- Identification of chemicals to inhibit the kinase activity of leucine-rich repeat kinase 2 (LRRK2), a Parkinson's disease-associated protein
[作者:Yun, H; Heo, HY; Kim, HH; DooKim, N; Seol, W,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2953-2957 , 文章类型: Article,,卷期:2011年21-10]
- Parkinson's disease (PD) is a late-onset neurodegenerative disease which occurs at more than 1% in populations aging 65-years and over. Recently, leucine-rich repeat kinase 2 (LRRK2) has been identified as a causative ge...
- In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors
[作者:Wang, T; Ioannidis, S; Almeida, L; Block, MH; Davies, AM; Lamb, ML; Scott, DA; Su, M; Zhang, HJ; Alimzhanov, M; Bebernitz, G; Bell, K; Zinda, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2958-2961 , 文章类型: Article,,卷期:2011年21-10]
- Synthesis and biological evaluation of a series of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors was reported. Biochemical screening, followed by profile optimization, resulted in JAK2 inhibitors ex...
- Synthesis and evaluation of novel N-fluoropyridyl derivatives of tropane as potential PET imaging agents for the dopamine transporter
[作者:Liu, JY; Zhu, L; Plossl, K; Lieberman, BP; Kung, HF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2962-2965 , 文章类型: Article,,卷期:2011年21-10]
- A series of novel N-fluoropyridyl-containing tropane derivatives were synthesized and their binding affinities for the dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine (NET) were determined via...
- 2-Arylimidazo[2,1-b]benzothiazoles: A new family of amyloid binding agents with potential for PET and SPECT imaging of Alzheimer's brain
[作者:Alagille, D; DaCosta, H; Baldwin, RM; Tamagnan, GD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2966-2968 , 文章类型: Article,,卷期:2011年21-10]
- We designed and synthesized a small series of 2-aryl-imidazo[2,1-b]benzothiazole, representing a combination of motifs from the two most potent amyloid imaging agents, PIB and IMPY. The binding affinity of the new compou...
- NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor
[作者:Beria, I; Bossi, RT; Brasca, MG; Caruso, M; Ceccarelli, W; Fachin, G; Fasolini, M; Forte, B; Fiorentini, F; Pesenti, E; Pezzetta, D; Posteri, H; Scolaro, A; Depaolini, SR; Valsasina, B,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2969-2974 , 文章类型: Article,,卷期:2011年21-10]
- As part of our drug discovery effort, we identified and developed 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as PLK1 inhibitors. We now report the optimization of this class that led to the identification of N...
- Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII
[作者:Rami, M; Maresca, A; Smaine, FZ; Montero, JL; Scozzafava, A; Winum, JY; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2975-2979 , 文章类型: Article,,卷期:2011年21-10]
- A new series of sulfonamides was synthesized by the reaction of the boroxazolidone complex of L-lysine with isothiocyanates incorporating sulfamoyl moieties and diverse organic scaffolds. The obtained thioureas have been...
- Diaryl urea analogues of SB-334867 as orexin-1 receptor antagonists
[作者:Perrey, DA; Gilmour, BP; Runyon, SP; Thomas, BF; Zhang, YN,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2980-2985 , 文章类型: Article,,卷期:2011年21-10]
- As a part of our program to develop OX1-CB1 bivalent ligands, we required a better understanding of the basic structure-activity relationships (SARs) of orexin antagonists. A series of SB-334867 analogues were synthesize...
- Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors
[作者:Zhao, XZ; Maddali, K; Metifiot, M; Smith, SJ; Vu, BC; Marchand, C; Hughes, SH; Pommier, Y; Burke, TR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2986-2990 , 文章类型: Article,,卷期:2011年21-10]
- New tricyclic HIV-1 integrase (IN) inhibitors were prepared that combined structural features of bicyclic pyrimidinones with recently disclosed 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones. This combination resulted in the ...
