47 research outputs found
3-Phenyl-2-(prop-2-ynÂyloxy)-1-benzofuro[3,2-d]pyrimidin-4(3H)-one
In the title compound, C19H12N2O3, the 1-benzofuro[3,2-d]pyrimidinone unit is approximately planar, the maximum deviation from the mean plane being 0.045â
(1)â
Ă
. The attached phenyl ring makes a dihedral angle of 86.73â
(6)° with the fused ring system. The packing of the molÂecules in the crystal structure is mainly governed by CâHâŻÏ hydrogen-bonding interÂactions
Ethyl 2-methyl-6-(propan-2-ylÂamino)-4-sulfanylÂidene-3H,11H-pyrimido[1,6-c]quinazoline-1-carboxylÂate
The title compound, C18H22N4O2S, contains a substituted pyrimidine ring fused to both a benzene ring and a substituted thioxopyrimidine ring. The pyrimidine and thioxopyrimidine rings adopt distorted chair conformations. In the crystal, adjacent molÂecules are linked by pairs of NâHâŻS and NâHâŻO hydrogen bonds to generate centrosymmetric R
2
2(8) and R
2
2(16) loops, respectively. This combination leads to [100] chains of molÂecules
Ethyl 1-(6-chloro-3-pyridylmethÂyl)-5-methyl-1H-1,2,3-triazole-4-carboxylÂate
In the title compound, C12H13ClN4O2, the triazole ring carries methyl and ethoxyÂcarbonyl groups, and is bound via a methylÂene bridge to a chloroÂpyridine unit. There is evidence for significant electron delocalization in the triazolyl system. IntraÂmolecular CâHâŻO and interÂmolecular CâHâŻN hydrogen bonds stabilize the structure
3,3âČ-(1,4-PhenylÂene)bisÂ[2-(propylÂamino)Âbenzofuro[3,2-d]pyrimidin-4(3H)-one] ethanol disolvate
The title compound, C32H28N6O4·2C2H5OH, consists of two 2-(propylÂamino)Âbenzofuro[3,2-d]pyrimidin-4(3H)-one units connected, via one of the pyrimidine N atoms, to a bridging benzene ring in the 1,4 positions. Two ethanol solvent molÂecules are also present. The main molÂecule lies on a center of symmetry located at the center of the benzene ring. The fused-ring system of the benzofuro[3,2-d]pyrimidine moiety is nearly planar (r.m.s. deviation = 0.016â
Ă
) and forms a dihedral angle of 78.21â
(7)° with the central benzene ring. The crystal structure features OâHâŻO and NâHâŻO interÂactions. The C atoms of the propylÂamino side chain in the main molÂecule and the ethyl group in the solvent molÂecule are disordered over two positions, with site-occupancy factors 0.34:0.66 and 0.42:0.58, respectively
Rap2B promotes migration and invasion of human suprarenal epithelioma
The aim of our study was to elucidate the role of Rap2B in the development of human suprarenal epithelioma and to investigate the effect of Rap2B on suprarenal epithelioma cells migration and invasion. We use tissue microarray and immunohistochemistry to evaluate Rap2B staining in 75 suprarenal epithelioma tissues and 75 tumor-adjacent normal renal tissues. And the expression of Rap2B protein in human suprarenal epithelioma cells and tissues was detected by western blot simultaneously. The role of Rap2B in suprarenal epithelioma cells migration and invasion was detected by using wound healing assay, cell migration assay, and matrigel invasion assay. After that, we performed western blot analysis and gelatin zymography to detect MMP-2 protein expression and enzyme activity. Our research showed that Rap2B expression was increased in tumor tissues compared with tumor-adjacent normal renal tissues. But no correlation was found between Rap2B expression and clinicopathological parameters. In addition, we found that Rap2B promoted the cell migration and invasion abilities, and Rap2B increased MMP-2 expression and enzyme activity in suprarenal epithelioma cells. Our data indicated that Rap2B expression is significantly increased in human suprarenal epithelioma and Rap2B can promote the cell migration and invasion abilities, which may provide a new target for the treatment of suprarenal epithelioma
3-Isopropyl-2-p-tolÂyloxy-5,6,7,8-tetraÂhydro-1-benzothieno[2,3-d]pyrimidin-4(3H)-one
In the title compound, C20H22N2O2S, the central thienoÂpyrimidine ring system is essentially planar, with a maximum displacement of 0.023â
(2)â
Ă
. The attached cycloÂhexene ring is disordered over two possible conformations, with an occupancy ratio of 0.776â
(12):0.224â
(12). Neither interÂmolecular hydrogen-bonding interÂactions nor ÏâÏ stacking interÂactions are present in the crystal structure. The molÂecular conformation and crystal packing are stabilized by three intraÂmolecular CâHâŻO hydrogen bonds and two CâHâŻÏ interÂactions
Pharmacokinetics of Acetaminophen and Metformin Hydrochloride in Rats After Exposure to Simulated High Altitude Hypoxia
