200 research outputs found

    DESIGN, SYNTHESIS AND MOLECULAR DOCKING STUDY OF HYBRID QUINOLINE-4-YL-OXADIAZOLES/OXATHIADIAZOLES AS POTENT ANTIFUNGAL AGENTS

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    Objective: The aim of the present work was to design and synthesize hybrid quinoline-4-yl-oxadiazoles/oxathiadiazole derivatives and evaluate them for in vitro antifungal activity against human disease causing pathogens.Methods: The compounds 5(a-d), 6(a-d) and 7(a-d) were efficiently synthesized in good yields. The synthesized compounds were characterized using 1H NMR, 13C NMR and Mass spectra. The synthesized compounds were screened for in vitro antifungal activity and minimum inhibitory concentration (MIC) values were determined using standard agar method. Molecular docking study was performed against fungal enzyme P450 cytochrome lanosterol 14α-demethylase using VLife MDS 4.3 software.Results: The synthesized compounds had shown good to moderate in vitro antifungal activity. The compound 6a (MIC range = 15-25 µg/ml) from 1,2,3,5-oxathiadiazole-2-oxide series showed most potent activity amongst the synthesized compounds when compared with standard clotrimazole (MIC range = 12.5-25 µg/ml). The molecular docking study of synthesized compounds showed good binding interactions against active site of fungal enzyme P450 cytochrome lanosterol 14α-demethylase.Conclusion: The results of in vitro antifungal activity and molecular docking study revealed that the synthesized compounds have potential antifungal activity and can be further optimized and developed as a lead compound.Â

    Correlation between reflectivity and photoluminescent properties of porous silicon films

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    Porous silicon (PS) layers were formed on p-type, oriented, 1–5 Ω cm resistivity Cz silicon wafers by electrochemical etching in an HF:C2H5OH (1:2 by volume) electrolyte at room temperature at a constant current density 20 mA/cm2. The etching duration was varied to achieve PS layers of different morphologies and thicknesses. Both the photoluminescence (PL) and the total diffused reflectivity spectra of the PS layers were measured. It was found that for the PS layers grown for etching durations of less than 90 s the PL emission is insignificant and reflectivity is quite low. Such PS layers can be used as antireflection coatings (ARC) on solar cells. The PS layers formed for etching durations greater than 90 s show a significant PL emission in 500–800 nm range with peak lying in 630–660 nm wavelength range. When etching duration increases from 90 s to 8 min the PL intensity increases and the PL peak shows a blue shift. With further increase in etching duration the PL intensity decreases and PL peak shows a red shift. The reflectivity of the photoluminescent layers increases with etching duration showing a highest value for a sample grown for 8 min. Further increase in etching duration up to 20 min the reflectivity decreases and then increases. Striking observation is that both the PL emission intensity and reflectivity in the wavelength range of 550–800 nm are maximum for the PS layer grown for the etching duration of 8 min

    Efficient one-pot synthesis, molecular docking and in silico ADME prediction of bis-(4-hydroxycoumarin-3-yl) methane derivatives as antileishmanial agents

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    Bis-(4-hydroxycoumarin-3-yl) methane derivatives 3(a-l) were synthesized from 4-hydroxycoumarin and substituted aromatic aldehydes using succinimide-N-sulfonic acid as catalyst and evaluated for their in vitro antileishmanial activity against promastigotes form of Leishmania donovani. Compounds 3a (IC50= 155 μg/mL), 3g (IC50= 157.5 μg/mL) and 3l (IC50= 150 μg/mL) were shown significant antileishmanial activity when compared with standard sodium stibogluconate (IC50= 490 μg/mL). Also, synthesized compounds 3(a-l) did not show cytotoxicity against HeLa cell line upto tested concentrations. Further, molecular docking study against Adenine phosphoribosyltransferase of Leishmania donovani showed good binding interactions. ADME properties were analyzed and showed good oral drug candidate like properties. The synthesized compounds were also shown good drug likeness and drug score values when compared with drugs currently used in therapy. The present study has helped us in identifying a new lead that could be exploited as a potential antileishmanial agent

    Autonomous vehicles: A study of implementation and security

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    Autonomous vehicles have been invented to increase the safety of transportation users. These vehicles can sense their environment and make decisions without any external aid to produce an optimal route to reach a destination. Even though the idea sounds futuristic and if implemented successfully, many current issues related to transportation will be solved, care needs to be taken before implementing the solution. This paper will look at the pros and cons of implementation of autonomous vehicles. The vehicles depend highly on the sensors present on the vehicles and any tampering or manipulation of the data generated and transmitted by these can have disastrous consequences, as human lives are at stake here. Various attacks against the different type of sensors on-board an autonomous vehicle are covered

