- Novel 12-membered non-antibiotic macrolides from erythromycin A; EM900 series as novel leads for anti-inflammatory and/or immunomodulatory agents
[作者：Sugawara, A; Sueki, A; Hirose, T; Nagai, K; Gouda, H; Hirono, S; Shima, H; Akagawa, KS; Omura, S; Sunazuka, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3373-3376 , 文章类型： Article，,卷期：2011年21-11]
- Herein, we report the design and synthesis of the novel 12-membered non-antibiotic macrolide (8R,9S)-8,9- dihydro-6,9-epoxy-8,9-anhydropseudoerythromycin A (EM900), which was found to be a potent anti-inflammatory and/or...
- Design, synthesis and in vitro antibacterial activity of 7-(4-alkoxyimino-3-aminomethylpiperidin-1-yl) fluoroquinolone derivatives
[作者：Chai, Y; Wang, J; Liu, ML; Yi, H; Sun, LY; You, XF; Guo, HY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3377-3380 , 文章类型： Article，,卷期：2011年21-11]
- We report herein the design and synthesis of novel 7-(4-alkoxyimino-3-aminomethylpiperidin-1-yl) fluoroquinolone derivatives. The antibacterial activity of the newly synthesized compounds was evaluated and compared with ...
- Synthesis and anti-tumor activity of novel ethyl 3-aryl-4-oxo-3,3a,4,6-tetrahydro-1H- furo[3,4-c]pyran-3a-carboxylates
[作者：Wang, TT; Liu, J; Zhong, HY; Chen, H; Lv, ZL; Zhang, YK; Zhang, MF; Geng, DP; Niu, CJ; Li, YM; Li, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3381-3383 , 文章类型： Article，,卷期：2011年21-11]
- A series of ethyl 3-aryl-4-oxo-3,3a,4,6-tetrahydro-1H-furo[3,4-c]pyran-3a-carboxylates were prepared through the metal-catalyzed domino reaction of alkylidene malonates and 1,4-butynediol under a one-pot reaction conditi...
- 3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation
[作者：Chen, JJ; Nguyen, T; D'Amico, DC; Qian, WY; Human, J; Aya, T; Biswas, K; Fotsch, C; Han, NH; Liu, QY; Nishimura, N; Peterkin, TAN; Yang, K; Zhu, JW; Riahi, BB; Hungate, RW; Andersen, NG; Colyer, JT; Faul, MM; Kamassah, A; Wang, J; Jona, J; Kumar, G; Johnson, E; Askew, BC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3384-3389 , 文章类型： Article，,卷期：2011年21-11]
- The discovery of novel and highly potent oxopiperazine based B1 receptor antagonists is described. Compared to the previously described arylsulfonylated (R)-3-amino-3-phenylpropionic acid series, the current compounds sh...
- 3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists
[作者：Walsh, SP; Severino, A; Zhou, CY; He, JF; Liang, GB; Tan, CP; Cao, J; Eiermann, GJ; Xu, L; Salituro, G; Howard, AD; Mills, SG; Yang, LH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3390-3394 , 文章类型： Article，,卷期：2011年21-11]
- The design, synthesis, and structure-activity relationship (SAR) for a series of beta-substituted 3-(4-aryloxyaryl) propanoic acid GPR40 agonists is described. Systematic replacement of the pendant aryloxy group led to i...
- Two methionine aminopeptidases from Acinetobacter baumannii are functional enzymes
[作者：Yuan, H; Chai, SC; Lam, CK; Xu, HH; Ye, QZ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3395-3398 , 文章类型： Article，,卷期：2011年21-11]
- Drug resistance in Gram-negative bacteria, such as Acinetobacter baumannii, is emerging as a significant healthcare problem. New antibiotics with a novel mechanism of action are urgently needed to overcome the drug resis...
