Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Structure-Antibacterial Activity Relationships Of N-Substituted-(D-/L-Alaninyl) 1H-1,2,3-Triazolylmethyl Oxazolidinones

Version 1 : Received: 30 August 2018 / Approved: 30 August 2018 / Online: 30 August 2018 (14:35:03 CEST)

A peer-reviewed article of this Preprint also exists.

Phillips, O.A.; Udo, E.E.; D’silva, R.J. Structure-Antibacterial Activity Relationships of N-Substituted-(d-/l-Alaninyl) 1H-1,2,3-Triazolylmethyl Oxazolidinones. Sci. Pharm. 2018, 86, 42. Phillips, O.A.; Udo, E.E.; D’silva, R.J. Structure-Antibacterial Activity Relationships of N-Substituted-(d-/l-Alaninyl) 1H-1,2,3-Triazolylmethyl Oxazolidinones. Sci. Pharm. 2018, 86, 42.

Abstract

Bacterial resistance towards existing class of antibacterial drugs continues to increase posing significant threat to clinical usefulness of these drugs. This increasing and alarming rates of antibacterial resistance development and the decline in the number of new antibacterial drugs approval continue to serve as major impetus for research into discovery and development of new antibacterial agents. We synthesized a series D-/L-alaninyl substituted triazolyl oxazolidinone derivatives and evaluated their antibacterial activity against selected standard Gram-positive and Gram-negative bacterial strains. Overall, the compounds showed moderate to strong antibacterial activity. Compounds 9d and 10d (D- and L-alaninyl derivatives bearing 3,5-dinitrobenzoyl substituent), 10e (D-alaninyl derivative bearing 5-nitrofurancarbonyl group) and 9f and 10f (D- and L-alaninyl derivatives bearing 5-nitrothiophene carbonyl moiety) demonstrated antibacterial activity (MIC:2 g/mL) against S. aureus, S. epidermidis, E. faecalis and M. catarrhalis standard bacterial strains. No significant differences were noticeable between the antibacterial activity of the D- and L-alaninyl derivatives as a result of the stereochemistry of the compounds.

Keywords

Antibacterial, Linezolid, SARs, Alaninyl-oxazolidinone, Triazolyl-oxazolidinone

Subject

Biology and Life Sciences, Biochemistry and Molecular Biology

Comments (0)

We encourage comments and feedback from a broad range of readers. See criteria for comments and our Diversity statement.

Leave a public comment
Send a private comment to the author(s)
* All users must log in before leaving a comment
Views 0
Downloads 0
Comments 0
Metrics 0


×
Alerts
Notify me about updates to this article or when a peer-reviewed version is published.
We use cookies on our website to ensure you get the best experience.
Read more about our cookies here.