- 4-Anilino-6-phenyl-quinoline inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2)
[作者：Olsson, H; Sjo, P; Ersoy, O; Kristoffersson, A; Larsson, J; Norden, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4738-4740 , 文章类型： Article，,卷期：2010年20-16]
- A class of inhibitors of mitogen activated protein kinase-activated kinase 2 (MK2) was discovered via high-throughput screening. This compound class demonstrates activity against the enzyme with sub-mu M IC50 values, and...
- Synthesis and structure-activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiazol-2-amines derivatives as NPY Y5 antagonists
[作者：Biagetti, M; Leslie, CP; Mazzali, A; Seri, C; Pizzi, DA; Bentley, J; Genski, T; Di Fabio, R; Zonzini, L; Caberlotto, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4741-4744 , 文章类型： Article，,卷期：2010年20-16]
- A novel class of small molecule NPY Y5 antagonists based around an azabicyclo[3.1.0]hexane scaffold was identified through modi. cation of a screening hit. Structure-activity relationships and efforts undertaken to achie...
- Inhibition of the R1 fragment of the cadmium-containing zeta-class carbonic anhydrase from the diatom Thalassiosira weissflogii with anions
[作者：Viparelli, F; Monti, SM; De Simone, G; Innocenti, A; Scozzafava, A; Xu, Y; Morel, FMM; Supuran, CT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4745-4748 , 文章类型： Article，,卷期：2010年20-16]
- We investigated the catalytic activity and inhibition of both the zinc and cadmium-containing R1 fragment of the zeta-class carbonic anhydrase (CA, EC 4.2.1.1) from the marine diatom Thalassiosira weissflogii. Our data p...
- A novel series of [3.2.1] azabicyclic biaryl ethers as alpha 3 beta 4 and alpha 6/4 beta 4 nicotinic receptor agonists
[作者：Lowe, JA; DeNinno, SL; Coe, JW; Zhang, L; Mente, S; Hurst, RS; Mather, RJ; Ward, KM; Shrikhande, A; Rollema, H; Johnson, DE; Horner, W; Gorczyca, R; Tingley, FD; Kozak, R; Majchrzak, MJ; Tritto, T; Sadlier, J; Shaffer, CL; Ellerbrock, B; Osgood, SM; MacDougall, MC; McDowell, LL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4749-4752 , 文章类型： Article，,卷期：2010年20-16]
- We report the synthesis of a series of [3.2.1]azabicyclic biaryl ethers as selective agonists of alpha 3- and alpha 6-containing nicotinic receptors. In particular, compound 17a from this series is a potent alpha 3 beta ...
- Exploration of a new series of CCR5 antagonists: Multi-dimensional optimization of a sub-series containing N-substituted pyrazoles
[作者：Lemoine, RC; Petersen, AC; Setti, L; Jekle, A; Heilek, G; deRosier, A; Ji, CH; Berry, P; Rotstein, DM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4753-4756 , 文章类型： Article，,卷期：2010年20-16]
- The introduction of N-substituted pyrazoles in a new series of CCR5 antagonists was shown to substantially increase antiviral activity. (C) 2010 Elsevier Ltd. All rights reserved.
- Synthesis and cannabinoid-1 receptor binding affinity of conformationally constrained analogs of taranabant
[作者：Kopka, IE; Lin, LS; Jewell, JP; Lanza, TJ; Fong, TM; Shen, CP; Lao, ZJ; Ha, S; Castonguay, LG; Van der Ploeg, L; Goulet, MT; Hagmann, WK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4757-4761 , 文章类型： Article，,卷期：2010年20-16]
- The design, synthesis, and binding activity of ring constrained analogs of the acyclic cannabinoid-1 receptor (CB1R) inverse agonist taranabant 1 are described. The initial inspiration for these taranabant derivatives wa...
- Synthesis and pharmacological evaluation of condensed heterocyclic 6-substituted 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole and 1,3,4-oxadiazole derivatives of isoniazid
[作者：Gilani, SJ; Khan, SA; Siddiqui, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4762-4765 , 文章类型： Article，,卷期：2010年20-16]
- The significance of this study was to prepare various isoniazid derivatives by introducing the isoniazid core into several molecules to explore the possibilities of some altered biological activities. Series of 6-substit...
