排序方式: 共有34条查询结果,搜索用时 46 毫秒
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John A. Lowe Shari L. DeNinno Jotham W. Coe Lei Zhang Scot Mente Raymond S. Hurst Robert J. Mather Karen M. Ward Alka Shrikhande Hans Rollema David E. Johnson Weldon Horner Roxanne Gorczyca F. David Tingley Rouba Kozak Mark J. Majchrzak Theresa Tritto Jen Sadlier Chris L. Shaffer Brenda Ellerbrock Laura L. McDowell 《Bioorganic & medicinal chemistry letters》2010,20(16):4749-4752
We report the synthesis of a series of [3.2.1]azabicyclic biaryl ethers as selective agonists of α3- and α6-containing nicotinic receptors. In particular, compound 17a from this series is a potent α3β4 and α6/4β4 receptor agonist in terms of both binding and functional activity. Compound 17a also shows potent in vivo activity in CNS-mediated animal models that are sensitive to antipsychotic drugs. Compound 17a may thus be a useful tool for studying the role of α3β4 and α6/4β4 nicotinic receptors in CNS pharmacology. 相似文献
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Alexandra Meziti Eleni Mente Konstantinos Ar. Kormas 《Systematic and applied microbiology》2012,35(7):473-482
The impact of different diets on the gut microbiota of reared Nephrops norvegicus was investigated based on bacterial 16S rRNA gene diversity. Specimens were collected from Pagasitikos Gulf (Greece) and kept in experimental rearing tanks, under in situ conditions, for 6 months. Treatments included three diets: frozen natural (mussel) food (M), dry formulated pellet (P) and starvation (S). Gut samples were collected at the initiation of the experiment, and after 3 and 6 months. Tank water and diet samples were also analyzed for bacterial 16S rRNA gene diversity. Statistical analysis separated the two groups fed or starved (M and P vs. S samples). Most gut bacteria were not related to the water or diet bacteria, while bacterial diversity was higher in the starvation samples. M and P samples were dominated by Gammaproteobacteria, Epsilonproteobacteria and Tenericutes. Phylotypes clustering in Photobacterium leiognathi, Shewanella sp. and Entomoplasmatales had high frequencies in the M and P samples but low sequence frequencies in S samples. The study showed that feeding resulted in the selection of specific species, which also occurs in the natural population, and might be associated with the animal's nutrition. 相似文献
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Emre Menteşe Hakan Bektaş Bahar Bilgin Sokmen Mustafa Emirik Demet Çakır Bahittin Kahveci 《Bioorganic & medicinal chemistry letters》2017,27(13):3014-3018
A new series of benzimidazole compounds including hydrazinecarbothioamide, 1,2,4-triazole, 1,3,4-oxadiazole and imine function were synthesized starting from 5,6-dichloro-2-cyclopropyl-1H-benzimidazole. All of the benzimidazole derivatives exhibited good urease inhibitor activity. Compound 6a proved to be the most potent showing an enzyme inhibitory activity with an IC50 = 0.06 µM. Molecular docking studies were also conducted on enzyme extracted from Jack bean urease to identify the binding mode of the newly synthesized compounds. 相似文献