- Benzoxaborole antimalarial agents. Part 2: Discovery of fluoro-substituted 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles
[作者:Zhang, YK; Plattner, JJ; Freund, YR; Easom, EE; Zhou, YS; Ye, L; Zhou, HC; Waterson, D; Gamo, FJ; Sanz, LM; Ge, M; Li, ZY; Li, LC; Wang, HL; Cui, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1299-1307 , 文章类型: Article,,卷期:2012年22-3]
- A series of new boron-containing benzoxaborole compounds was designed and synthesized for a continuing structure-activity relationship (SAR) investigation to assess the antimalarial activity changes derived from side-cha...
- [F-18]GE-180: A novel fluorine-18 labelled PET tracer for imaging Translocator protein 18 kDa (TSPO)
[作者:Wadsworth, H; Jones, PA; Chau, WF; Durrant, C; Fouladi, N; Passmore, J; O'Shea, D; Wynn, D; Morisson-Iveson, V; Ewan, A; Thaning, M; Mantzilas, D; Gausemel, I; Khan, I; Black, A; Avory, M; Trigg, W,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1308-1313 , 文章类型: Article,,卷期:2012年22-3]
- A series of tricyclic compounds have been synthesised and evaluated in vitro for affinity against Translocator protein 18 kDa (TSPO) and for preferred imaging properties. The most promising of the compounds were radiolab...
- Anion inhibition studies of an alpha-carbonic anhydrase from the living fossil Astrosclera willeyana
[作者:Ohradanova, A; Vullo, D; Pastorekova, S; Pastorek, J; Jackson, DJ; Worheide, G; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1314-1316 , 文章类型: Article,,卷期:2012年22-3]
- An alpha-carbonic anhydrase (CA, EC 4.2.1.1) isolated from the living fossil sponge Astrosclera willeyana, Astrosclerin, was investigated for its inhibition profile with simple inorganic anions, complex anions and other ...
- New bisabolane sesquiterpenoids from a marine-derived fungus Aspergillus sp isolated from the sponge Xestospongia testudinaria
[作者:Sun, LL; Shao, CL; Chen, JF; Guo, ZY; Fu, XM; Chen, M; Chen, YY; Li, R; de Voogd, NJ; She, ZG; Lin, YC; Wang, CY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1326-1329 , 文章类型: Article,,卷期:2012年22-3]
- Three new phenolic bisabolane sesquiterpenoid dimers, disydonols A-C (1-3), and one known compound (S)-(+)-sydonol (4) were isolated from the fermentation broth of a marine-derived fungus Aspergillus sp., which was isola...
- Pyrazoloquinolines as PDE10A inhibitors: Discovery of a tool compound
[作者:McElroy, WT; Tan, Z; Basu, K; Yang, SW; Smotryski, J; Ho, GD; Tulshian, D; Greenlee, WJ; Mullins, D; Guzzi, M; Zhang, XP; Bleickardt, C; Hodgson, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1335-1339 , 文章类型: Article,,卷期:2012年22-3]
- A series of pyrazoloquinolines, possessing (hetero)arylhydroxymethyl substituents at the quinoline C-4 position were evaluated as PDE10A inhibitors. Among these, methylpyrimidyl analogue 15 was identified as having good ...
- Substituents at the naphthalene C3 position of (-)-Cercosporamide derivatives significantly affect the maximal efficacy as PPAR gamma partial agonists
[作者:Furukawa, A; Arita, T; Fukuzaki, T; Satoh, S; Mori, M; Honda, T; Matsui, Y; Wakabayashi, K; Hayashi, S; Araki, K; Ohsumi, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1348-1351 , 文章类型: Article,,卷期:2012年22-3]
- Peroxisome proliferator-activated receptor gamma (PPAR gamma) is a potential drug target for treating type 2 diabetes. The selective PPAR gamma modulators (SPPARMs), which partially activate the PPAR gamma transcriptiona...
- Synthesis and carbonic anhydrase inhibitory properties of novel cyclohexanonyl bromophenol derivatives
[作者:Balaydin, HT; Senturk, M; Menzek, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1352-1357 , 文章类型: Article,,卷期:2012年22-3]
- The Naturally occurring novel cyclohexanonyl bromophenol 2(R)-2-(2,3,6-tribromo-4,5-dihydroxybenzyl) cyclohexanone (4) was synthesized as a racemic compound. Cyclohexylphenyl methane derivatives (10-17) with Br, OMe, CO,...
- Discovery of novel selective inhibitors for EGFR-T790M/L858R
[作者:Bai, F; Liu, HY; Tong, LJ; Zhou, W; Liu, L; Zhao, ZJ; Liu, XF; Jiang, HL; Wang, XC; Xie, H; Li, HL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1365-1370 , 文章类型: Article,,卷期:2012年22-3]
- Through a receptor-based and ligand-based combined virtual screening protocol, 21 novel compounds covering 15 scaffolds were identified as novel inhibitors for EGFR-T790M/L858R, among which, 12 of them were identified as...
- Synthesis and interaction with midkine of biotinylated chondroitin sulfate tetrasaccharides
[作者:Tamura, J; Tsutsumishita-Nakai, N; Nakao, Y; Kawano, M; Kato, S; Takeda, N; Nadanaka, S; Kitagawa, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1371-1374 , 文章类型: Article,,卷期:2012年22-3]
- Regiospecifically sulfated chondroitin sulfate repeating tetrasaccharides, CS-OO, GlcA beta-GalNAc beta-GlcA beta-GalNAc beta; CS-EE, GlcA beta-GalNAc(4S6S)beta-GlcA beta-GalNAc(4S6S)beta; and CS-AA, GlcA beta-GalNAc(4S)...
- An efficient synthesis of highly functionalized novel chromeno[4,3-b]pyrroles and indolizino[6,7-b]indoles as potent antimicrobial and antioxidant agents
[作者:Arumugam, N; Raghunathan, R; Almansour, AI; Karama, U,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1375-1379 , 文章类型: Article,,卷期:2012年22-3]
- A facile and efficient synthesis of novel chromeno[4,3-b]pyrroles has been accomplished by intramolecular 1,3-dipolar cycloaddition which on subsequent Pictet-Spengler cyclisation in presence of p-toluenesulfonic acid yi...
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