH; Lyons, KA; Parsons, WH; Garcia, ML; Priest, BT; Smith, MM; Felix, JP; Williams, BS; Kaczorowski, GJ; McGowan, E; Abbadie, C; Martin, WJ; McMasters, DR; Gao, YD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5329-5333 , 文章类型: Article,,卷期:2009年19-18]
- Analogs of the previously reported voltage gated sodium channel blocker CDA54 were prepared in which one of the amide functions was replaced with aromatic and non-aromatic heterocycles. Replacement of the amide with an a...
- Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist
[作者:Satoh, A; Nagatomi, Y; Hirata, Y; Ito, S; Suzuki, G; Kimura, T; Maehara, S; Hikichi, H; Satow, A; Hata, M; Ohta, H; Kawamoto, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5464-5468 , 文章类型: Article,,卷期:2009年19-18]
- We identified 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide 27 as a potent mGluR1 antagonist. The compound possessed excellent subtype selectivity and good PK profile in rats. It al...
- Dihydropyrazolopyrimidines containing benzimidazoles as K(V)1.5 potassium channel antagonists
[作者:Lloyd, J; Finlay, HJ; Atwal, K; Kover, A; Prol, J; Yan, L; Bhandaru, R; Vaccaro, W; Huynh, T; Huang, CS; Conder, M; Jenkins-West, T; Sun, HB; Li, DS; Levesque, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5469-5473 , 文章类型: Article,,卷期:2009年19-18]
- Dihydropyrazolopyrimidines with a C6 heterocycle substituent were found to have high potency for block of K(V)1.5. Investigation of the substitution in the benzimidazole ring and the substituent in the 5-position of the ...
- Discovery of isoxazole voltage gated sodium channel blockers for treatment of chronic pain
[作者:Shao, PP; Ye, F; Weber, AE; Li, XH; Lyons, KA; Parsons, WH; Garcia, ML; Priest, BT; Smith, MM; Felix, JP; Williams, BS; Kaczorowski, GJ; McGowan, E; Abbadie, C; Martin, WJ; McMasters, DR; Gao, YD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5334-5338 , 文章类型: Article,,卷期:2009年19-18]
- A series of novel isoxazole voltage gated sodium channel blockers have been synthesized and evaluated. Substitutions on the benzylic position of benzamide were investigated to determine their effect on Na(v)1.7 inhibitor...
- Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists
[作者:Suzuki, T; Kameda, M; Ando, M; Miyazoe, H; Sekino, E; Ito, S; Masutani, K; Kamijo, K; Takezawa, A; Moriya, M; Ito, M; Ito, J; Nakase, K; Matsushita, H; Ishihara, A; Takenaga, N; Tokita, S; Kanatani, A; Sato, N; Fukami, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5339-5345 , 文章类型: Article,,卷期:2009年19-18]
- Optimization of the lead 2a led to the identification of a novel diarylketoxime class of melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. Our focus was directed toward improvement of hERG activity and metab...
- Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT2c agonists
[作者:Andrews, MD; Green, MP; Allerton, CMN; Batchelor, DV; Blagg, J; Brown, AD; Gordon, DW; McMurray, G; Millns, DJ; Nichols, CL; Watson, L,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5346-5350 , 文章类型: Article,,卷期:2009年19-18]
- This Letter reports the design and synthesis of several novel series of piperazinyl pyrimidinones as 5-HT2C agonists. Several of the compounds presented exhibit good in vitro potency and selectivity over the closely rela...
- Bioisosteric replacement of the hydrazide pharmacophore of the cannabinoid-1 receptor antagonist SR141716A. Part I: Potent, orally-active 1,4-disubstituted imidazoles
[作者:Dow, RL; Hadcock, JR; Scott, DO; Schneider, SR; Paight, ES; Iredale, PA; Carpino, PA; Griffith, DA; Hammond, M; DaSilva-Jardine, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5351-5354 , 文章类型: Article,,卷期:2009年19-18]
- A new series of CB1 receptor antagonists incorporating an imidazole-based isosteric replacement for the hydrazide moiety of rimonabant (SR141716) is disclosed. Members of this imidazole series possess potent/selective bi...
- Spiro-naphthyridinone piperidines as inhibitors of S. aureus and E. coli enoyl-ACP reductase (FabI)
[作者:Sampson, PB; Picard, C; Handerson, S; McGrath, TE; Domagala, M; Leeson, A; Romanov, V; Awrey, DE; Thambipillai, D; Bardouniotis, E; Kaplan, N; Berman, JM; Pauls, HW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5355-5358 , 文章类型: Article,,卷期:2009年19-18]
- Spiropiperidine naphthyridinone inhibitors of Staphylococcus aureus and Escherichia coli FabI have been prepared. Compounds 14a and 14c were identified as having sub-nanomolar E. coli FabI activity and are among the most...
- Design and synthesis of novel substituted quinazoline derivatives as antileishmanial agents
[作者:Agarwal, KC; Sharma, V; Shakya, N; Gupta, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5474-5477 , 文章类型: Article,,卷期:2009年19-18]
- 4-(Substituted-benzylidine)-2-substituted-5,6-dihydrobenzo[h]quinazoline (5a-p) and 4-(substituted-benzylidine)-2-substituted-3, 4, 5, 6-tetrahydrobenzo[h]quinazoline (6a-p) have been synthesized from 2-(substituted-benz...
- Antimicrobial dendrimer active against Escherichia coli biofilms
[作者:Hou, SY; Zhou, CH; Liu, ZG; Young, AW; Shi, ZH; Ren, DC; Kallenbach, NR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5478-5481 , 文章类型: Article,,卷期:2009年19-18]
- We have investigated the ability of a previously reported antimicrobial peptide dendrimer (RW)(4D) to inactivate Escherichia coli RP437 in planktonic culture and in biofilms. The results show that the dendrimer inhibits ...
- Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
[作者:Tian, XT; Qin, BJ; Lu, H; Lai, WH; Jiang, SB; Lee, KH; Chen, CH; Xie, L,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5482-5485 , 文章类型: Article,,卷期:2009年19-18]
- Two series (4 and 5) of diarylpyridine derivatives were designed, synthesized, and evaluated for anti-HIV-1 activity. The most promising compound, 5e, inhibited HIV-1 IIIB, NL4-3, and RTMDR1 with low nanomolar EC50 value...
- Solubilized phenyl-pyrazole ureas as potent, selective 5-HT2A inverse-agonists and their application as antiplatelet agents
[作者:Dosa, PI; Strah-Pleynet, S; Jayakumar, H; Casper, M; Decaire, M; Xiong, YF; Lehmann, J; Choi, K; Elwell, K; Wong, A; Webb, RR; Adams, JW; Ramirez, J; Richman, JG; Thomsen, W; Semple, G; Teegarden, BR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5486-5489 , 文章类型: Article,,卷期:2009年19-18]
- Potent 5-HT2A inverse-agonists containing phenyl-pyrazole ureas with an amino side chain were identified. Optimization of this series resulted in selective compounds that proved effective in modulating 5HT-induced amplif...
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