- 2,6-Disubstituted pyrazines and related analogs as NR2B site antagonists of the NMDA receptor with anti-depressant activity
[作者：Brown, DG; Maier, DL; Sylvester, MA; Hoerter, TN; Menhaji-Klotz, E; Lasota, CC; Hirata, LT; Wilkins, DE; Scott, CW; Trivedi, S; Chen, TM; McCarthy, DJ; Maciag, CM; Sutton, EJ; Cumberledge, J; Mathisen, D; Roberts, J; Gupta, A; Liu, F; Elmore, CS; Alhambra, C; Krumrine, JR; Wang, X; Ciaccio, PJ; Wood, MW; Campbell, JB; Johansson, MJ; Xia, J; Wen, XT; Jiang, J; Wang, XP; Peng, ZZ; Hu, T; Wang, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3399-3403 , 文章类型： Article，,卷期：2011年21-11]
- Herein we describe the discovery of compounds that are competitive antagonists of the CP101-606 binding site within the NR2B subtype of the NMDA receptor. The compounds identified do not possess phenolic functional group...
- Synthesis and evaluation of heteroarylalanine diacids as potent and selective neutral endopeptidase inhibitors
[作者：Glossop, MS; Bazin, RJ; Dack, KN; Fox, DNA; MacDonald, GA; Mills, M; Owen, DR; Phillips, C; Reeves, KA; Ringer, TJ; Strang, RS; Watson, CAL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3404-3406 , 文章类型： Article，,卷期：2011年21-11]
- Heteroarylalanine derivatives 4 were designed as potential inhibitors of neutral endopeptidase (NEP EC 3.4.24.11). Selectivity over other zinc metalloproteinases was explored through occupation of the S2' sub-site within...
- Efficacy switching SAR of mGluR5 allosteric modulators: Highly potent positive and negative modulators from one chemotype
[作者：Sams, AG; Mikkelsen, GK; Brodbeck, RM; Pu, XS; Ritzen, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3407-3410 , 文章类型： Article，,卷期：2011年21-11]
- A series of metabotropic glutamate 5 receptor (mGluR5) allosteric ligands with positive, negative or no modulatory efficacy is described. The ability of this series to yield both mGluR5 PAMs and NAMs with single-digit na...
- Macrocyclic lactams as potent Hsp90 inhibitors with excellent tumor exposure and extended biomarker activity
[作者：Zapf, CW; Bloom, JD; McBean, JL; Dushin, RG; Nittoli, T; Otteng, M; Ingalls, C; Golas, JM; Liu, H; Lucas, J; Boschelli, F; Hu, YB; Vogan, E; Levin, JI,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3411-3416 , 文章类型： Article，,卷期：2011年21-11]
- A novel series of macrocyclic ortho-aminobenzamide Hsp90 inhibitors is reported. In continuation of our research in this area, macrocyclic amides and lactams were explored to reduce the risk of hERG liabilities. This eff...
- New antiplasmodial indole alkaloids from Hunteria zeylanica
[作者：Nugroho, AE; Sugai, M; Hirasawa, Y; Hosoya, T; Awang, K; Hadi, AHA; Ekasari, W; Widyawaruyanti, A; Morita, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3417-3419 , 文章类型： Article，,卷期：2011年21-11]
- Two new indole alkaloids, bisnicalaterine D (1), consisting of an eburnane and a corynanthe type of skeletons, and nicalaterine A (2) were isolated from the bark of Hunteria zeylanica. Their structures were elucidated by...
- Macrocyclic chelator assembled RGD multimers for tumor targeting
[作者：Zhang, XF; Liu, HG; Miao, Z; Kimura, R; Fan, FY; Cheng, Z,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3423-3426 , 文章类型： Article，,卷期：2011年21-11]
- Macrocyclic chelators have been extensively used for complexation of metal ions. A widely used chelator, DOTA, has been explored as a molecular platform to assemble multiple bioactive peptides in this paper. The multival...
- A novel, broad-spectrum antitumor compound containing the 1-hydroxycyclohexa-2,5-dien-4-one group: The disclosure of a new antitumor pharmacophore in protoapigenone 1
[作者：Yuan, QY; Liu, ZW; Xiong, CM; Wu, LQ; Wang, JP; Ruan, JL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3427-3430 , 文章类型： Article，,卷期：2011年21-11]
- The synthesis of a new compound 9 containing the 4-hydroxy-2,5-cyclohexadien-1-one system, a key elements toward elucidation of the protoapigenone 1 antitumor pharmacophore, was described. The compound showed potent in v...
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