- Synthesis of novel oxime-containing pyrazole derivatives and discovery of regulators for apoptosis and autophagy in A549 lung cancer cells
[作者：Zheng, LW; Li, Y; Ge, D; Zhao, BX; Liu, YR; Lv, HS; Ding, J; Miao, JY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4766-4770 , 文章类型： Article，,卷期：2010年20-16]
- A series of novel oxime-containing pyrazole derivatives were synthesized by the reaction of ethyl 3-phenyl-1H-pyrazole-5-carboxylate derivatives and 2-bromo-1-phenylethanone followed by the reaction with hydroxylamine hy...
- Refinement of the pharmacophore of 3,4-dihydroquinazoline-2(1H)-thiones for their anti-melanogenesis activity
[作者：Thanigaimalai, P; Sharma, VK; Lee, KC; Yun, CY; Kim, Y; Jung, SH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4771-4773 , 文章类型： Article，,卷期：2010年20-16]
- In order to de. ne the structural requirements of quinazoline-2(1H)-thiones 1 for their inhibitory activity on melanogenesis, a novel series of 3,4-dihydroquinazoline-2(1H)-thiones (3a-h) were prepared and screened for t...
- Inhibitors of osteoclastogenesis from Lawsonia inermis leaves
[作者：Nguyen, XC; Nguyen, XN; Nguyen, PT; Nguyen, HN; Nguyen, TD; Hoang, LTA; Le, MH; Phan, VK; Chau, VM; Won, JH; Chung, WY; Kim, YH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4782-4784 , 文章类型： Article，,卷期：2010年20-16]
- Ten phenolic compounds (1-10) were isolated from a methanol extract of Lawsonia inermis leaves including two new ones, lawsoniasides A (1) and B (2). Their structures were elucidated by spectroscopic methods (NMR and FTI...
- Aspergillus oryzae type III polyketide synthase CsyA is involved in the biosynthesis of 3,5-dihydroxybenzoic acid
[作者：Seshime, Y; Juvvadi, PR; Kitamoto, K; Ebizuka, Y; Nonaka, T; Fujii, I,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4785-4788 , 文章类型： Article，,卷期：2010年20-16]
- As a novel superfamily of type III polyketide synthases in microbes, four genes csyA, csyB, csyC, and csyD, were found in the genome of Aspergillus oryzae, an industrially important filamentous fungus. In order to analyz...
- Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: Structure-activity relationship of P2 ' substituents
[作者：Truong, AP; Probst, GD; Aquino, J; Fang, L; Brogley, L; Sealy, JM; Hom, RK; Tucker, JA; John, V; Tung, JS; Pleiss, MA; Konradi, AW; Sham, HL; Dappen, MS; Toth, G; Yao, NH; Brecht, E; Pan, H; Artis, DR; Ruslim, L; Bova, MP; Sinha, S; Yednock, TA; Zmolek, W; Quinn, KP; Sauer, JM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4789-4794 , 文章类型： Article，,卷期：2010年20-16]
- Herein we describe further evolution of hydroxyethylamine inhibitors of BACE-1 with enhanced permeability characteristics necessary for CNS penetration. Variation at the P2' position of the inhibitor with more polar subs...
- Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors
[作者：Blackburn, C; Duffey, MO; Gould, AE; Kulkarni, B; Liu, JX; Menon, S; Nagayoshi, M; Vos, TJ; Williams, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4795-4799 , 文章类型： Article，,卷期：2010年20-16]
- A high throughput screen identified N-aroylpyrazoline 1 as a selective inhibitor of the V600E mutant of B-Raf kinase. Parallel synthesis of acyl, aroyl, and sulfonyl derivatives led to the identification of several poten...
- Discovery and optimization of pyrazoline compounds as B-Raf inhibitors
[作者：Duffey, MO; Adams, R; Blackburn, C; Chau, RW; Chen, S; Galvin, KM; Garcia, K; Gould, AE; Greenspan, PD; Harrison, S; Huang, SC; Kim, MS; Kulkarni, B; Langston, S; Liu, JX; Ma, LT; Menon, S; Nagayoshi, M; Rowland, RS; Vos, TJ; Xu, TL; Yang, JJ; Yu, SX; Zhang, Q,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4800-4804 , 文章类型： Article，,卷期：2010年20-16]
- The discovery of novel pyrazoline derivatives as B-Raf (V600E) inhibitors is described in this report. Chemical modi. cation of the pyrazoline scaffold led to the development of SAR and identified potent and selective in...
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