نتایج جستجو برای: 12a
تعداد نتایج: 652 فیلتر نتایج به سال:
The Tropical Rainfall Measuring Mission (TRMM) is a NASA satellite project initiated to address a gap in our ability to accurately observe detailed rainfall patterns over the tropical continents and oceans. To support TRMM, several field campaigns were conducted. The TRMM-LBA (Large-scale Biosphere Atmosphere) experiment was conducted over the southwestern region of the Amazon (state of Rondôni...
We demonstrate strong evidence of entropy matching that rotating dyonic black holes in Einstein-Maxwell-Dilaton-Axion theory is holographically dual to a 2D conformal field (CFT). first investigate the duality on Kerr-Sen hole with nonvanishing dilaton and axion charges. The near-horizon geometry extremal spacetime possesses $SL(2,R)\ifmmode\times\else\texttimes\fi{}U(1)$ isometry where asympto...
In a previous study, we have identified 3-alkyl-1,5-diaryl-1H-1,2,4-triazoles to be a novel class of cannabinoid type 1 receptor (CB1R) antagonists. In order to expand the number of cannabinoid ligands with a central 1,2,4-triazole scaffold, we have synthesized a novel series of 1-benzyl-1H-1,2,4-triazoles, and some of them were evaluated by CB1R radioligand binding assays. Compound 12a showed ...
Lividamine and paromamine were converted into two key intermediate ethylenic aldehydes 10a and 10b. Reductive amination of the two aldehydes yielded the protected sisamine 11a and the three analogs 11b, 12a and 12b. These four derivatives were deprotected to yield the four pseudodisaccharides 1a, 1b, 2a and 2b which were less active in vitro than neamine against Escherichia coli ATCC 9637 and S...
Efficient synthesis of phenanthridin-6(5H)-one derivatives 12a-n in a four-component reaction of aldehyde hydrazone, aromatic aldehydes and malononitrile in Q-Tubes is reported. The results showed that the methodology has the advantage of being a one-pot synthesis of tricyclic systems in good yields. Potential routes leading to formation of compounds 12 are discussed. The structures of the synt...
A novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis. Structure-based drug design strategies led to the discovery of potent sub-micromolar inhibitors 11a-c and 12a-c from a weak-binding fragment-like s...
Further modification of salvinorin A (1a), the major active component of Salvia divinorum, has resulted in the synthesis of novel neoclerodane diterpenes with opioid receptor affinity and activity. We report in this study that oxadiazole 11a and salvidivin A (12a), a photooxygenation product of 1a, have been identified as the first neoclerodane diterpenes with kappa antagonist activity. This in...
C-Glycosyl-(S)- and (R)-alanines 12a and 12b were synthesized from the known beta-C-glycoside 1. The nitrogen function was introduced by aza-Claisen rearrangement of the allylic thiocyanate 7, derived from the corresponding alcohol 6. The absolute configuration of the newly created chiral carbon center (C-3) was assigned by X-ray diffraction analysis of the intermediate 3(S)-isothiocyanato-D-gl...
1090-7807/ 2016 The Authors. Published by Elsevier Inc. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/). Michael J. Knight a,⇑, Risto A. Kauppinen a,b a School of Experimental Psychology, University of Bristol, 12a Priory Road, Bristol, BS8 1TU, United Kingdom Clinical Research and Imaging Centre, University of Bristol, 60 St Michael’s Hill, ...
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