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1.
Fluoro-substituted and heteroaromatic compounds are valuable intermediates for a variety of applications in pharma- and agrochemistry and synthetic chemistry. This study investigates the chemoenzymatic preparation of chiral alcohols bearing a heteroaromatic ring with an increasing degree of fluorination in α-position. Starting from readily available picoline derivatives prochiral α-halogenated acyl moieties were introduced with excellent selectivity and 64–95 % yield. The formed carbonyl group was subsequently reduced to the corresponding alcohols using the alcohol dehydrogenase from Lactobacillus kefir, yielding an enantiomeric excess of 95–>99 % and up to 98 % yield.  相似文献   
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Recently, investigations of the complex mechanisms of allostery have led to a deeper understanding of G protein-coupled receptor (GPCR) activation and signaling processes. In this context, muscarinic acetylcholine receptors (mAChRs) are highly relevant due to their exemplary role in the study of allosteric modulation. In this work, we compare and discuss two sets of putatively dualsteric ligands, which were designed to connect carbachol to different types of allosteric ligands. We chose derivatives of TBPB [1-(1′-(2-tolyl)-1,4′-bipiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one] as M1-selective putative bitopic ligands, and derivatives of benzyl quinolone carboxylic acid (BQCA) as an M1 positive allosteric modulator, varying the distance between the allosteric and orthosteric building blocks. Luciferase protein complementation assays demonstrated that linker length must be carefully chosen to yield either agonist or antagonist behavior. These findings may help to design biased signaling and/or different extents of efficacy.  相似文献   
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Yu  Zhi  Shi  Xiuzhi  Zhou  Jian  Rao  Dijun  Chen  Xin  Dong  Wenming  Miao  Xiaohu  Ipangelwa  Timo 《Engineering with Computers》2021,37(2):991-1006
Engineering with Computers - The indirect and accurate determination of blast-induced rock movement has important significance in the reduction of ore loss and dilution and in the protection of...  相似文献   
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There is a demand for a clean label of ice cream in the food industry. To meet this requirement, alternative surfactants and hydrocolloids without an additive number have to be found. Here, a caseinate hydrolysate with improved interfacial properties was investigated as such an additive. Replacing only the surfactant resulted in ice cream characteristics, comparable to using a commercial emulsifier (INS 472b). Thus, a clean labeling of the surfactant using this hydrolysate is possible. By contrast, replacing the hydrocolloid additionally led to an unfavorable ice cream texture and stability.  相似文献   
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In this paper, a novel constitutive model combining continuum damage with embedded discontinuity is developed for explicit dynamic analyses of quasi‐brittle failure phenomena. The model is capable of describing the rate‐dependent behavior in dynamics and the three phases in failure of quasi‐brittle materials. The first phase is always linear elastic, followed by the second phase corresponding to fracture‐process zone creation, represented with rate‐dependent continuum damage with isotropic hardening formulated by utilizing consistency approach. The third and final phase, involving nonlinear softening, is formulated by using an embedded displacement discontinuity model with constant displacement jumps both in normal and tangential directions. The proposed model is capable of describing the rate‐dependent ductile to brittle transition typical of cohesive materials (e.g., rocks and ice). The model is implemented in the finite element setting by using the CST elements. The displacement jump vector is solved for implicitly at the local (finite element) level along with a viscoplastic return mapping algorithm, whereas the global equations of motion are solved with explicit time‐stepping scheme. The model performance is illustrated by several numerical simulations, including both material point and structural tests. The final validation example concerns the dynamic Brazilian disc test on rock material under plane stress assumption. Copyright © 2014 John Wiley & Sons, Ltd.  相似文献   
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文章介绍了搭载人类自体干细胞的纤维支架技术及其在软组织再生中的应用优势。选用藻酸盐材料结合人体干细胞搭载关键技术制成的纤维支架,同时具有促进血管再生和触发成脂分化的能力。  相似文献   
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