- Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor
[作者：Fichtner, M; Lee, E; Tomlinson, E; Scott, D; Cornelius, P; Patterson, TA; Carpino, PA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2738-2743 , 文章类型： Article，,卷期：2012年22-8]
- A novel series of spirocyclic derivatives was synthesized and evaluated as NPY Y5R antagonists for the treatment of obesity. Cis and trans analogs 7a and 8a were equipotent in a Y5R binding assay (K-i's <= 1 nM) and disp...
- Synthesis of new bergenin derivatives as potent inhibitors of inflammatory mediators NO and TNF-alpha
[作者：Shah, MR; Arfan, M; Amin, H; Hussain, Z; Qadir, MI; Choudhary, MI; VanDerveer, D; Mesaik, MA; Soomro, S; Jabeen, A; Khan, IU,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2744-2747 , 文章类型： Article，,卷期：2012年22-8]
- Bergenin is an isocoumarin natural product which aides in fat loss, healthy weight maintenance, enhancing the lipolytic effects of norepinephrine, inhibiting the formation of interleukin 1 alpha and cyclooxygenases-2. He...
- Synthesis and evaluation of piperidine urea derivatives as efficacious 11 beta-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice
[作者：Zhang, LM; Chen, JH; Ning, MM; Zou, QA; Leng, Y; Shen, JH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2748-2752 , 文章类型： Article，,卷期：2012年22-8]
- 11 beta-Hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) has attracted considerable attention as a potential target for the treatment of diabetes and metabolic syndrome. Herein we report the design, synthesis and effic...
- Fluorescent nucleosides with 'on-off' switching function, pH-responsive fluorescent uridine derivatives
[作者：Saito, Y; Miyamoto, S; Suzuki, A; Matsumoto, K; Ishihara, T; Saito, I,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2753-2756 , 文章类型： Article，,卷期：2012年22-8]
- We synthesized various pH-responsive fluorescent deoxyuridine derivatives (1a-g). These fluorescent nucleosides exhibited distinctive fluorescence at 470-600 nm in aqueous solvents containing methanol only at acidic to n...
- Synthesis of [Tyr-5-Psi(CH2NMe)-Tyr-6]RA-VII, a reduced peptide bond analogue of RA-VII, an antitumor bicyclic hexapeptide
[作者：Hasuda, T; Hitotsuyanagi, Y; Shinada, M; Takeya, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2757-2759 , 文章类型： Article，,卷期：2012年22-8]
- A reduced peptide bond analogue of RA-VII, [Tyr-5-Psi(CH2NMe)-Tyr-6]RA-VII (3), was designed and synthesized. The key reduced cycloisodityrosine unit was prepared by reduction of the cycloisodityrosine derived from natur...
- A new pancreatic lipase inhibitor from Broussonetia kanzinoki
[作者：Ahn, JH; Liu, Q; Lee, C; Ahn, MJ; Yoo, HS; Hwang, BY; Lee, MK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2760-2763 , 文章类型： Article，,卷期：2012年22-8]
- A new phenolic compound, broussonone A (1) were isolated from the stem barks of Broussonetia kanzinoki (Moraceae), together with two diphenylpropanes, broussonin A (2), broussonin B (3), two flavans, 7,4 '-dihydroxyflava...
- Synthesis of highly potent novel anti-tubercular isoniazid analogues with preliminary pharmacokinetic evaluation
[作者：Ramani, AV; Monika, A; Indira, VL; Karyavardhi, G; Venkatesh, J; Jeankumar, VU; Manjashetty, TH; Yogeeswari, P; Sriram, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2764-2767 , 文章类型： Article，,卷期：2012年22-8]
- Thirty two novel isoniazid analogues were prepared by one-pot three component condensations of isoniazid (INH), 3-mercaptopropionic acid and various aryl/heteroaryl aldehydes. The synthesized compounds were evaluated for...
- Thiosemicarbazone fragment embedded within 1,2,4-triazole ring as inhibitors of Entamoeba histolytica
[作者：Siddiqui, SM; Salahuddin, A; Azam, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2768-2771 , 文章类型： Article，,卷期：2012年22-8]
- A series of 1,2,4-triazole derivatives containing thiosemicarbazone linkage was synthesized and evaluated for their in vitro antiamoebic activity against HM1:IMSS strain of Entamoeba histolytica. All the compounds were c...
- Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors
[作者：Xu, K; Xiao, ZY; Tang, YB; Huang, L; Chen, CH; Ohkoshi, E; Lee, KH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2772-2774 , 文章类型： Article，,卷期：2012年22-8]
- Fourteen naphthoquinone derivatives (1-14) were designed based on a putative proteasome inhibitor PI-083. These compounds were synthesized and evaluated against A549, DU145, KB, and KBvin tumor cell lines. Six compounds ...
- Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology. Part 2: Propellane derivatives with an amide side chain
[作者：Nagase, H; Akiyama, J; Nakajima, R; Hirayama, S; Nemoto, T; Gouda, H; Hirono, S; Fujii, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2775-2779 , 文章类型： Article，,卷期：2012年22-8]
- We designed and synthesized propellane derivatives with a 6- or 7-amide side chain on the basis of the active conformation of the kappa selective agonist nalfurafine. The 6-amides showed high affinities for the kappa rec...
- Inhibition of tumor suppressor protein p53-dependent transcription by a tetramerization domain peptide via hetero-oligomerization
[作者：Wada, J; Kamada, R; Imagawa, T; Chuman, Y; Sakaguchi, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2780-2783 , 文章类型： Article，,卷期：2012年22-8]
- Tumor suppressor protein p53 induces cell cycle arrest, apoptosis, and senescence in response to cellular stresses. The p53 tetramer formation is essential for its functions. Despite of these crucial functions of p53 for...
- Pyrazine-based Syk kinase inhibitors
[作者：Forns, P; Esteve, C; Taboada, L; Alonso, JA; Orellana, A; Maldonado, M; Carreno, C; Ramis, I; Lopez, M; Miralpeix, M; Vidal, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2784-2788 , 文章类型： Article，,卷期：2012年22-8]
- A series of aminopyrazines as inhibitors of Syk kinase activity and showing inhibition of LAD2 cells degranulation is described. Optimization of the carboxamide motif with aminomethylpiperidines provided high potency inh...
- 3-(N-Arylsulfamoyl)benzamides, inhibitors of human sirtuin type 2 (SIRT2)
[作者：Choi, SH; Quinti, L; Kazantsev, AG; Silverman, RB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2789-2793 , 文章类型： Article，,卷期：2012年22-8]
- Inhibition of sirtuin 2 (SIRT2) is known to be protective against the toxicity of disease proteins in Parkinson's and Huntington's models of neurodegeneration. Previously, we developed SIRT2 inhibitors based on the 3-(N-...
- Indole-propionic acid derivatives as potent, S1P(3)-sparing and EAE efficacious sphingosine-1-phosphate 1 (S1P(1)) receptor agonists
[作者：Meng, QH; Zhao, BW; Xu, QF; Xu, XS; Deng, GH; Li, CY; Luan, LB; Ren, F; Wang, HL; Xu, H; Xu, Y; Zhang, HB; Xiang, JN; Elliott, JD; Guo, TB; Zhao, YG; Zhang, W; Lu, HT; Lin, XC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2794-2797 , 文章类型： Article，,卷期：2012年22-8]
- Novel indole-propionic acid derivatives were developed as sphingosine-1-phosphate (S1P) receptor agonists through a systematic SAR study. The optimized and S1P(3) selective S1P(1) agonist 9f induced peripheral blood lymp...
- Development of hypoxia-sensitive Gd3+-based MRI contrast agents
[作者：Iwaki, S; Hanaoka, K; Piao, W; Komatsu, T; Ueno, T; Terai, T; Nagano, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2798-2802 , 文章类型： Article，,卷期：2012年22-8]
- Hypoxia occurs in various diseases, including cancer, ischemia, and acute and chronic vascular diseases. Here we describe the design and synthesis of the first hypoxia-sensitive MRI contrast agents, SAGds. SAGds showed a...
- Discovery of S-777469: An orally available CB2 agonist as an antipruritic agent
[作者：Odan, M; Ishizuka, N; Hiramatsu, Y; Inagaki, M; Hashizume, H; Fujii, Y; Mitsumori, S; Morioka, Y; Soga, M; Deguchi, M; Yasui, K; Arimura, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2803-2806 , 文章类型： Article，,卷期：2012年22-8]
- The discovery of novel CB2 ligands based on the 3-carbamoyl-2-pyridone derivatives by adjusting the size of side chain at 1-, 5-and 6-position is reported. The structure-activity relationship around this template lead to...
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