AN EFFICIENT SYNTHESIS OF SOME NOVEL BIOACTIVE AZETIDINONE DERIVATIVES INCLUDING 5-(BENZOFURAN-2-YL) AND 1-PHENYL-1H-PYRAZOLE-3-CARBOXAMIDE MOIETY
INTERNATIONAL JOURNAL OF PHARMACEUTICAL SCIENCES AND RESEARCH
Authors: Idrees, M.; Kola, S.; Siddiqui, N. J.
Abstract
In continuation of our efforts in the development of novel drugs, in the present article we have described synthesis of a series of novel azetidinones derivatives (4a-i) containing 5-(benzofuran-2-yl) and 1-phenyl-1H-pyrazole-3-carboxamide moiety, with excellent yields and without formation of undesirable side products from cyclo condensation reaction of N'- (benzylidene)-5- (benzofuran-2-yl) -1 -phenyl -1H -pyrazole- 3-carbohydrazide derivatives (3a-i) with chloro acetyl chloride in the presence of triethylamine in DMF. Carbohydrazones of aryl aldehydes (3a-i) used as the starting compound was obtained by one-pot condensation of 5-(benzofuran-2-yl)-1-phenyl-1H-pyrazole-3-carbohydrazide (1) with various substituted aromatic aldehydes (2a-i) and a catalytic amount of acetic acid in ethanol. The structures of newly synthesized compounds have been established through elemental analysis and spectral studies like IR, H-1 NMR, C-13-NMR and Mass spectra. All the synthesized compounds were screened for their in-vitro antibacterial activity against different strains of microbes such as S. aureus, E. coli, P. vulgaris and S. typhi at different concentration. The result of the bioactivity confirmed that most of the newly synthesized compounds showed the significant activity when compared with the standard drug Chloramphenicol which might be due to the cyclic carbonyl group present in azetidinones.
Salmonella enterica Phylogeny Based on Whole-Genome Sequencing Reveals Two New Clades and Novel Patterns o Horizontally Acquired Genetic Elements
MBIO
Authors: Worley, Jay; Meng, Jianghong; Allard, Marc W.; Brown, Eric W.; Timme, Ruth E.
Abstract
Using whole-genome sequence (WGS) data from the GenomeTrakr network, a globally distributed network of laboratories sequencing foodborne pathogens, we present a new phylogeny of Salmonella enterica comprising 445 isolates from 266 distinct serovars and originating from 52 countries. This phylogeny includes two previously unidentified S. enterica subsp. enterica clades. Serovar Typhi is shown to be nested within Glade A. Our findings are supported by both phylogenetic support, based on a core genome alignment, and Bayesian approaches, based on single-nucleotide polymorphisms. Serovar assignments were refined by in silico analysis using SeqSero. More than 10% of serovars were either polyphyletic or paraphyletic. We found variable genetic content in these isolates relating to gene mobilization and virulence factors which have different distributions within clades. Gifsy-1-and Gifsy-2-like phages appear more prevalent in Glade A; other viruses are more evenly distributed. Our analyses reveal IncFII is the predominant plasmid replicon in S. enterica. Few core or Glade-defining virulence genes are observed, and their distributions appear probabilistic in nature. Together, these patterns demonstrate that genetic exchange within S. enterica is more extensive and frequent than previously realized, which significantly alters how we view the genetic structure of the bacterial species. IMPORTANCE Rapid improvements in nucleotide sequencing access and affordability have led to a drastic increase in availability of genetic information. This information will improve the accuracy of molecular descriptions, including serovars, within S. enterica. Although the concept of serovars continues to be useful, it may have more significant limitations than previously understood. Furthermore, the discrete absence or presence of specific genes can be an unstable indicator of phylogenetic identity. Whole-genome sequencing provides more rigorous tools for assessing the distributions of these genes. Our phylogenetic and genetic content analyses reveal how active genetic elements are dynamically distributed within a species, allowing us to better understand genetic reservoirs and underlying bacterial evolution.