- Discovery of small molecule human FPR1 receptor antagonists
[作者:Unitt, J; Fagura, M; Phillips, T; King, S; Perry, M; Morley, A; MacDonald, C; Weaver, R; Christie, J; Barber, S; Mohammed, R; Paul, M; Cook, A; Baxter, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2991-2997 , 文章类型: Article,,卷期:2011年21-10]
- The identification of two novel series of formyl peptide receptor 1 (FPR1) antagonists are reported, represented by methionine benzimidazole 6 and diamide 7. Both series specifically inhibited the binding of labelled fML...
- Radiosynthesis and preliminary evaluation of 4-[F-18]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1
[作者:Yamasaki, T; Fujinaga, M; Yoshida, Y; Kumata, K; Yui, JJ; Kawamura, K; Hatori, A; Fukumura, T; Zhang, MR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2998-3001 , 文章类型: Article,,卷期:2011年21-10]
- The purpose of this study was to develop 4-[F-18]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide ([F-18]FITM, [F-18]4) as a new PET ligand for imaging metabotropic glutamate receptor su...
- Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors
[作者:Kim, S; Jung, JK; Lee, HS; Kim, Y; Kim, J; Choi, K; Baek, DJ; Moon, B; Oh, KS; Lee, BH; Shin, KJ; Pae, AN; Nam, G; Roh, EJ; Cho, YS; Choo, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3002-3006 , 文章类型: Article,,卷期:2011年21-10]
- A serine-threonine kinase IKK-2 plays an important role in activation of NF-kappa B through phosphorylation of the inhibitor of NF-kappa B (I kappa B). As NF-kappa B is a major transcription factor that regulates genes r...
- Synthesis and evaluation of quinoxaline derivatives as potential influenza NS1A protein inhibitors
[作者:You, L; Cho, EJ; Leavitt, J; Ma, LC; Montelione, GT; Anslyn, EV; Krug, RM; Ellington, A; Robertus, JD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3007-3011 , 文章类型: Article,,卷期:2011年21-10]
- A library of quinoxaline derivatives were prepared to target non-structural protein 1 of influenza A (NS1A) as a means to develop anti-influenza drug leads. An in vitro fluorescence polarization assay demonstrated that t...
- A green expedient synthesis of pyridopyrimidine-2-thiones and their antitubercular activity
[作者:Rajesh, SM; Kumar, RS; Libertsen, LA; Perumal, S; Yogeeswari, P; Sriram, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3012-3016 , 文章类型: Article,,卷期:2011年21-10]
- The pseudo four-component domino reactions of N-substituted-4-piperidones, substituted aromatic aldehydes and thiourea in the presence of solid sodium ethoxide under solvent-free conditions afforded pyridopyrimidine-2-th...
- Synthesis and in vitro cytotoxic evaluation of N-alkylbromo and N-alkylphthalimido-isatins
[作者:Singh, P; Kaur, S; Kumar, V; Bedi, PMS; Mahajan, MP; Sehar, I; Pal, HC; Saxena, AK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3017-3020 , 文章类型: Article,,卷期:2011年21-10]
- The manuscript pertains to the synthesis and in vitro cytotoxic evaluation of a series of N-alkylbromo and N-alkylphthalimido-isatins against four different human cancer cell lines namely Colon: HCT-15; Liver: Hep-2; Lun...
- Structure and characteristics of reassembled fluorescent protein, a new insight into the reassembly mechanisms
[作者:Isogai, M; Kawamoto, Y; Inahata, K; Fukada, H; Sugimoto, K; Tada, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3021-3024 , 文章类型: Article,,卷期:2011年21-10]
- Bimolecular fluorescence complementation (BiFC) assay has been used widely to visualize protein-protein interactions in cells. However, there is a problem that fluorescent protein fragments have an ability to associate w...
- Novel 3-chlorooxazolidin-2-ones as antimicrobial agents
[作者:Shiau, TP; Turtle, ED; Francavilla, C; Alvarez, NJ; Zuck, M; Friedman, L; O'Mahony, DJR; Low, E; Anderson, MB; Najafi, R; Jain, RK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3025-3028 , 文章类型: Article,,卷期:2011年21-10]
- Antimicrobial resistance against many known therapeutics is on the rise. We examined derivatives of 3-chlorooxazolidin-2-one 1a (X = H) as antibacterial and antifungal agents. The key findings were that the activity and ...
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