The pharmacokinetic characteristics of drugs were altered under high altitude hypoxia, thereby affecting the absorption, distribution, metabolism, and excretion of drug. However, there are few literatures on the pharmacokinetic changes of antipyretic and pain-relieving drugs and cardiovascular system drugs at high altitude. This study aimed to evaluate the pharmacokinetics of acetaminophen and metformin hydrochloride in rats under simulated high altitude hypoxia condition. Mechanically, the protein and mRNA expression of uridine diphosphate glucuronyltransferase 1A1 (UGT1A1) and organic cation transporter 2 (OCT2) were investigated by enzyme linked immunosorbent assay (ELISA) and quantitative real-time polymerase chain reaction (qRT-PCR), respectively. Compared with the normoxia group, the t1/2 and AUC of acetaminophen were significantly increased, and the CL/F was significantly decreased in rats after exposure to simulated high altitude hypoxia. The t1/2 of metformin hydrochloride was significantly increased by simulated high altitude hypoxia. No significant differences in AUC and CL/F of metformin hydrochloride were observed when comparing the hypoxia group with the normoxia group. The protein and mRNA expression of UGT1A1 and OCT2 were decreased significantly under hypoxia in rats. This study found obvious changes in the pharmacokinetics of acetaminophen and metformin hydrochloride in rats after exposure to simulated high altitude hypoxia, and they might be due to significant decreases in the expressions of UGT1A1 and OCT2. To sum up, our data suggested that the pharmacokinetics of acetaminophen and metformin hydrochloride should be reexamined, and the optimal dose should be reassessed under hypoxia exposure
Robust estimation of bacterial cell count from optical density
Optical density (OD) is widely used to estimate the density of cells in liquid culture, but cannot be compared between instruments without a standardized calibration protocol and is challenging to relate to actual cell count. We address this with an interlaboratory study comparing three simple, low-cost, and highly accessible OD calibration protocols across 244 laboratories, applied to eight strains of constitutive GFP-expressing E. coli. Based on our results, we recommend calibrating OD to estimated cell count using serial dilution of silica microspheres, which produces highly precise calibration (95.5% of residuals <1.2-fold), is easily assessed for quality control, also assesses instrument effective linear range, and can be combined with fluorescence calibration to obtain units of Molecules of Equivalent Fluorescein (MEFL) per cell, allowing direct comparison and data fusion with flow cytometry measurements: in our study, fluorescence per cell measurements showed only a 1.07-fold mean difference between plate reader and flow cytometry data
Global urban environmental change drives adaptation in white clover
Urbanization transforms environments in ways that alter biological evolution. We examined whether urban environmental change drives parallel evolution by sampling 110,019 white clover plants from 6169 populations in 160 cities globally. Plants were assayed for a Mendelian antiherbivore defense that also affects tolerance to abiotic stressors. Urban-rural gradients were associated with the evolution of clines in defense in 47% of cities throughout the world. Variation in the strength of clines was explained by environmental changes in drought stress and vegetation cover that varied among cities. Sequencing 2074 genomes from 26 cities revealed that the evolution of urban-rural clines was best explained by adaptive evolution, but the degree of parallel adaptation varied among cities. Our results demonstrate that urbanization leads to adaptation at a global scale
Extraction of magnesium from garnierite by carbothermal reduction in vacuum
The aim of the traditional pyrometallurgical processes is to extract nickel and iron in garnierite, but it is difficult to extract magnesium of higher value in minerals. Aimed at solving this problem, the extraction of magnesium from garnierite is proposed and studied in this study. The effects of different reduction temperatures, different reduction times and dosage of CaO additions in experiments were investigated. The experimental results indicate that the extraction rate of magnesium can reach 93.23% when the mass ratio of mineral/reductant is 100:28.3, system pressure is 50 Pa, reduction temperature is 1823 K, and reduction time is 120 min, and, at the same time, the purity of metal magnesium in the condensate can be up to 91.88%. Under these conditions, the extraction rate of magnesium can increase to 99.45% by adding 25 wt% CaO, and the purity of the metal magnesium in the condensate exceeds 90%. CaO as the additive can effectively improve the extraction rate of magnesium and promote the recovery and utilization of magnesium. The mechanism is that CaO replaces âOâMgâ in the âOâMgâOâSiâOâ structure to form free MgO, which is reduced to Mg vapor by carbon and condensed into magnesium metal in the condensation zone to achieve the purpose of removing and collecting Mg from the garnierite. At the same time, the reduced slag is rich in Ni and Fe, which can be used for the extraction of Ni and Fe. Compared with the traditional pyrometallurgical process, the process can extract magnesium from garnierite, and the process is short and its operation is simple, which is a potential technology