- Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: Discovery, characterization and preliminary SAR of a promising lead
[作者：Thoma, G; Baenteli, R; Lewis, I; Wagner, T; Oberer, L; Blum, W; Glickman, F; Streiff, MB; Zerwes, HG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6185-6188 , 文章类型： Article，,卷期：2009年19-21]
- The special ergoline 1 is a highly potent, selective antagonist of the chemokine receptor CXCR3. The surprising selectivity of this LSD-related compound can be explained by different electronic and steric properties of t...
- Functional and biochemical analysis of a key series of ramoplanin analogues
[作者：Fang, X; Nam, J; Shin, D; Rew, Y; Boger, DL; Walker, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6189-6191 , 文章类型： Article，,卷期：2009年19-21]
- Ramoplanin is a potent lipoglycodepsipeptide antibiotic that is active against a wide range of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococcus (V...
- Discovery of a potent, metabolically stabilized resorcylic lactone as an anti-inflammatory lead
[作者：Du, H; Matsushima, T; Spyvee, M; Goto, M; Shirota, H; Gusovsky, F; Chiba, K; Kotake, M; Yoneda, N; Eguchi, Y; DiPietro, L; Harmange, JC; Gilbert, S; Li, XY; Davis, H; Jiang, Y; Zhang, Z; Pelletier, R; Wong, N; Sakurai, H; Yang, H; Ito-Igarashi, H; Kimura, A; Kuboi, Y; Mizui, Y; Tanaka, I; Ikemori-Kawada, M; Kawakami, Y; Inoue, A; Kawai, T; Kishi, Y; Wang, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6196-6199 , 文章类型： Article，,卷期：2009年19-21]
- With bioactivity-guided phenotype screenings, a potent anti-inflammatory compound f152A1 has been isolated, characterized and identified as the known natural product LL-Z1640-2. Metabolic instability precluded its use fo...
- A naturally occurring brominated furanone covalently modifies and inactivates LuxS
[作者：Zang, TZ; Lee, BWK; Cannon, LM; Ritter, KA; Dai, SJ; Ren, DC; Wood, TK; Zhou, ZS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6200-6204 , 文章类型： Article，,卷期：2009年19-21]
- Halogenated furanones, a group of natural products initially isolated from marine red algae, are known to inhibit bacterial biofilm formation, swarming, and quorum sensing. However, their molecular targets and the precis...
- Bicyclic alpha,omega-dicarboxylic acid derivatives from a colonial tunicate of the family Polyclinidae
[作者：Bao, B; Dang, HT; Zhang, P; Hong, J; Lee, CO; Cho, HY; Jung, JH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6205-6208 , 文章类型： Article，,卷期：2009年19-21]
- In the course of our search for bioactive metabolites from a colonial tunicate of the family Polyclinidae, six new (1-6) cyclic fatty acid derivatives were isolated. Their planar structures were established on the basis ...
- Synthesis and in vitro autoradiographic evaluation of a novel high-affinity radioiodinated ligand for imaging brain cannabinoid subtype-1 receptors
[作者：Donohue, SR; Varnas, K; Jia, ZS; Gulyas, B; Pike, VW; Halldin, C,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6209-6212 , 文章类型： Article，,卷期：2009年19-21]
- There is strong interest to study the involvement of brain cannabinoid subtype-1 (CB1) receptors in neuropsychiatric disorders with single photon emission computed tomography ( SPECT) and a suitable radioligand. Here we ...
- Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors
[作者：Shiozaki, M; Imai, H; Maeda, K; Miura, T; Yasue, K; Suma, A; Yokota, M; Ogoshi, Y; Haas, J; Fryer, AM; Laird, ER; Littmann, NM; Andrews, SW; Josey, JA; Mimura, T; Shinozaki, Y; Yoshiuchi, H; Inaba, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6213-6217 , 文章类型： Article，,卷期：2009年19-21]
- A series of 1-sulfonylaminocyclopropanecarboxylates was synthesized as ADAMTS-5 (Aggrecanase-2) inhibitors. After an intensive investigation of the central cyclopropane core including its absolute stereochemistry and sub...
- Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases
[作者：Bryant, C; Kerr, ID; Debnath, M; Ang, KKH; Ratnam, J; Ferreira, RS; Jaishankar, P; Zhao, DM; Arkin, MR; McKerrow, JH; Brinen, LS; Renslo, AR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6218-6221 , 文章类型： Article，,卷期：2009年19-21]
- We describe here the identification of non-peptidic vinylsulfones that inhibit parasite cysteine proteases in vitro and inhibit the growth of Trypanosoma brucei brucei parasites in culture. A high resolution (1.75 angstr...
- Synthesis of (R,S)-[4-C-11]baclofen via Michael addition of nitromethane labeled with short-lived C-11
[作者：Kato, K; Zhang, MR; Suzuki, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6222-6224 , 文章类型： Article，,卷期：2009年19-21]
- The synthesis of (R, S)-[4-C-11] baclofen, the first C-11-labeled GABA(B) agonist, was demonstrated via Michael addition of nitro[C-11] methane as a key step. A tetrabutylammonium. uoride promoted Michael addition of nit...
- Discovery of 3-(3-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051-a xanthine oxidoreductase inhibitor for the treatment of hyperuricemia
[作者：Sato, T; Ashizawa, N; Matsumoto, K; Iwanaga, T; Nakamura, H; Inoue, T; Nagata, O,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6225-6229 , 文章类型： Article，,卷期：2009年19-21]
- Our previous study identified 2-[2-(2-methoxy-ethoxy)-ethoxy]-5-[5-(2-methyl-4-pyridyl)-1H-[1,2,4]-triazol-3-yl]-benzonitrile (2) as a safe and potent xanthine oxidoreductase (XOR) inhibitor for the treatment of hyperuri...
- Inhibitor profiling of the Pseudomonas aeruginosa virulence factor LasB using N-alpha mercaptoamide template-based inhibitors
[作者：Cathcart, GR; Gilmore, BF; Greer, B; Harriott, P; Walker, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6230-6232 , 文章类型： Article，,卷期：2009年19-21]
- We report on the synthesis and biological evaluation of a focussed library of N-alpha mercaptoamide containing dipeptides as inhibitors of the zinc metallopeptidase Pseudomonas aeruginosa elastase (LasB, EC 3.4.24.26). T...
- Inhibition of ErbB2(Her2) expression with small molecule transcription factor mimics
[作者：Lee, LW; Taylor, CEC; Desaulniers, JP; Zhang, MC; Hojfeldt, JW; Pan, Q; Mapp, AK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6233-6236 , 文章类型： Article，,卷期：2009年19-21]
- Small molecules that mimic the transcriptional activation domain of eukaryotic transcriptional activators have the potential to serve as effective inhibitors of transcriptional processes. Here we show that one class of t...
- Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists
[作者：Pasternak, A; Goble, SD; Dejesus, RK; Hreniuk, DL; Chung, CC; Tota, MR; Mazur, P; Feighner, SD; Howard, AD; Mills, SG; Yang, LH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6237-6240 , 文章类型： Article，,卷期：2009年19-21]
- This Letter describes optimization of ghrelin receptor antagonists and inverse agonists starting from a screening hit. (C) 2009 Elsevier Ltd. All rights reserved.
- Synthesis, antiproliferative, and pharmacokinetic properties of 3-and 17-double-modified analogs of 2-methoxyestradiol
[作者：Agoston, GE; Shah, JH; Suwandi, L; Hanson, AD; Zhan, XG; LaVallee, TM; Pribluda, V; Treston, AM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6241-6244 , 文章类型： Article，,卷期：2009年19-21]
- The syntheses of 21 analogs of 2-methoxyestradiol are presented, including ENMD-1198 which was selected for advancement into Phase 1 clinical trials in oncology. These analogs were evaluated for anti-proliferative activi...
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