- Prenyloxyphenylpropanoids as a novel class of anticonvulsive agents
[作者：Genovese, S; Epifano, F; Curini, M; Dudra-Jastrzebska, M; Luszczki, JJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5419-5422 , 文章类型： Article，,卷期：2009年19-18]
- In this study, we synthesized some natural and semi-synthetic prenyloxyphenylpropanoids (e.g., acetophenones, benzoic and cinnamic acids, chalcones, and coumarins), and we assessed their in vivo neuroprotective activity,...
- C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKC theta inhibitors: Part I
[作者：Subrath, J; Wang, D; Wu, BQ; Niu, CS; Boschelli, DH; Lee, J; Yang, XK; Brennan, A; Chaudhary, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5423-5425 , 文章类型： Article，,卷期：2009年19-18]
- We earlier reported that 3-pyridinecarbonitriiles with a 4-methylindolyl-5-amino group at C-4 and a phenyl group at C-5 were inhibitors of PKC theta. Keeping the group at C-4 of the pyridine core constant, we varied the ...
- From natural products to achiral drug prototypes: Potent thrombin inhibitors based on P-2/P-3 dihydropyrid-2-one core motifs
[作者：Hanessian, S; Therrien, E; Zhang, JB; van Otterlo, W; Xue, YF; Gustafsson, D; Nilsson, I; Fjellstrom, O,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5429-5432 , 文章类型： Article，,卷期：2009年19-18]
- A series of dihydropyrid-2-ones was synthesized and tested for inhibitory activity against serine protease enzymes. Moderate to low nanomolar inhibitory activities were obtained against thrombin and excellent selectivity...
- Substrate specificity of N-acetylhexosamine kinase towards N-acetylgalactosamine derivatives
[作者：Cai, L; Guan, WY; Wang, WJ; Zhao, W; Kitaoka, M; Shen, J; O'Neil, C; Wang, PG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5433-5435 , 文章类型： Article，,卷期：2009年19-18]
- We report herein a bacterial N-acetylhexosamine kinase, NahK, with broad substrate specificity towards structurally modified GalNAc analogues, and the production of a GalNAc-1-phosphate library using this kinase. (C) 200...
- Identification of positron emission tomography ligands for NPY Y5 receptors in the brain
[作者：Takahashi, H; Haga, Y; Shibata, T; Nonoshita, K; Sakamoto, T; Moriya, M; Ohe, T; Chiba, M; Mitobe, Y; Kitazawa, H; Iwaasa, H; Ishihara, A; Ishii, Y; Kanatani, A; Fukami, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5436-5439 , 文章类型： Article，,卷期：2009年19-18]
- A series of trans-3-oxospiro[(aza)isobenzofuran-1(3H),1'-cyclohexane]-4'-carboxamide derivatives were synthesized and profiled for NPY Y5 binding affinity, brain and CSF penetrability in rats, and susceptibility to human...
- Disubstituted pyrimidines as Lck inhibitors
[作者：Hunt, JA; Beresis, RT; Goulet, JL; Holmes, MA; Hong, XFJ; Kovacs, E; Mills, SG; Ruzek, RD; Wong, F; Hermes, JD; Park, YW; Salowe, SP; Sonatore, LM; Wu, L; Woods, A; Zaller, DM; Sinclair, PJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5440-5443 , 文章类型： Article，,卷期：2009年19-18]
- We have developed a family of 4-benzimidazolyl-N-piperazinethyl-pyrimidin-2-amines that are subnanomolar inhibitors of Lck. A subset of these Lck inhibitors, with heterocyclic substituents at the benzimidazole C5, are al...
- Synthesis and evaluation of inhibitors of cytochrome P450 3A (CYP3A) for pharmacokinetic enhancement of drugs
[作者：Flentge, CA; Randolph, JT; Huang, PP; Klein, LL; Marsh, KC; Harlan, JE; Kempf, DJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5444-5448 , 文章类型： Article，,卷期：2009年19-18]
- The HIV protease inhibitor ritonavir (RTV) is also a potent inhibitor of the metabolizing enzyme cytochrome P450 3A (CYP3A) and is clinically useful in HIV therapy in its ability to enhance human plasma levels of other H...
