Design and synthesis of new quinoline hybrid derivatives and their antimicrobial, antimalarial and antitubercular activities

986-998All the molecules have been designed on the basis of previously reported active pharmacophores via molecular hybridization. A convenient protocol for the preparation of N-((2-(piperazin-1-yl) quinolin-3-yl)methyl)aniline derivatives via mutli-step synthesis has been described. Spectral analysis using Mass, 1H and 13C NMR spectral techniques have been studied in order to confirm the structure of synthesized end molecules. All synthesized compounds have been screened for in vitro antimicrobial, antimalarial and antitubercular activities. Structural activity relationship study (SAR) have also been discussed. Interestingly, target molecules are found to show good to excellent antibacterial, antifungal and antimalarial potency

Is a combination of varenicline and nicotine patch more effective in helping smokers quit than varenicline alone? A randomised controlled trial

This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited

Phylogenetic groups and cephalosporin resistance genes of Escherichia coli from diseased food-producing animals in Japan

A total of 318 Escherichia coli isolates obtained from different food-producing animals affected with colibacillosis between 2001 and 2006 were subjected to phylogenetic analysis: 72 bovine isolates, 89 poultry isolates and 157 porcine isolates. Overall, the phylogenetic group A was predominant in isolates from cattle (36/72, 50%) and pigs (101/157, 64.3%) whereas groups A (44/89, 49.4%) and D (40/89, 44.9%) were predominant in isolates from poultry. In addition, group B2 was not found among diseased food-producing animals except for a poultry isolate. Thus, the phylogenetic group distribution of E. coli from diseased animals was different by animal species. Among the 318 isolates, cefazolin resistance (minimum inhibitory concentrations: ≥32 μg/ml) was found in six bovine isolates, 29 poultry isolates and three porcine isolates. Of them, 11 isolates (nine from poultry and two from cattle) produced extended spectrum β-lactamase (ESBL). The two bovine isolates produced blaCTX-M-2, while the nine poultry isolates produced blaCTX-M-25 (4), blaSHV-2 (3), blaCTX-M-15 (1) and blaCTX-M-2 (1). Thus, our results showed that several types of ESBL were identified and three types of β-lactamase (SHV-2, CTX-M-25 and CTX-M-15) were observed for the first time in E. coli from diseased animals in Japan

Comparative genomics of European Avian Pathogenic E. coli (APEC)

Background Avian pathogenic Escherichia coli (APEC) causes colibacillosis, which results in significant economic losses to the poultry industry worldwide. However, the diversity between isolates remains poorly understood. Here, a total of 272 APEC isolates collected from the United Kingdom (UK), Italy and Germany were characterised using multiplex polymerase chain reactions (PCRs) targeting 22 equally weighted factors covering virulence genes, R-type and phylogroup. Following these analysis, 95 of the selected strains were further analysed using Whole Genome Sequencing (WGS). Results The most prevalent phylogroups were B2 (47%) and A1 (22%), although there were national differences with Germany presenting group B2 (35.3%), Italy presenting group A1 (53.3%) and UK presenting group B2 (56.1%) as the most prevalent. R-type R1 was the most frequent type (55%) among APEC, but multiple R-types were also frequent (26.8%). Following compilation of all the PCR data which covered a total of 15 virulence genes, it was possible to build a similarity tree using each PCR result unweighted to produce 9 distinct groups. The average number of virulence genes was 6-8 per isolate, but no positive association was found between phylogroup and number or type of virulence genes. A total of 95 isolates representing each of these 9 groupings were genome sequenced and analysed for in silico serotype, Multilocus Sequence Typing (MLST), and antimicrobial resistance (AMR). The UK isolates showed the greatest variability in terms of serotype and MLST compared with German and Italian isolates, whereas the lowest prevalence of AMR was found for German isolates. Similarity trees were compiled using sequencing data and notably single nucleotide polymorphism data generated ten distinct geno-groups. The frequency of geno-groups across Europe comprised 26.3% belonging to Group 8 representing serogroups O2, O4, O18 and MLST types ST95, ST140, ST141, ST428, ST1618 and others, 18.9% belonging to Group 1 (serogroups O78 and MLST types ST23, ST2230), 15.8% belonging to Group 10 (serogroups O8, O45, O91, O125ab and variable MLST types), 14.7% belonging to Group 7 (serogroups O4, O24, O35, O53, O161 and MLST type ST117) and 13.7% belonging to Group 9 (serogroups O1, O16, O181 and others and MLST types ST10, ST48 and others). The other groups (2, 3, 4, 5 and 6) each contained relatively few strains. However, for some of the genogroups (e.g. groups 6 and 7) partial overlap with SNPs grouping and PCR grouping (matching PCR groups 8 (13 isolates on 22) and 1 (14 isolates on 16) were observable). However, it was not possible to obtain a clear correlation between genogroups and unweighted PCR groupings. This may be due to the genome plasticity of E. coli that enables strains to carry the same virulence factors even if the overall genotype is substantially different. Conclusions The conclusion to be drawn from the lack of correlations is that firstly, APEC are very diverse and secondly, it is not possible to rely on any one or more basic molecular or phenotypic tests to define APEC with clarity, reaffirming the need for whole genome analysis approaches which we describe here. This study highlights the presence of previously unreported serotypes and MLSTs for APEC in Europe. Moreover, it is a first step on a cautious reconsideration of the merits of classical identification criteria such as R typing, phylogrouping and serotyping

