- Synthesis and characterization of multifunctional hyperbranched polyesters as prospective contrast agents for targeted MRI
[作者:Sideratou, Z; Tsiourvas, D; Theodossiou, T; Fardis, M; Paleos, CM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4177-4181 , 文章类型: Article,,卷期:2010年20-14]
- Based on a commercially available hyperbranched aliphatic polyester, novel multifunctional gadolinium complexes were prepared bearing protective PEG chains, a folate targeting ligand and EDTA or DTPA chelate moieties. Th...
- Interaction of aminoadamantane derivatives with the influenza A virus M2 channel-Docking using a pore blocking model
[作者:Eleftheratos, S; Spearpoint, P; Ortore, G; Kolocouris, A; Martinelli, A; Martin, S; Hay, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4182-4187 , 文章类型: Article,,卷期:2010年20-14]
- Interaction of aminoadamantanes with the influenza A virus M2 proton channel was analyzed by docking simulations of a series of synthetic aminoadamantane derivatives, of differing binding affinity, into the crystal struc...
- High-throughput sequencing for the identification of binding molecules from DNA-encoded chemical libraries
[作者:Buller, F; Steiner, M; Scheuermann, J; Mannocci, L; Nissen, I; Kohler, M; Beisel, C; Neri, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4188-4192 , 文章类型: Article,,卷期:2010年20-14]
- DNA-encoded chemical libraries are large collections of small organic molecules, individually coupled to DNA fragments that serve as amplifiable identification bar codes. The isolation of specific binders requires a quan...
- Synthesis of diaryl-azo derivatives as potential antifungal agents
[作者:Xu, H; Zeng, XW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4193-4195 , 文章类型: Article,,卷期:2010年20-14]
- As compared with a commercially available agricultural fungicide hymexazol, some phenyl-azo phenol derivatives (e.g., 4a, 4b, 4f, 4n, 4q, 4u, and 4v) exhibited the more promising and pronounced antifungal activities in v...
- Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat
[作者:Coleman, PJ; Schreier, JD; Roecker, AJ; Mercer, SP; McGaughey, GB; Cox, CD; Hartman, GD; Harrell, CM; Reiss, DR; Doran, SM; Garson, SL; Anderson, WB; Tang, C; Prueksaritanont, T; Winrow, CJ; Renger, JJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4201-4205 , 文章类型: Article,,卷期:2010年20-14]
- Orexins are excitatory neuropeptides that regulate arousal and sleep. Orexin receptor antagonists promote sleep and offer potential as a new therapy for the treatment of insomnia. In this Letter, we describe the synthesi...
- Synthesis of two marine farnesylacetones that dilate the basilar arteries of rabbits
[作者:Oh, S; Park, BG; Ham, J; Lee, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4206-4209 , 文章类型: Article,,卷期:2010年20-14]
- We have synthesized novel vasodilatation farnesylacetones 1 and 2, which are major active constituents of Sargassum siliquastrum collected from the coast of the East Sea in Korea, in 9 steps. A test of the vasodilatation...
- Pre-clinical characterization of aryloxypyridine amides as histamine H-3 receptor antagonists: Identification of candidates for clinical development
[作者:Letavic, MA; Aluisio, L; Atack, JR; Bonaventure, P; Carruthers, NI; Dugovic, C; Everson, A; Feinstein, MA; Fraser, IC; Hoey, K; Jiang, XH; Keith, JM; Koudriakova, T; Leung, P; Lord, B; Lovenberg, TW; Ly, KS; Morton, KL; Motley, ST; Nepomuceno, D; Rizzolio, M; Rynberg, R; Sepassi, K; Shelton, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4210-4214 , 文章类型: Article,,卷期:2010年20-14]
- The pre-clinical characterization of novel aryloxypyridine amides that are histamine H-3 receptor antagonists is described. These compounds are high affinity histamine H-3 ligands that penetrate the CNS and occupy the hi...
- Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Benzyl derivatives with broad potency against resistant mutant viruses
[作者:Kertesz, DJ; Brotherton-Pleiss, C; Yang, MM; Wang, ZG; Lin, XF; Qiu, ZX; Hirschfeld, DR; Gleason, S; Mirzadegan, T; Dunten, PW; Harris, SF; Villasenor, AG; Hang, JQ; Heilek, GM; Klumpp, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4215-4218 , 文章类型: Article,,卷期:2010年20-14]
- An analysis of the binding motifs of known HIV-1 non-nucleoside reverse transcriptase inhibitors has led to discovery of novel piperidine-linked aminopyrimidine derivatives with broad activity against wildtype as well as...
- Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers
[作者:Lee, JE; Koh, HY; Seo, SH; Baek, YY; Rhim, H; Cho, YS; Choo, H; Pae, AN,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4219-4222 , 文章类型: Article,,卷期:2010年20-14]
- T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pain. In this study, as a part of our ongoing efforts to develop potent T-type calcium channel blockers, w...
- Discovery of aminopyridines substituted with benzoxazole as orally active c-Met kinase inhibitors
[作者:Cho, SY; Han, SY; Ha, JD; Ryu, JW; Lee, CO; Jung, H; Kang, NS; Kim, HR; Koh, JS; Lee, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4223-4227 , 文章类型: Article,,卷期:2010年20-14]
- We report the synthesis and biological evaluation of aminopyridines substituted with benzoxazole. The SAR of the aminopyridines was explored to improve the inhibitory activity against c-Met and to decrease hERG affinity....
- Chemoselective regulation of TREK2 channel: Activation by sulfonate chalcones and inhibition by sulfonamide chalcones
[作者:Kim, EJ; Ryu, HW; Curtis-Long, MJ; Han, J; Kim, JY; Cho, JK; Kang, D; Park, KH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4237-4239 , 文章类型: Article,,卷期:2010年20-14]
- Although it has not been extensively studied, a significant volume of literature suggests that TREK2 will probably turn out to be an important channel in charge of tuning neuronal transmitter and hormone levels. Thus, ph...
- Synthesis of Tc-99m labeled 1,2,3-triazole-4-yl c-met binding peptide as a potential c-met receptor kinase positive tumor imaging agent
[作者:Kim, EM; Joung, MH; Lee, CM; Jeong, HJ; Lim, ST; Sohn, MH; Kim, DW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4240-4243 , 文章类型: Article,,卷期:2010年20-14]
- The mesenchymal-epithelial transition factor (c-Met), which is related to tumor cell growth, angiogenesis and metastases, is known to be overexpressed in several tumor types. In this study, we synthesized technetium-99m ...
- Montmorillonite K-10 catalyzed cyclization of N-ethoxycarbonyl-N '-arylguanidines: Access to pyrimido[4,5-c]carbazole and pyrimido[5,4-b]indole derivatives
[作者:Debray, J; Zeghida, W; Baldeyrou, B; Mahieu, C; Lansiaux, A; Demeunynck, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4244-4247 , 文章类型: Article,,卷期:2010年20-14]
- Two new heterocycles, pyrimido[4,5-c]carbazole and pyrimido[5,4-b]indole, were prepared in three steps from 3-aminocarbazole and 3-aminoindole, respectively. The key Friedel-Crafts intramolecular cyclization was realized...
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