- Positional effects of monofluorinated phenylalanines on histone acetyltransferase stability and activity
[作者：Voloshchuk, N; Zhu, AY; Snydacker, D; Montclare, JK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5449-5451 , 文章类型： Article，,卷期：2009年19-18]
- To explore the impact of global incorporation of fluorinated aromatic amino acids on protein function, we investigated the effects of three monofluorinated phenylalanine analogs para-fluorophenylalanine (pFF), meta-fluor...
- Pyrrole[2,3-d]azepino compounds as agonists of the farnesoid X receptor (FXR)
[作者：Mehlmann, JF; Crawley, ML; Lundquist, JT; Unwalla, RJ; Harnish, DC; Evans, MJ; Kim, CY; Wrobel, JE; Mahaney, PE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5289-5292 , 文章类型： Article，,卷期：2009年19-18]
- Pyrrole[2,3-d]azepines have been identified as potent agonists of the farnesoid X receptor (FXR). Based on the planar X-ray crystal structure of WAY-362450 1 in the ligand binding domain and molecular modeling studies, n...
- NO-NSAIDs: Gastric-sparing nitric oxide-releasable prodrugs of non-steroidal anti-inflammatory drugs
[作者：Nemmani, KVS; Mali, SV; Borhade, N; Pathan, AR; Karwa, M; Pamidiboina, V; Senthilkumar, SP; Gund, M; Jain, AK; Mangu, NK; Dubash, NP; Desai, DC; Sharma, S; Satyam, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5297-5301 , 文章类型： Article，,卷期：2009年19-18]
- Recently, a new class of nitric-oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs) is being studied as 'Safe NSAIDs' because of their gastric-sparing properties. As an extension of our novel disulfide link...
- 5-(2-Pyrimidinyl)-imidazo[1,2-a]pyridines are antibacterial agents targeting the ATPase domains of DNA gyrase and topoisomerase IV
[作者：Starr, JT; Sciotti, RJ; Hanna, DL; Huband, MD; Mullins, LM; Cai, H; Gage, JW; Lockard, M; Rauckhorst, MR; Owen, RM; Lall, MS; Tomilo, M; Chen, HF; McCurdy, SP; Barbachyn, MR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5302-5306 , 文章类型： Article，,卷期：2009年19-18]
- Dual inhibitors of bacterial gyrB and parE based on a 5-(2-pyrimidinyl)-imidazo[1,2-a]pyridine template exhibited MICs (mu g/mL) of 0.06-64 (Sau), 0.25-64 (MRSA), 0.06-64 (Spy), 0.06-64 (Spn), and 0.03-64 (FQR Spn). Sele...
- Discovery and biological profile of isoindolinone derivatives as novel metabotropic glutamate receptor 1 antagonists: A potential treatment for psychotic disorders
[作者：Ito, S; Hirata, Y; Nagatomi, Y; Satoh, A; Suzuki, G; Kimura, T; Satow, A; Maehara, S; Hikichi, H; Hata, M; Ohta, H; Kawamoto, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5310-5313 , 文章类型： Article，,卷期：2009年19-18]
- We describe here the discovery and biological profile of a series of isoindolinone derivatives as developed mGluR1 antagonists. Our combined strategy of rapid parallel synthesis and conventional medicinal optimization su...
- Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors
[作者：Shen, HC; Ding, FX; Deng, QL; Xu, SY; Chen, HS; Tong, XC; Tong, V; Zhang, XP; Chen, YL; Zhou, GC; Pai, LY; Alonso-Galicia, M; Zhang, B; Roy, S; Tata, JR; Berger, JP; Colletti, SL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5314-5320 , 文章类型： Article，,卷期：2009年19-18]
- 3,3-Disubstituted piperidine-derived trisubstituted urea entA-2b was discovered as a highly potent and selective soluble epoxide hydrolase (sEH) inhibitor. Despite the good compound oral exposure, excellent sEH inhibitio...
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