Investigations of split-injection ratios and dwell times on the spray characteristics using a solenoid high-pressure multi-hole injector

Copyright © 2021 The Author(s). An on-going challenge with Gasoline direct injection (GDI) engines is achieving rapid activation of the exhaust catalyst during cold starts, in order to reduce the Nitrogen Oxide (NOx) emissions. Injecting late in the compression stroke, in the efforts to form a stratified mixture, provides the fuel insufficient time to be entrained with the surrounding charge. This results in locally fuel rich diffusion combustion and the formation of high levels of particulate matter. Employing a split injection strategy can help tackle these issues. The current study examines the effects of a split injection strategy on the spray characteristics. Varying pulse width (PW) combinations, split ratios and dwell times are investigated using a Solenoid actuated high pressure injector. The injected quantity and the droplet characteristics of a target plume are investigated. The experiments were performed in a constant volume spray chamber. The droplet velocities and sizes were measured using Phase Doppler Particle Anemometry (PDA). Short and large PWs, in the range of 0.3–0.8 ms, were investigated. The results revealed that the highest injected quantity of fuel was measured with the shortest dwell time of 2 ms, owing to increased interactions between the injection events, which led to larger Sauter mean diameters (SMDs) measured. The SMDs for the shorter PW of 0.4 ms were generally larger than 0.8 ms PW. The droplets in this case were affected by the closely spaced opening and closing events of the Solenoid valve.EPSRC; Changa

Synthesis and biological evaluation of 2-azetidinone and thiazolidine-4-one derivatives containing dibenzothiazepine nucleus

1051-1059In the present study, 3-chloro-1-(dibenzo[b,f][1,4]thiazepin-11-ylamino)-4-(substituted phenyl)azetidin-2-one 2a–k and 3-(dibenzo[b,f][1,4]thiazepin-11-ylamino)-2-(substituted phenyl)thiazolidin-4-one 3a–k derivatives have been synthesized via the reaction of (Z)-11-(2-(substituted benzylidene) hydrazinyl) dibenzo[b,f][1,4] thiazepine 1a-k with chloro acetyl chloride and thiogycolic acid respectively under mild reaction conditions. The structures of all synthesised compounds have been assigned on the basis of FT-IR, 1H and 13C NMR spectral data as well as elemental analysis. The title compounds have been screened for their preliminary in vitro antimicrobial activity against a panel of pathogenic strains and in vitro antimycobacterial activity against Mycobacterium tuberculosis H37 Rv