rac- and meso-Cyclohexanoids: Their α-, β-glycosidases,antibacterial, antifungal activities,and molecular docking studies

An efficient and versatile synthesis method has been postulated for hydroxymethylated rac - and meso-cyclohexanoid derivatives. The synthesis of these stereoisomers was achieved easily with traditional methods using hexahydroisobenzofuran 6 , prepared from commercially available cis-hydrophthalic anhydride. The study, involving diastereoselective epoxidation and cis-hydroxylation, was conducted to obtain epoxy-, cis-, and trans-diol-furans 7, 8 , and 9 . After sulfamic acid-catalyzed ring-opening reaction of the epoxide and furan rings, rac- and meso-tetraacetates 14, 15 , and 16 were afforded. Hydrolysis of acetate groups with ammonia in absolute methanol yielded the desired tetrols rac -17 , meso -18 , and meso -19 . All structures, after purification by chromatographic methods and elucidation by spectral techniques, were screened against α- and β-glucosidases. Compounds 7, 8, 10, 17, 18 , and 19 were also evaluated for their antibacterial and antifungal activity against some selected synthesized compounds with varying degrees of inhibitory effects on the growth of different pathogenic microorganisms by the well-diffusion method. In addition, Saccharomyces cerevisiae α-glucosidase molecular modeling studies were performed for all rac- and meso-compounds 7, 8, 10, 17, 18 , and 19 .     

Design,synthesis, and biological evaluation of 1‐ethyl‐3‐(thiazol‐2‐yl)urea derivatives as Escherichia coli DNA gyrase inhibitors

Discovery of novel DNA gyrase B inhibitors remains an attractive field in the search for new antibacterial drugs to overcome the known bacterial resistance mechanisms. In the present study, we designed and synthesized novel ethylurea derivatives of 4,5,6,7‐tetrahydrobenzo[1,2‐d]thiazole‐2,6‐diamine, 2‐(2‐aminothiazol‐4‐yl)acetic acid, and benzo[1,2‐d]thiazole‐2,6‐diamine and evaluated their Escherichia coli DNA gyrase inhibition. The most potent DNA gyrase inhibitors in the prepared library of compounds were benzo[1,2‐d]thiazoles 32–34 , 36 , and 37 with IC₅₀ values in the low micromolar range. The most promising inhibitors identified were evaluated against selected Gram‐positive and Gram‐negative bacterial strains. Compound 33 showed a MIC of 50 μM against an E. coli efflux pump‐defective strain, which suggests that efflux decreases the on‐target concentrations of these compounds.     

Safety and efficacy of retrograde intrarenal surgery in geriatric patients by age groups

International Urology and Nephrology - To evaluate the effects of aging on the success rate of retrograde intrarenal surgery (RIRS) and the development of medical and surgical complications by...     

Identification of Three Novel and One Known Mutation in the WFS1 Gene in Four Unrelated Turkish Families: The Role of Homozygosity Mapping in the Early Diagnosis

Objective:Bi-allelic mutations in the wolframin gene (WFS1) cause Wolfram syndrome 1 (WS1 or DIDMOAD) characterized by non-autoimmune diabetes mellitus, optic atrophy, diabetes insipidus, sensorineural deafness, urinary tract abnormalities, and neuropsychiatric disorders. Patients presenting with an incomplete phenotype of WS1 were evaluated using homozygosity mapping and subsequent whole-exome sequencing.Methods:Four unrelated consanguineous Turkish families, including seven affected children, and their unaffected parents and siblings were evaluated. Homozygosity mapping was performed, followed by whole-exome sequencing of WFS1. Mutations were classified according to results of “in silico” analyses, protein prediction, and functional consequences.Results:Homozygosity mapping confirmed shared homozygous regions on chromosome 4 (chr4p16.1) between the affected individuals, that was absent in their unaffected siblings. Exome sequencing identified three novel (c.1215T>A, c.554G>A, c.1525_1540dup) and one known (c.1522_1523delTA) mutations in WFS1. All mutations were predicted to cause stop codon leading to early termination of protein synthesis and complete loss-of-function. All patients were found to be homozygous for the change, with parents and other unaffected siblings being carriers.Conclusion:Our study expands the mutation spectrum of WSF1 mutations with three novel mutations. Homozygosity mapping may provide enrichment for molecular genetic analysis and early diagnosis of WS1 patients with incomplete phenotype, particularly in consanguineous pedigrees.     

Effect of chitosan nanoparticle,QMix, and EDTA on TotalFill BC sealers’ dentinal tubule penetration: a confocal laser scanning microscopy study

Odontology - The aim of the present study was to compare the effect of chitosan nanoparticle, QMix, and 17% EDTA on the penetrability of a calcium silicate-based sealer into dentinal tubules using...     

Phytoremediation of Water Polluted by Thallium,Cadmium, Zinc,and Lead with the Use of Macrophyte Callitriche cophocarpa

The objective of the present work was to study the phytoremediation capacity of Callitriche cophocarpa concerning water contaminated with thallium (Tl), cadmium (Cd), zinc (Zn), and lead (Pb) derived from the natural environment. We found that after a 10-day incubation period, shoots of C. cophocarpa effectively biofiltrated the water so that it met (for Cd, Zn, and Pb) appropriate quality standards. The order of accumulation of the investigated elements by shoots (mg kg^?1 dry weight) were as follows: Zn (1120) < Tl (251) < Cd (71) < Pb (35). The order of bioconcentration factors were as follows: Cd (1177) < Tl (1043) < Zn (718) < Pb (597). According to Microtox bioassay, C. cophocarpa significantly eradicated polluted water toxicity. During the experiment, the physiological status of plants was monitored by taking measurements of photosystem II activity (maximum efficiency of PSII, photochemical fluorescence quenching, nonphotochemical fluorescence quenching, and quantum efficiency of PSII), photosynthetic pigment contents, and shoot morphology. Plants exposed to metallic pollution did not exhibit significant changes in their physiological status compared with the control. This work is potentially applicable to the future use of C. cophocarpa in the phytoremediation of polluted, natural watercourses.     

Clinical comparison between the bleaching efficacy of light‐emitting diode and diode laser with sodium perborate

The aim of this clinical study was to test the efficacy of a light‐emitting diode (LED) light and a diode laser, when bleaching with sodium perborate. Thirty volunteers were selected to participate in the study. The patients were randomly divided into two groups. The initial colour of each tooth to be bleached was quantified with a spectrophotometer. In group A, sodium perborate and distilled water were mixed and placed into the pulp chamber, and the LED light was source applied. In group B, the same mixture was used, and the 810 nm diode laser was applied. The final colour of each tooth was quantified with the same spectrophotometer. Initial and final spectrophotometer values were recorded. Mann–Whitney U‐test and Wicoxon tests were used to test differences between both groups. Both devices successfully whitened the teeth. No statistical difference was found between the efficacy of the LED light and the diode laser.