- Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H(4) and the ion channel serotonin 5-HT(3A)
[作者:Verheij, MHP; de Graaf, C; de Kloe, GE; Nijmeijer, S; Vischer, HF; Smits, RA; Zuiderveld, OP; Hulscher, S; Silvestri, L; Thompson, AJ; van Muijlwijk-Koezen, JE; Lummis, SCR; Leurs, R; de Esch, IJP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5460-5464 , 文章类型: Article,,卷期:2011年21-18]
- A fragment library was screened against the G protein-coupled histamine H(4) receptor (H(4)R) and the ligand-gated ion channel serotonin 5-HT(3A) (5-HT(3A)R). Interestingly, significant overlap was found between H(4)R an...
- Design and synthesis of spiro[indole-thiazolidine]spiro[indole-pyrans] as antimicrobial agents
[作者:Sakhuja, R; Panda, SS; Khanna, L; Khurana, S; Jain, SC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5465-5469 , 文章类型: Article,,卷期:2011年21-18]
- A series of novel spiro[indole-thiazolidine]spiro[indole-pyran] derivatives were synthesized from N-(bromoalkyl)indol-2,3-diones via monospiro-bisindole intermediates; the two indole nuclei being connected via N-(CH(2))(...
- SAR analysis of innovative selective small molecule antagonists of sphingosine-1-phosphate 4 (S1P(4)) receptor
[作者:Urbano, M; Guerrero, M; Zhao, J; Velaparthi, S; Schaeffer, MT; Brown, S; Rosen, H; Roberts, E,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5470-5474 , 文章类型: Article,,卷期:2011年21-18]
- Recent evidence suggests an innovative application of chemical modulators targeting the S1P(4) receptor as novel mechanism-based drugs for the treatment of influenza virus infection. Modulation of the S1P(4) receptor may...
- Discovery, synthesis and SAR of azinyl- and azolylbenzamides antagonists of the P2X(7) receptor
[作者:Subramanyam, C; Duplantier, AJ; Dombroski, MA; Chang, SP; Gabel, CA; Whitney-Pickett, C; Perregaux, DG; Labasi, JM; Yoon, K; Shepard, RM; Fisher, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5475-5479 , 文章类型: Article,,卷期:2011年21-18]
- The discovery, of a series of 2-Cl-5-heteroaryl-benzamide antagonists of the P2X(7) receptor via parallel medicinal chemistry is described. Initial analogs suffered from poor metabolic stability and low Vd(ss). Multi par...
- A water-soluble 1,8-naphthalimide-based 'turn on' fluorescent chemosensor for selective and sensitive recognition of mercury ion in water
[作者:Dai, HL; Xu, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5141-5144 , 文章类型: Article,,卷期:2011年21-18]
- A water-soluble 1,8-naphthalimide-based fluorescent chemosensor 1, bearing two acetic carboxylic moieties, exhibited high selectivity and sensitivity for recognition of Hg(2+) ion in water over other heavy and transition...
- A novel macrocyclic lactone with insecticidal bioactivity from Streptomyces microflavus neau3
[作者:Wang, XJ; Zhang, J; Liu, CX; Gong, DL; Zhang, H; Wang, JD; Yan, YJ; Xiang, WS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5145-5148 , 文章类型: Article,,卷期:2011年21-18]
- A novel macrocyclic lactone (1) was isolated from the fermentation broth of Streptomyces microflavus neau3, and the structure was elucidated by extensive spectroscopic analysis. Compound 1 showed high acaricidal activity...
- Synthesis of various 3-nitropropionamides as Mycobacterium tuberculosis isocitrate lyase inhibitor
[作者:Sriram, D; Yogeeswari, P; Methuku, S; Vyas, DRK; Senthilkumar, P; Alvala, M; Jeankumar, VU,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5149-5154 , 文章类型: Article,,卷期:2011年21-18]
- Various 3-nitropropionamides were synthesized and evaluated for in vitro activities against log and starved phase culture of two mycobacterial species and Mycobacterium tuberculosis (MTB) isocitrate lyase (ICL) enzyme in...
- The natural product CCR5 antagonist anibamine and its analogs as anti-prostate cancer agents
[作者:Haney, KM; Zhang, F; Arnatt, CK; Yuan, YY; Li, G; Ware, JL; Gewirtz, DA; Zhang, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5159-5163 , 文章类型: Article,,卷期:2011年21-18]
- Prostate cancer is a leading cause of death among males in the United States. As the chemokine receptor CCR5 is over-expressed in more aggressive forms of prostate cancer, and is also a critical receptor in inflammation,...
- New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: Exploring the S2 ' region
[作者:Malamas, MS; Erdei, J; Gunawan, I; Barnes, K; Hui, Y; Johnson, M; Robichaud, A; Zhou, P; Yan, YF; Solvibile, W; Turner, J; Fan, KY; Chopra, R; Bard, J; Pangalos, MN,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5164-5170 , 文章类型: Article,,卷期:2011年21-18]
- The proteolytic enzyme beta-secretase (BACE1) plays a central role in the synthesis of the pathogenic beta-amyloid in Alzheimer's disease. SAR studies of the S2' region of the BACE1 ligand binding pocket with pyrazolyl a...
- Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines
[作者:Li, XM; Hilgers, M; Cunningham, M; Chen, ZY; Trzoss, M; Zhang, JH; Kohnen, L; Lam, T; Creighton, C; Kedar, GC; Nelson, K; Kwan, B; Stidham, M; Brown-Driver, V; Shaw, KJ; Finn, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5171-5176 , 文章类型: Article,,卷期:2011年21-18]
- Dihydrofolate reductase (DHFR) inhibitors such as trimethoprim(TMP) have long played a significant role in the treatment of bacterial infections. Not surprisingly, after decades of use there is now bacterial resistance t...
- Synthesis and biological evaluation of some novel N-aryl-1,4-dihydropyridines as potential antitubercular agents
[作者:Trivedi, AR; Dodiya, DK; Dholariya, BH; Kataria, VB; Bhuva, VR; Shah, VH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5181-5183 , 文章类型: Article,,卷期:2011年21-18]
- 1,4-Dihydropyridines are the emerging class of antitubercular agent. Recently, studies have revealed that 1,4-dihydropyridine-3,5-dicarbamoyl derivatives with lipophilic groups have demonstrated excellent antitubercular ...
- A novel indium-111-labeled gonadotropin-releasing hormone peptide for human prostate cancer imaging
[作者:Guo, HX; Gallazzi, F; Sklar, LA; Miao, YB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5184-5187 , 文章类型: Article,,卷期:2011年21-18]
- The purpose of this study was to evaluate the tumor targeting and imaging properties of a novel (111)In-labeled gonadotropin-releasing hormone (GnRH) peptide {1,4,7,10-tetraazacyclododecane1,4,7,10-tetraacetic acid (DOTA...
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