    Cyber physical systems: A smart city perspective

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    Cyber-physical system (CPS) is a terminology used to describe multiple systems of existing infrastructure and manufacturing system that combines computing technologies (cyber space) into the physical space to integrate human interaction. This paper does a literature review of the work related to CPS in terms of its importance in today’s world. Further, this paper also looks at the importance of CPS and its relationship with internet of things (IoT). CPS is a very broad area and is used in variety of fields and some of these major fields are evaluated. Additionally, the implementation of CPS and IoT is major enabler for smart cities and various examples of such implementation in the context of Dubai and UAE are researched. Finally, security issues related to CPS in general are also reviewed

    Mutations in phosphodiesterase 6 identified in familial cases of retinitis pigmentosa.

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    To delineate the genetic determinants associated with retinitis pigmentosa (RP), a hereditary retinal disorder, we recruited four large families manifesting cardinal symptoms of RP. We localized these families to regions on the human genome harboring the α and β subunits of phosphodiesterase 6 and identified mutations that were absent in control chromosomes. Our data suggest that mutations in PDE6A and PDE6B are responsible for the retinal phenotype in these families

    Loss of function mutations in RP1 are responsible for retinitis pigmentosa in consanguineous familial cases.

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    PurposeThis study was undertaken to identify causal mutations responsible for autosomal recessive retinitis pigmentosa (arRP) in consanguineous families.MethodsLarge consanguineous families were ascertained from the Punjab province of Pakistan. An ophthalmic examination consisting of a fundus evaluation and electroretinography (ERG) was completed, and small aliquots of blood were collected from all participating individuals. Genomic DNA was extracted from white blood cells, and a genome-wide linkage or a locus-specific exclusion analysis was completed with polymorphic short tandem repeats (STRs). Two-point logarithm of odds (LOD) scores were calculated, and all coding exons and exon-intron boundaries of RP1 were sequenced to identify the causal mutation.ResultsThe ophthalmic examination showed that affected individuals in all families manifest cardinal symptoms of RP. Genome-wide scans localized the disease phenotype to chromosome 8q, a region harboring RP1, a gene previously implicated in the pathogenesis of RP. Sanger sequencing identified a homozygous single base deletion in exon 4: c.3697delT (p.S1233Pfs22*), a single base substitution in intron 3: c.787+1G>A (p.I263Nfs8*), a 2 bp duplication in exon 2: c.551_552dupTA (p.Q185Yfs4*) and an 11,117 bp deletion that removes all three coding exons of RP1. These variations segregated with the disease phenotype within the respective families and were not present in ethnically matched control samples.ConclusionsThese results strongly suggest that these mutations in RP1 are responsible for the retinal phenotype in affected individuals of all four consanguineous families

    Pathogenic mutations in TULP1 responsible for retinitis pigmentosa identified in consanguineous familial cases.

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    PurposeTo identify pathogenic mutations responsible for autosomal recessive retinitis pigmentosa (arRP) in consanguineous familial cases.MethodsSeven large familial cases with multiple individuals diagnosed with retinitis pigmentosa were included in the study. Affected individuals in these families underwent ophthalmic examinations to document the symptoms and confirm the initial diagnosis. Blood samples were collected from all participating members, and genomic DNA was extracted. An exclusion analysis with microsatellite markers spanning the TULP1 locus on chromosome 6p was performed, and two-point logarithm of odds (LOD) scores were calculated. All coding exons along with the exon-intron boundaries of TULP1 were sequenced bidirectionally. We constructed a single nucleotide polymorphism (SNP) haplotype for the four familial cases harboring the K489R allele and estimated the likelihood of a founder effect.ResultsThe ophthalmic examinations of the affected individuals in these familial cases were suggestive of RP. Exclusion analyses confirmed linkage to chromosome 6p harboring TULP1 with positive two-point LOD scores. Subsequent Sanger sequencing identified the single base pair substitution in exon14, c.1466A>G (p.K489R), in four families. Additionally, we identified a two-base deletion in exon 4, c.286_287delGA (p.E96Gfs77*); a homozygous splice site variant in intron 14, c.1495+4A>C; and a novel missense variation in exon 15, c.1561C>T (p.P521S). All mutations segregated with the disease phenotype in the respective families and were absent in ethnically matched control chromosomes. Haplotype analysis suggested (p<10(-6)) that affected individuals inherited the causal mutation from a common ancestor.ConclusionsPathogenic mutations in TULP1 are responsible for the RP phenotype in seven familial cases with a common ancestral mutation responsible for the disease phenotype in four of the seven families
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