- Design and synthesis of potent carboxylic acid DGAT1 inhibitors with high cell permeability
[作者:Bali, U; Barba, O; Dawson, G; Gattrell, WT; Horswill, JG; Pan, DA; Procter, MJ; Rasamison, CM; Smith, CPS; Taylor-Warne, A; Wong-Kai-In, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:824-828 , 文章类型: Article,,卷期:2012年22-2]
- A series of potent carboxylic acid DGAT1 inhibitors with high permeability were developed from a virtual screening hit. Strategies were employed to reduce Pgp substrate recognition and increase passive permeability, resu...
- Synthesis and binding affinity at alpha 4 beta 2 and alpha 7 nicotinic acetylcholine receptors of new analogs of epibatidine and epiboxidine containing the 7-azabicyclo[2.2.1]hept-2-ene ring system
[作者:Dallanoce, C; Matera, C; Pucci, L; Gotti, C; Clementi, F; De Amici, M; De Micheli, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:829-832 , 文章类型: Article,,卷期:2012年22-2]
- A group of novel racemic nicotinic ligands structurally related to epibatidine or epiboxidine [(+/-)-10-(+/-)-17] was synthesized through a palladium-catalyzed cross-coupling between the appropriate vinyl triflate and a ...
- Study on binding modes between cellobiose and beta-glucosidases from glycoside hydrolase family 1
[作者:Liu, LF; Zeng, ZT; Zeng, GM; Chen, M; Zhang, Y; Zhang, JC; Fang, X; Jiang, M; Lu, LH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:837-843 , 文章类型: Article,,卷期:2012年22-2]
- The hydrolysis of cellobiose by beta-glucodisases is an important step of cellulose biodegradation. However, the interactive mechanism between cellobiose and beta-glucosidases is still unclear until now. Thus, in this st...
- Synthesis of 5-benzyl-2-phenylpyrazolo[1,5-a]pyrazin-4,6(5H,7H)-dione derivatives and discovery of an apoptosis inducer for H322 lung cancer cells
[作者:Lv, HS; Kong, XQ; Ming, QQ; Jin, X; Miao, JY; Zhao, BX,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:844-849 , 文章类型: Article,,卷期:2012年22-2]
- A series of substituted 5-benzyl-2-phenylpyrazolo[1,5-a]pyrazin-4,6(5H,7H)-dione derivatives was synthesized by one-step reaction of ethyl 3-phenyl-1H-pyrazole-5-carboxylate derivatives and N-arylalkyl-2-chloroacetamide....
- Novel potent 2,5-pyrrolidinedione peptidomimetics as aminopeptidase N inhibitors. Design, synthesis and activity evaluation
[作者:Li, QB; Fang, H; Wang, XJ; Hu, GY; Wang, Q; Xu, WF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:850-853 , 文章类型: Article,,卷期:2012年22-2]
- A series of novel aminopeptidase N inhibitors with 2,5-pyrrolidinedione scaffold were chemically synthesized. Their preliminary biological activities in enzyme kinetics and cell assay in vitro and anti-metastasis profile...
- SAR studies of C2 ethers of 2H-pyrano[2,3-d]pyrimidine-2,4,7(1H,3H)-triones as nicotinic acid receptor (NAR) agonist
[作者:Huang, XH; Su, J; Rao, AU; Tang, HQ; Zhou, W; Zhu, XH; Chen, X; Liu, ZD; Huang, Y; Degrado, S; Xiao, D; Qin, J; Aslanian, R; McKittrick, BA; Greenfeder, S; van Heek, M; Chintala, M; Palani, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:854-858 , 文章类型: Article,,卷期:2012年22-2]
- Based on in house screening lead compound 1 for the NAR project, SAR studies have been focused on the modification of the C2 ethers of the pyrimidinedione core structure. In this effort, an unpredictable SAR trend was ov...
- Dithiocarbamates are strong inhibitors of the beta-class fungal carbonic anhydrases from Cryptococcus neoformans, Candida albicans and Candida glabrata
[作者:Monti, SM; Maresca, A; Viparelli, F; Carta, F; De Simone, G; Muhlschlegel, FA; Scozzafava, A; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:859-862 , 文章类型: Article,,卷期:2012年22-2]
- A series of N-mono- and N,N-disubstituted dithiocarbamates have been investigated as inhibitors of three beta-carbonic anhydrases (CAs, EC 4.2.1.1) from the fungal pathogens Cryptococcus neoformans, Candida albicans and ...
- A DNA aptamer sensor for 8-oxo-7,8-dihydroguanine
[作者:Roy, J; Chirania, P; Ganguly, S; Huang, HD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:863-867 , 文章类型: Article,,卷期:2012年22-2]
- Abasic site-containing DNA duplex is a versatile structural motif that can be used for the design of purine aptamers and sensors. In this study, several modifications were introduced to the abasic site to explore possibl...
- Amides of xanthurenic acid as zinc-dependent inhibitors of Lp-PLA(2)
[作者:Lin, ECK; Hu, Y; Amantea, CM; Pham, LM; Cajica, J; Okerberg, E; Brown, HE; Fraser, A; Du, LL; Kohno, Y; Ishiyama, J; Kozarich, JW; Shreder, KR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:868-871 , 文章类型: Article,,卷期:2012年22-2]
- AX10185, the phenyl amide of xanthurenic acid, was found to be a sub-100 nM inhibitor of Lp-PLA(2). However, in the presence of EDTA the inhibitory activity of AX10185 was extinguished while the enzymatic activity of Lp-...
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