- Fuscoside E: A strong anti-inflammatory diterpene from Caribbean octocoral Eunicea fusca
[作者：Reina, E; Puentes, C; Rojas, J; Garcia, J; Ramos, FA; Castellanos, L; Aragon, M; Ospina, LF,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5888-5891 , 文章类型： Article，,卷期：2011年21-19]
- The screen of 10 soft coral extracts collected from the Colombian Caribbean Sea in the TPA-induced ear edema model allowed us to identify Eunicea fusca extract among others as an interesting source of active compounds. T...
- Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II
[作者：Knaus, EE; Innocenti, A; Scozzafava, A; Supuran, CT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5892-5896 , 文章类型： Article，,卷期：2011年21-19]
- A series of compounds incorporating regioisomeric phenylethynylbenzenesulfonamide moieties has been investigated for the inhibition of four human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms, hCA I, II, IX and XII. Inhi...
- Synthesis and in-vitro anticancer activity of 3,5-bis(indolyl)-1,2,4-thiadiazoles
[作者：Kumar, D; Kumar, NM; Chang, KH; Gupta, R; Shah, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5897-5900 , 文章类型： Article，,卷期：2011年21-19]
- A series of 3,5-bis(indolyl)-1,2,4-thiadiazoles were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. The reaction of indole-3-thiocarboxamide 3 with iodobenzene diacetate underw...
- In vivo anti-inflammatory and antioxidant properties of ellagitannin metabolite urolithin A
[作者：Ishimoto, H; Shibata, M; Myojin, Y; Ito, H; Sugimoto, Y; Tai, A; Hatano, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5901-5904 , 文章类型： Article，,卷期：2011年21-19]
- Urolithin A is a major metabolite produced by rats and humans after consumption of pomegranate juice or pure ellagitannin geraniin. In this study, we investigated the anti-inflammatory effect of urolithin A on carrageena...
- Synthesis of a quinazoline derivative: A new alpha(1)-adrenoceptor ligand for conjugation to quantum dots to study alpha(1)-adrenoceptors in living cells
[作者：Zhou, GH; Wang, L; Ma, YD; Wang, LP; Zhang, YY; Jiang, W,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5905-5909 , 文章类型： Article，,卷期：2011年21-19]
- Quantum dots (QDs) that are conjugated to small molecule derivatives of drugs and endogenous ligands may be useful tools to study the distribution and dynamic of membrane bound receptors, ion channels and transporters in...
- Strategies to improve in vivo toxicology outcomes for basic candidate drug molecules
[作者：Luker, T; Alcaraz, L; Chohan, KK; Blomberg, N; Brown, DS; Butlin, RJ; Elebring, T; Griffin, AM; Guile, S; St-Gallay, S; Swahn, BM; Swallow, S; Waring, MJ; Wenlock, MC; Leeson, PD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5673-5679 , 文章类型： Article，,卷期：2011年21-19]
- A valid PLS-DA model to predict attrition in pre-clinical toxicology for basic oral candidate drugs was built. A combination of aromatic/aliphatic balance, flatness, charge distribution and size descriptors helped predic...
- Sulfonamides as selective oestrogen receptor beta agonists
[作者：Roberts, LR; Armor, D; Barker, C; Bent, A; Bess, K; Brown, A; Favor, DA; Ellis, D; Irving, SL; MacKenny, M; Phillips, C; Pullen, N; Stennett, A; Strand, L; Styles, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5680-5683 , 文章类型： Article，,卷期：2011年21-19]
- A series of p-hydroxybenzenesulphonamides ER beta receptor agonists were discovered and several compounds identified had excellent selectivity over the related ER alpha receptor. One of these, compound 11, had an interes...
- Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. The influence of compound flexibility on microsomal stability
[作者：Johnson, PS; Ryckmans, T; Bryans, J; Beal, DM; Dack, KN; Feeder, N; Harrison, A; Lewis, M; Mason, HJ; Mills, J; Newman, J; Pasquinet, C; Rawson, DJ; Roberts, LR; Russell, R; Spark, D; Stobie, A; Underwood, TJ; Ward, R; Wheeler, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5684-5687 , 文章类型： Article，,卷期：2011年21-19]
- The V1a receptor has emerged as an attractive target for a range of indications including Raynaud's disease and dysmenorrhoea. As part of an effort to discover a new class of orally active V1a antagonist, we optimised a ...
