Biomimetic enterobactin analogue mediates iron-uptake and cargo transport into E. coli and P. aeruginosa

The design, synthesis and biological evaluation of the artificial enterobactin analogue EntKL and several fluorophore-conjugates thereof are described. EntKL provides an attachment point for cargos such as fluorophores or antimicrobial...

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Design, Synthesis and Biological Evaluation of Pyrimidine Analogues as SecA Inhibitors

10.21203/rs.3.rs-188471/v1 ◽

2021 ◽

Author(s):

FANTE BAMBA ◽

Jinshan Jin ◽

Arpana S. Chaudhary ◽

Phang C. Tai ◽

Binghe Wang

Keyword(s):

Escherichia Coli ◽

Antimicrobial Agents ◽

Biological Evaluation ◽

Design Synthesis ◽

E Coli ◽

Secretion Pathway ◽

Antimicrobial Studies ◽

Pyrimidine Analogues ◽

Pyrimidine Analogs ◽

Synthesis And Biological Evaluation

Abstract SecA, a key component of the bacterial Sec-dependent secretion pathway, is an attractive target for the development of new antimicrobial agents. We have previously reported pyrimidine analogs as SecA inhibitors. Herein, we report an extension of the earlier work in the synthesis and evaluation of a series of 15 5-cyanothiouracil derivatives as SecA inhibitors. All the compounds have been evaluated for their inhibition of SecA ATPase (EcSecAN68) and for their antimicrobial activity against Escherichia coli NR698 (a leaky mutant) and Bacillus anthracis Sterne. Twelve compounds showed IC50 of less than 6.3 µM when tested against EcSecAN68. In antimicrobial studies against E. coli NR698, six compounds showed MIC of less than 12.5 µM with three being less than 6.3 µM. Against B. anthracis Sterne, three compounds showed MIC of less than 6.3 µM.

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Design, synthesis and evaluation of anti-inflammatory, analgesic and antibacterial activity of 2, 4, 6-trisubstituted quinazoline derivatives

Ovidius University Annals of Chemistry ◽

10.2478/auoc-2018-0014 ◽

2018 ◽

Vol 29 (2) ◽

pp. 97-102

Author(s):

Nivrati Jain ◽

Harshita Jain ◽

Ashish Jain ◽

Veerasamy Ravichandran ◽

Prateek Jain

Keyword(s):

Antibacterial Activity ◽

Antibacterial Agents ◽

Biological Evaluation ◽

Spectroscopy Analysis ◽

Design Synthesis ◽

E Coli ◽

Quinazoline Derivatives ◽

Anti Inflammatory ◽

Synthesis And Biological Evaluation ◽

Mass Spectroscopy Analysis

Abstract We described here the synthesis and biological evaluation of a series of 2, 4, 6-trisubstituted quinazoline derivatives as potential anti-inflammatory, analgesic and antibacterial agents. The synthesized compounds were characterized by FTIR, 1H NMR and mass spectroscopy analysis. We found that the compounds 6b, 6e, 6g, 6h and 6j showed better anti-inflammatory activity than indomethacin. Compounds 6b, 6e, 6h, 6j and 6l were found to exhibit appreciable analgesic activity, and 6b, 6g and 6k showed good antibacterial activity against Gram (+) bacteria: B. subtilis, S. aureus, S. epidermis, and Gram (-) bacteria: E. coli, P. aeruginosa and K. pneumoniae. Compound 6b showed overall better anti-inflammatory, analgesic and antibacterial activity among the synthesized compounds. The results of the present study could be helpful for the designing of effective anti-inflammatory, analgesic and antibacterial agents.

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