- Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies
[作者:Temperini, C; Innocenti, A; Scozzafava, A; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4282-4286 , 文章类型: Article,,卷期:2008年18-15]
- The new antitumor sulfamate EMD 486019 was investigated for its interaction with twelve catalytically active mammalian carbonic anhydrase (CA, EC 4.2.1.1) isozymes, hCA I - XIV. Similarly to 667-Coumate, a structurally r...
- Structure-activity relationship studies on vitamin D lactam derivatives as vitamin D receptor antagonist
[作者:Cho, K; Uneuchi, F; Kato-Nakamura, Y; Namekawa, JI; Ishizuka, S; Takenouchi, K; Nagasawa, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4287-4290 , 文章类型: Article,,卷期:2008年18-15]
- Structure-activity relationship studies on 1 alpha, 25-dihydroxyvitamin D-3-26,23-lactams (DLAMs), antagonists of vitamin D, were conducted, focusing on the substituents of the phenyl group. One of the derivatives (23S,2...
- Structure-activity relationships of 2-aryl-1H-indole inhibitors of the NorA efflux pump in Staphylococcus aureus
[作者:Ambrus, JI; Kelso, MJ; Bremner, JB; Ball, AR; Casadei, G; Lewis, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4294-4297 , 文章类型: Article,,卷期:2008年18-15]
- The synthesis of 22 2-aryl-1H-indoles, including 12 new compounds, has been achieved via Pd- or Rh-mediated methodologies, or selective electrophilic substitution. All three methods were based on elaborations from simple...
- N-benzyl-N-(pyrrolidin-3-yl) carboxamides as a new class of selective dual serotonin/noradrenaline reuptake inhibitors
[作者:Wakenhut, F; Fish, PV; Fray, MJ; Gurrell, I; Mills, JE; Stobie, A; Whitlock, GA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4308-4311 , 文章类型: Article,,卷期:2008年18-15]
- The structure-activity relationship and the synthesis of novel N-benzyl-N-(pyrrolidin-3-yl)carboxamides as dual serotonin (5-HT) and noradrenaline (NA) monoamine reuptake inhibitors are described. Compounds such as 18 ex...
- Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors
[作者:Xin, ZL; Zhao, HY; Serby, MD; Liu, B; Liu, M; Szczepankiewicz, BG; Nelson, LTJ; Smith, HT; Suhar, TS; Janis, RS; Cao, N; Camp, HS; Collins, CA; Sham, HL; Surowy, TK; Liu, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4298-4302 , 文章类型: Article,,卷期:2008年18-15]
- A series of structurally novel stearoyl-CoA desaturase1 (SCD1) inhibitors has been identified via molecular scaffold manipulation. Preliminary structure-activity relationship (SAR) studies led to the discovery of potent,...
- 4-(1,3-Thiazol-2-yl) morpholine derivatives as inhibitors of phosphoinositide 3-kinase
[作者:Alexander, R; Balasundaram, A; Batchelor, M; Brookings, D; Crepy, K; Crabbe, T; Deltent, MF; Driessens, F; Gill, A; Harris, S; Hutchinson, G; Kulisa, C; Merriman, M; Mistry, P; Parton, T; Turner, J; Whitcombe, I; Wright, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4316-4320 , 文章类型: Article,,卷期:2008年18-15]
- 4-(1,3-Thiazol-2-yl)morpholine derivatives have been identified as potent and selective inhibitors of phosphoinositide 3-kinase. The SAR data of selected examples are presented and the in vivo pro. ling of compound 18 is...
- N-acyl-3-amino-5H-furanone derivatives as new inhibitors of LuxR-dependent quorum sensing: Synthesis, biological evaluation and binding mode study
[作者:Estephane, J; Dauvergne, J; Soulere, L; Reverchon, S; Queneau, Y; Doutheau, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4321-4324 , 文章类型: Article,,卷期:2008年18-15]
- New N-acyl homoserine lactone analogues, N-acyl-3-amino-5H-furanone derivatives and some 4-halogeno counterparts, were synthesised and tested for their ability to modulate LuxR-dependent bacterial quorum sensing. Both ty...
- N-(thiazol-2-yl)-2-thiophene carboxamide derivatives as Abl inhibitors identified by a pharmacophore-based database screening of commercially available compounds
[作者:Manetti, F; Falchi, F; Crespan, E; Schenone, S; Maga, G; Botta, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4328-4331 , 文章类型: Article,,卷期:2008年18-15]
- Suggestions derived from a previous ligand-based ligand design approach and docking calculations aimed at finding compound with affinity toward Abl and molecular scaffolds previously untested as Abl inhibitors, led to th...
- Synthesis of hydantoin analogues of (2S, 3R, 4S)-4-hydroxyisoleucine with insulinotropic properties
[作者:Sergent, D; Wang, Q; Sasaki, NA; Ouazzani, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4332-4335 , 文章类型: Article,,卷期:2008年18-15]
- The first synthesis of an optically pure (2R,3R,4S)-hydantoin 2, analogue of (2S,3R,4S)-4-hydroxyisoleucine, was achieved in two steps in un-optimized 35% overall yield from previously reported aldehyde synthon 1. (2R,3R...
- Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064
[作者:Akwabi-Ameyaw, A; Bass, JY; Caldwell, RD; Caravella, JA; Chen, L; Creech, KL; Deaton, DN; Jones, SA; Kaldor, I; Liu, Y; Madauss, KP; Marr, HB; McFadyen, RB; Miller, AB; Navas, F; Parks, DJ; Spearing, PK; Todd, D; Williams, SP; Wisely, GB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4339-4343 , 文章类型: Article,,卷期:2008年18-15]
- Starting from the known FXR agonist GW 4064 1a, a series of stilbene replacements were prepared. The 6-substituted 1-naphthoic acid 1b was an equipotent FXR agonist with improved developability parameters relative to 1a....
- Synthesis and evaluation of heteroaryl-ketone derivatives as a novel class of VEGFR-2 inhibitors
[作者:Chekler, ELP; Katoch-Rouse, R; Kiselyov, AS; Sherman, D; Ouyang, X; Kim, K; Wang, Y; Hadari, YR; Doody, JF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4344-4347 , 文章类型: Article,,卷期:2008年18-15]
- We have discovered novel inhibitors of VEGFR-2 kinase with low nanomolar potency in both enzymatic and cell-based assays. Active series are heteroaryl-ketone compounds containing a central aromatic ring with either an in...
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