Several N-thiophosphonyl-glutamates were found to be potent competitive inhibitors of a zinc-dependent glutamyl hydrolase, carboxypeptidase G (CPG). Weak inhibition exhibited by an analogous N-phosphonyl-glutamate suggests that the enhanced potency of the phosphonamidothioates is due to the pres...
A protected 2-azido-2-deoxymannose is a key intermediate in the synthesis of alexine [(1R,2R,3R,7S,8S)-3-hydroxymethyl-1,2,7-trihydroxypyrrolizidine], 3-epialexine and 7-epialexine from D-glucose.
Recently the government of Ethiopia paid great attention to livestock and fish production sectors of the country. As evidence, the sector is organized in the form of ministry, Ethiopian Ministry of Livestock and Fisheries. This is great progress in the history of the country. These and other foc...
To construct a high-performance engineered endo-inulinase for fructo-oligosaccharides (FOS) production from inulin, an inulin binding module (IBM) was fused into either N- or C-terminal of an endo-inulinase. After heterologous expression, purification and characterization, the C-terminal fusion ...
Five soft metal complexes (1–5) of a 16-membered O2S3-macrocycle (L) with different topologies and coordination modes, including discrete to infinite forms, and endo-, exo-, and endo/exo-coordination, were prepared and structurally characterized. Both mercury(II) complexes, [Hg(L)(NO3)2] (1) an...
Several lines of evidence have shown that defects in the endo-lysosomal autophagy degradation pathway and the ubiquitin-proteasome system play a role in Alzheimer's Disease (AD) pathogenesis and pathophysiology. Early pathological changes, such as marked enlargement of endosomal compartment...
Studies on endo-inulinases from yeast are scarce, compared to those from other microbial sources. In this study, a novel endo-inulinase from Lipomyces starkeyi NRRL Y-11557 was identified, expressed in its soluble form, and characterized its physicochemically properties, together with its enzyma...
Autophagy and endo-lysosomal degradation are two parallel degradation pathways essential for maintaining neuronal health and function. Autophagosomes and endosomes sequester cellular cargo through different mechanisms, but these pathways converge upon fusion with lysosomes. Both pathways are spa...
Hitherto, how salt bridges contribute towards the structure-function of endo-mannanases has not been demonstrated. In the present study, we revealed that ManB-1601 (GH26 endo-mannanase from Bacillus sp.) has eight salt bridges which are highly conserved among GH26 endo-mannanases from Bacillus s...
The curing kinetics of endo-dicyclopentadiene (endo-DCPD) was analyzed using isothermal differential scanning calorimetry by experimentally acquiring kinetic parameters according to model fitting approaches. To investigate the effect of the decelerator, the curing kinetics of endo-DCPD with diff...
We synthesized a fluorogenic probe with a high-mannose type heptasaccharide structure to detect the hydrolytic activity of endo-β-N-acetylglucosaminidase from Streptomyces plicatus (Endo-H). The heptasaccharide derivative (1) was labeled with an N-methylanthraniloyl group as a reporter dye at t...
Approximately 40% of mammalian genome is made of transposable elements (TEs), and during specific biological processes, such as gametogenesis, they may be activated by global demethylation, so strict silencing mechanism is indispensable for genomic stability. Here, we performed small RNA-seq on ...
3-Chloro-2-fluorobut-2-en-4-olide (13) and 2-fluorobut-2-en-4-olide (14) were prepared by a six step synthesis starting from 1,2-dibromo-1,2-dichloro-1,2-difluoroethane (5). UV-initiated addition of 5 to ethylene afforded 1,4-dibromo-1,2-dichloro-1,2-difluorobutane (6a) that was easily dehydroch...
Protoporphyrinogen oxidase (PPO, E.C. 1.3.3.4) is the action target for several structurally diverse herbicides. A series of novel 4-(difluoromethyl)-1-(6-halo-2-substituted-benzothiazol-5-yl)-3-methyl-1H-1,2,4-triazol-5(4H)-ones 2a–z were designed and synthesized via the ring-closure of two or...
A series of bioactive Cu (II), Co (II), Ni (II) and Fe (III) complexes of the novel disperse azo dye ligand was obtained from the reaction between 5, 5, 7-trimethyl-4, 5, 6, 7-tetrahydro-1, 3-benzothiazol-2-amine and 2-thioxodihydropyrimidine-4, 6 (1H, 5H)-dione by the conventional diazo-couplin...
A series of new methyl 6-deoxy-6-[N′-alkyl/aryl-N″-(benzothiazol-2-yl)]guanidino-α-d-glucopyranosides were obtained from the reaction of an alkyl/aryl amine in the presence of HgCl2 and sugar-thiourea derivatives, followed by the removal of protecting groups. The sugar-thiourea derivatives we...
We report the synthesis of a Schiff base 1-(E)-[(6-methoxy-1,3-benzothiazol-2-yl)imino]methyl]naphthalen-2-ol from the reaction of 2-hydroxy-1-naphtaldehyde with 2-amino-6-methoxybenzothiazole. The molecular structure of the title compound was experimentally determined using X-ray single-crystal...
The high resolution 1H NMR spectra of four 3-ethyl-4-hydroxy-4-phenylpiperidines 1–4 have been recorded in CDCl3, C6D6, and (CD3)2CO and analysed. These compounds exist in chair conformation with axial orientation of hydroxyl group at C(4) and equatorial orientation of the remaining substituent...
Compound 6 was synthesized by regiospecific addition of 4-chlorothiophenol to diazoketone 5 in the presence of a rhodium (II) acetate catalyst. An annelation process pressumably proceeded via initial attack of methylamine on the bromoacrylic ester to give the methyl α-(methylamino)methylacrylat...
In vitro metabolism studies on a series of 3,5-bis(trifluoromethyl)benzyl ethers have identified 3,5-bis(trifluoromethyl)benzoic acid as a significant metabolite possibly arising via oxidation of the benzylic position. A methyl group was introduced in an effort to suppress this route of metaboli...
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