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Mert Olgun Karataş Harun Uslu Suat Sarı Mehmet Abdullah Alagöz Arzu Karakurt Bülent Alıcı 《Journal of enzyme inhibition and medicinal chemistry》2016,31(5):760-772
Among many others, coumarin derivatives are known to show human carbonic anhydrase (hCA) inhibitory activity. Since hCA inhibition is one of the underlying mechanisms that account for the activities of some antiepileptic drugs (AEDs), hCA inhibitors are expected to have anti-seizure properties. There are also several studies reporting compounds with an imidazole and/or benzimidazole moiety which exert these pharmacological properties. In this study, we prepared fifteen novel coumarin-bearing imidazolium and benzimidazolium chloride, nine novel benzoxazinone-bearing imidazolium and benzimidazolium chloride derivatives and evaluated their hCA inhibitory activities and along with fourteen previously synthesized derivatives we scanned their anticonvulsant effects. As all compounds inhibited purified hCA isoforms I and II, some of them also proved protective against Maximal electroshock seizure (MES) and ScMet induced seizures in mice. Molecular docking studies with selected coumarin derivatives have revealed that these compounds bind to the active pocket of the enzyme in a similar fashion to that previously described for coumarin derivatives. 相似文献
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David Danko Daniela Bezdan Evan E. Afshin Sofia Ahsanuddin Chandrima Bhattacharya Daniel J. Butler Kern Rei Chng Daisy Donnellan Jochen Hecht Katelyn Jackson Katerina Kuchin Mikhail Karasikov Abigail Lyons Lauren Mak Dmitry Meleshko Harun Mustafa Beth Mutai Russell Y. Neches Stas Zubenko 《Cell》2021,184(13):3376-3393.e17
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Seventy‐five isolates of Fusarium oxysporum f.sp. cepae, the causal agent of basal plate rot on onion, were obtained from seven provinces of Turkey. The isolates were characterized by vegetative compatibility grouping (VCGs) and restriction fragment length polymorphism (RFLP) analysis of the nuclear ribosomal DNA intergenic spacer region (IGS). Forty‐eight vegetative compatibility groups were found, each containing a single isolate. Only one isolate formed strong heterokaryons with the reference isolates of VCG 0423. Five isolates were heterokaryon self‐incompatible. Restriction fragment analysis with six different enzymes revealed 13 IGS types among 75 F. oxysporum isolates from Turkey as well as 16 reference isolates from Colorado, USA. The majority of single‐member VCGs produced identical RFLP banding patterns with minor deviations, considerably different from those of the reference VCG isolates. These results suggested that isolates of F. oxysporum f.sp. cepae in Turkey derived from distinct clonal lineages and mutations at one or more vegetative compatibility loci restrict heterokaryon formation. 相似文献
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Kocpinar Enver Fehim Gonul Baltaci Nurdan Ceylan Hamid Kalin Seyda Nur Erdogan Orhan Budak Harun 《Biological trace element research》2020,194(1):135-144
Biological Trace Element Research - This study is aimed at evaluating the effect of dietary zinc-methionine (Zn-Met) supplementation during 3 months prepartum up to 9 months... 相似文献
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Drug resistance tuberculosis is one of the challenging tasks that dictates the desperate need for the development of new antitubercular agents which operate via novel modes of action. Here, we are reporting on 4‐aminoquinazolines as M. tuberculosis N‐acetylglucosamine‐1‐phosphate uridyltransferase (GlmUMTB) inhibitors to overcome the problem of the MDR‐TB. Amongst the synthesized compounds, two of them were observed to be the effective compounds of the series (IC50=6.4 μM (H37Rv), MIC=25 μM (MDR‐TB) and IC50=2.9 μM (H37Rv), MIC=6.25 μM (MDR‐TB), respectively). 相似文献
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Rezaei Motlagh Shiva Harun Razif Awang Biak Dayang Radiah Hussain Siti Aslina Omar Rozita Khezri Ramin Elgharbawy Amal A. 《Journal of applied phycology》2021,33(4):2015-2029
Journal of Applied Phycology - Lipids and eicosapentaenoic acid (EPA) compounds from Nannochloropsis oceanica biomass were extracted using a combination of ionic liquids (ILs) and... 相似文献
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This study aimed to investigate the associations of hepatocyte nuclear factor 4 (HNF4) alpha single nucleotide polymorphisms (SNPs) and haplotype with insulin resistance and metabolic syndrome parameters. Nine SNPs spanning the HNF4 alpha P2 promoter (rs4810424, rs1884613 and rs1884614) and coding region (rs2144908, rs6031551, rs6031552, rs1885088, rs1028583 and rs3818247) were genotyped in 160 subjects without diabetes or metabolic syndrome. The HNF4 alpha P2 promoter SNPs rs4810424, rs1884613 and rs1884614 were associated with insulin resistance (p = 0.017; 0.037; 0.024) and body mass index (BMI) (p = 0.03; 0.035; 0.039). The intron 1D SNP rs2144908 was associated with high-density lipoprotein cholesterol (HDLc) (p = 0.020) and the intron 9 SNP rs3818247 showed association with systolic (p = 0.02) and diastolic (p = 0.034) blood pressure. HNF4 alpha common haplotype CCCGTC associated with higher insulin resistance (p = 0.022), fasting blood glucose (FBG) (p = 0.035) and lower HDLc (p = 0.001). In conclusion, subjects with HNF4 alpha P2 variants and haplotypes have been shown to have a higher insulin resistance and are therefore at a higher risk for developing type 2 diabetes mellitus. 相似文献
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This study was conducted in Turkish patients with polycystic ovary syndrome to determine the frequency of I/D polymorphism genotypes of angiotensin converting enzyme gene, and to examine the role of this polymorphism in polycystic ovary syndrome development. Genomic DNA obtained from 200 persons (100 patients with polycystic ovary syndrome and 100 healthy controls) was used in the study. DNA was multiplied by polymerase chain reaction using I and D allele-specific primers. Polymerase chain reaction products were assessed with a charge coupled device (CCD) camera by being exposed to 2% agarose gel electrophoresis. There was statistically significant difference between the groups with respect to genotype distribution (p < 0.001). The D allele frequency was indicated as 68% and I allele was as 32% in the patients, whereas it was 51.5-48.5% respectively in the control group. As a result of our study we may assert that angiotensin converting enzyme gene I/D polymorphism DD genotype should be considered as a genetic marker in polycystic ovary syndrome development in this Turkish study population. 相似文献