Structure-Antibacterial Activity Relationships of N-Substituted-(d-/l-Alaninyl) 1H-1,2,3-Triazolylmethyl Oxazolidinones

Phillips, Oludotun Adebayo; Udo, Edet Ekpenyong; D’silva, Roselyn Jennifer

doi:10.3390/scipharm86040042

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Structure-Antibacterial Activity Relationships of N-Substituted-(d-/l-Alaninyl) 1H-1,2,3-Triazolylmethyl Oxazolidinones

Oludotun Adebayo Phillips

^1,*

Edet Ekpenyong Udo

² and

Roselyn Jennifer D’silva

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Kuwait University, P.O. Box 24923, Safat 13110, Kuwait

Department of Microbiology, Faculty of Medicine, Kuwait University, P.O. Box 24923, Safat 13110, Kuwait

Author to whom correspondence should be addressed.

Sci. Pharm. 2018, 86(4), 42; https://doi.org/10.3390/scipharm86040042

Received: 30 August 2018 / Revised: 20 September 2018 / Accepted: 21 September 2018 / Published: 26 September 2018

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Abstract

Bacterial resistance towards the existing class of antibacterial drugs continues to increase, posing a significant threat to the clinical usefulness of these drugs. These increasing and alarming rates of antibacterial resistance development and the decline in the number of new antibacterial drugs’ approval continue to serve as a major impetus for research into the discovery and development of new antibacterial agents. We synthesized a series of 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 the 3,5-dinitrobenzoyl substituent), 10e (l-alaninyl derivative bearing the 5-nitrofurancarbonyl group) and 9f and 10f (d- and l-alaninyl derivatives bearing the 5-nitrothiophene carbonyl moiety) demonstrated antibacterial activity (MIC: 2 µg/mL) against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis and Moraxella 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. View Full-Text

Keywords: antibacterial; linezolid; SARs; alaninyl-oxazolidinone; triazolyl-oxazolidinone

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MDPI and ACS Style

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. https://doi.org/10.3390/scipharm86040042

AMA Style

Phillips OA, Udo EE, D’silva RJ. Structure-Antibacterial Activity Relationships of N-Substituted-(d-/l-Alaninyl) 1H-1,2,3-Triazolylmethyl Oxazolidinones. Scientia Pharmaceutica. 2018; 86(4):42. https://doi.org/10.3390/scipharm86040042

Chicago/Turabian Style

Phillips, Oludotun Adebayo, Edet Ekpenyong Udo, and Roselyn Jennifer D’silva. 2018. "Structure-Antibacterial Activity Relationships of N-Substituted-(d-/l-Alaninyl) 1H-1,2,3-Triazolylmethyl Oxazolidinones" Scientia Pharmaceutica 86, no. 4: 42. https://doi.org/10.3390/scipharm86040042

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Structure-Antibacterial Activity Relationships of N-Substituted-(d-/l-Alaninyl) 1H-1,2,3-Triazolylmethyl Oxazolidinones

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