- Cellular uptake of Aib-containing amphipathic helix peptide
[作者：Wada, S; Tsuda, H; Okada, T; Urata, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5688-5691 , 文章类型： Article，,卷期：2011年21-19]
- Cell-penetrating peptides (CPPs) are useful tools for the delivery of hydrophilic bioactive molecules, such as peptides, proteins, and oligonucleotides, across the cell membrane. To realize the delivery of therapeutic ma...
- Bicyclic heteroaryl inhibitors of stearoyl-CoA desaturase: From systemic to liver-targeting inhibitors
[作者：Ramtohul, YK; Powell, D; Leclerc, JP; Leger, S; Oballa, R; Black, C; Isabel, E; Li, CS; Crane, S; Robichaud, J; Guay, J; Guiral, S; Zhang, L; Huang, Z,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5692-5696 , 文章类型： Article，,卷期：2011年21-19]
- Optimization of a lead thiazole amide MF-152 led to the identification of potent bicyclic heteroaryl SCD1 inhibitors with good mouse pharmacokinetic profiles. In a view to target the liver for efficacy and to avoid SCD1 ...
- Mannich reaction derivatives of novobiocin with modulated physiochemical properties and their antibacterial activities
[作者：Tambo-Ong, A; Chopra, S; Glaser, BT; Matsuyama, K; Tran, T; Madrid, PB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5697-5700 , 文章类型： Article，,卷期：2011年21-19]
- Synthetic derivatives of the natural product antibiotic novobiocin were synthesized in order to improve their physiochemical properties. A Mannich reaction was used to introduce new side chains at a solventexposed positi...
- Discovery of inhibitors of plasminogen activator inhibitor-1: Structure-activity study of 5-nitro-2-phenoxybenzoic acid derivatives
[作者：Pandya, V; Jain, M; Chakrabarti, G; Soni, H; Parmar, B; Chaugule, B; Patel, J; Joshi, J; Joshi, N; Rath, A; Raviya, M; Shaikh, M; Sairam, KVVM; Patel, H; Patel, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5701-5706 , 文章类型： Article，,卷期：2011年21-19]
- Two novel series of 5-nitro-2-phenoxybenzoic acid derivatives are designed as potent PAI-1 inhibitors using hybridization and conformational restriction strategy in the tiplaxtinin and piperazine chemo types. The lead co...
- Effects of linker elongation in a series of N-(2-benzofuranylmethyl)-N '-(methoxyphenylalkyl) piperazine sigma(1) receptor ligands
[作者：Moussa, IA; Banister, SD; Akladios, FN; Chua, SW; Kassiou, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5707-5710 , 文章类型： Article，,卷期：2011年21-19]
- In our continued exploration of disubstituted piperazine derivatives as sigma (sigma) receptor ligands with central nervous system (CNS) activity, a series of N-(2-benzofuranylmethyl)-N'-(methoxyphenylalkyl) piperazines ...
- Towards rational design of cannabinoid receptor 1 (CB1) antagonists for peripheral selectivity
[作者：Fulp, A; Bortoff, K; Zhang, YA; Seltzman, H; Snyder, R; Maitra, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5711-5714 , 文章类型： Article，,卷期：2011年21-19]
- CB1 receptor antagonists that are peripherally restricted were targeted. Compounds with permanent charge as well as compounds that have increased polar surface area were made and tested against CB1 for binding and activi...
- Coprismycins A and B, neuroprotective phenylpyridines from the dung beetle-associated bacterium, Streptomyces sp.
[作者：Kim, SH; Ko, H; Bang, HS; Park, SH; Kim, DG; Kwon, HC; Kim, SY; Shin, J; Oh, DC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5715-5718 , 文章类型： Article，,卷期：2011年21-19]
- Two new phenylpyridines, named coprismycins A and B (1 and 2), and previously reported dipyridines (3-6) were isolated from a culture of Streptomyces sp. associated with the dung beetle, Copris tripartitus. The structure...
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