- Discovery of 4-aryl-2-oxo-2H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay
[作者：Kemnitzer, W; Jiang, SC; Zhang, H; Kasibhatla, S; Crogan-Grundy, C; Blais, C; Attardo, G; Denis, R; Lamothe, S; Gourdeau, H; Tseng, B; Drewe, J; Cai, SX,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5571-5575 , 文章类型： Article，,卷期：2008年18-20]
- As a continuation of our efforts to discover and develop the apoptosis inducing 4-aryl-4H-chromenes as potential anticancer agents, we explored the removal of the chiral center at the 4-position and prepared a series of ...
- Novel 5-HT1A/1B/1D receptors antagonists with potent 5-HT reuptake inhibitory activity
[作者：Serafinowska, HT; Blaney, FE; Lovell, PJ; Merlo, GG; Scott, CM; Smith, PW; Starr, KR; Watson, JM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5581-5585 , 文章类型： Article，,卷期：2008年18-20]
- Novel 2-methyl-5-quinolinyl-1-piperazinylalkyl-3,4-dihydro-2H-1,4-benzoxazin-3-ones showing high affinities for the 5-HT1A/1B/1D receptors coupled with potent 5-HT reuptake inhibitory activity have been discovered. This ...
- Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent
[作者：Pingali, H; Jain, M; Shah, S; Basu, S; Makadia, P; Goswami, A; Zaware, P; Patil, P; Godha, A; Giri, S; Goel, A; Patel, M; Patel, H; Patel, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5586-5590 , 文章类型： Article，,卷期：2008年18-20]
- A series of novel 1,3-dioxane-2-carboxylic acid derivatives containing alkyl chain tether and substituted phenyl group as a lipophilic tail have been prepared as agonists of PPAR alpha and gamma. c-5-[6-(4-Methanesulfony...
- Aminostyrylbenzofuran derivatives as potent inhibitors for A beta fibril formation
[作者：Byun, JH; Kim, H; Kim, Y; Mook-Jung, I; Kim, DJ; Lee, WK; Yoo, KH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5591-5593 , 文章类型： Article，,卷期：2008年18-20]
- The synthesis of a novel series of aminostyrylbenzofuran derivatives 1a-w and their inhibitory activities for A beta fibril formation were described. All the synthesized compounds were evaluated by thioflavin T (ThT) ass...
- PASS-assisted exploration of antidepressant activity of 1,3,4-trisubstituted-beta-lactam derivatives
[作者：Mittal, M; Goel, RK; Bhargava, G; Mahajan, MP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5347-5349 , 文章类型： Article，,卷期：2008年18-20]
- Assisted by PASS predictions, the antidepressant activity of 1,3,4-trisubstituted monocyclic beta-lactams in seasonal affective disorders is described. (C) 2008 Elsevier Ltd. All rights reserved.
- Development of mitochondria-targeted derivatives of resveratrol
[作者：Biasutto, L; Mattarei, A; Marotta, E; Bradaschia, A; Sassi, N; Garbisa, S; Zoratti, M; Paradisi, C,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5594-5597 , 文章类型： Article，,卷期：2008年18-20]
- To target natural polyphenols to the subcellular site where their redox properties might be exploited at best, that is, mitochondria, we have synthesised new proof-of-principle derivatives by linking resveratrol (3,4',5-...
- Small, non-peptide C5a receptor antagonists: Part 1
[作者：Blagg, J; Mowbray, C; Pryde, DC; Salmon, G; Schmid, E; Fairman, D; Beaumont, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5601-5604 , 文章类型： Article，,卷期：2008年18-20]
- The optimisation of a series of amides for C5a receptor binding and functional activity, and physicochemical properties is described. The initial hit, 1 (IC50 1 mu M), was discovered during high throughput screening, fro...
- Small, non-peptide C5a receptor antagonists: Part 2
[作者：Blagg, J; Mowbray, C; Pryde, D; Salmon, G; Fairman, D; Schmid, E; Beaumont, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5605-5608 , 文章类型： Article，,卷期：2008年18-20]
- Starting from 2, several highly potent C5a receptor antagonists were synthesised through alpha-amide substitution. Attempts to increase the polarity of these compounds through the introduction of basic centres or incorpo...
- Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1
[作者：Westaway, SM; Thompson, M; Rami, HK; Stemp, G; Trouw, LS; Mitchell, DJ; Seal, JT; Medhurst, SJ; Lappin, SC; Biggs, J; Wright, J; Arpino, S; Jerman, JC; Cryan, JE; Holland, V; Winborn, KY; Coleman, T; Stevens, AJ; Davis, JB; Gunthorpe, MJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5609-5613 , 文章类型： Article，,卷期：2008年18-20]
- 6-Phenylnicotinamide (2) was previously identified as a potent TRPV1 antagonist with activity in an in vivo model of inflammatory pain. Optimization of this lead through modi. cation of both the biaryl and heteroaryl com...
- The 'Ethereal' nature of TLR4 agonism and antagonism in the AGP class of lipid A mimetics
[作者：Bazin, HG; Murray, TJ; Bowen, WS; Mozaffarian, A; Fling, SP; Bess, LS; Livesay, MT; Arnold, JS; Johnson, CL; Ryter, KT; Cluff, CW; Evans, JT; Johnson, DA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5350-5354 , 文章类型： Article，,卷期：2008年18-20]
- To overcome the chemical and metabolic instability of the secondary fatty acyl residues in the AGP class of lipid A mimetics, the secondary ether lipid analogs of the potent TLR4 agonist CRX-527 (2) and TLR4 antagonist C...
- Studies on the synthesis of neamine-dinucleosides and neamine-PNA conjugates and their interaction with RNA
[作者：Mei, H; Xing, L; Cai, L; Jin, HW; Zhao, P; Yang, ZJ; Zhang, LR; Zhang, LH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5355-5358 , 文章类型： Article，,卷期：2008年18-20]
- Two types of neamine derivatives, neamine-dinucleotide conjugates 8a-g and neamine-PNA conjugates 12a-c and 14a-d, were synthesized. Compound 8a-g were synthesized by the condensation of azidoneamine with dinucleotide-5'...
- Engineering of avermectin biosynthetic genes to improve production of ivermectin in Streptomyces avermitilis
[作者：Li, M; Chen, Z; Lin, XP; Zhang, X; Song, Y; Wen, Y; Li, JL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5359-5363 , 文章类型： Article，,卷期：2008年18-20]
- Two new recombinants of avermectin polyketide synthases were constructed by domain and module swapping in Streptomyces avermitilis 73-12. However, only the strain, S. avermitilis OI-31, formed by domain substitution coul...
- Synthesis and biological evaluation of alkoxycoumarins as novel nematicidal constituents
[作者：Takaishi, K; Izumi, M; Baba, N; Kawazu, K; Nakajima, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5614-5617 , 文章类型： Article，,卷期：2008年18-20]
- We synthesized all of the monomethoxycoumarins, 5-alkoxycoumarins and their derivatives, and investigated their nematicidal activity against the phytopathogenic nematode, Bursaphelenchus xylophilus. Among the compounds, ...
- Discovery of pyrimidine benzimidazoles as Lck inhibitors: Part I
[作者：Zhang, GB; Ren, PD; Gray, NS; Sim, TB; Liu, Y; Wang, X; Che, JW; Tian, SS; Sandberg, ML; Spalding, TA; Romeo, R; Iskandar, M; Chow, D; Seidel, HM; Karanewsky, DS; He, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5618-5621 , 文章类型： Article，,卷期：2008年18-20]
- A series of 4-amino-6-benzimidazole-pyrimidines was designed to target lymphocyte-specific tyrosine kinase (Lck), a member of the Src kinase family. Highly efficient parallel syntheses were devised to prepare analogues f...
- bis-pyridinium cyclophanes: Novel ligands with high affinity for the blood-brain barrier choline transporter
[作者：Zhang, ZF; Lockman, PR; Mittapalli, RK; Allen, DD; Dwoskin, LP; Crooks, PA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5622-5625 , 文章类型： Article，,卷期：2008年18-20]
- A series of bis-pyridinium cyclophane analogs designed as conformationally restricted bis-quaternary ammonium compounds were evaluated for their affinity for the blood-brain barrier (BBB) choline transporter. All the cyc...
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