Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates

Siva S. Panda

doi:10.1016/j.bmcl.2014.01.065

Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates

Siva S. Panda

Chemistry and Biochemistry

Research output: Contribution to journal › Article › peer-review

44 Scopus citations

Abstract

Amino acid conjugates of quinolone, metronidazole and sulfadiazine antibiotics were synthesized in good yields using benzotriazole methodology. All the conjugates were screened for their antibacterial activity using methods adapted from the Clinical and Laboratory Standards Institute. Antibiotic conjugates were tested for activity in four medically relevant organisms; Staphylococcus aureus (RN4220), Escherichia coli (DH5α), Pseudomonas aeruginosa (PAO1), and Bacillus subtilis (168). Several antibiotic conjugates show promising results against several of the strains screened.

Original language	English (US)
Pages (from-to)	1856-1861
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	24
Issue number	7
DOIs	https://doi.org/10.1016/j.bmcl.2014.01.065
State	Published - Apr 1 2014

Keywords

Antibacterial
Antibiotics
Benzotriazole
Conjugates
Lipophilicity

ASJC Scopus subject areas

Biochemistry
Clinical Biochemistry
Molecular Biology
Molecular Medicine
Organic Chemistry
Drug Discovery
Pharmaceutical Science
General Medicine

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10.1016/j.bmcl.2014.01.065

Cite this

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title = "Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates",

abstract = "Amino acid conjugates of quinolone, metronidazole and sulfadiazine antibiotics were synthesized in good yields using benzotriazole methodology. All the conjugates were screened for their antibacterial activity using methods adapted from the Clinical and Laboratory Standards Institute. Antibiotic conjugates were tested for activity in four medically relevant organisms; Staphylococcus aureus (RN4220), Escherichia coli (DH5α), Pseudomonas aeruginosa (PAO1), and Bacillus subtilis (168). Several antibiotic conjugates show promising results against several of the strains screened.",

keywords = "Antibacterial, Antibiotics, Benzotriazole, Conjugates, Lipophilicity",

author = "Panda, {Siva S.}",

note = "Funding Information: We thank the University of Florida and the Kenan Foundation for financial support. This paper was also funded in part by generous support from King Abdulaziz University, under grant No. (D-006/431). The authors, therefore, acknowledge the technical and financial support of KAU. We also thank to Dr. C.D. Hall for helpful suggestions. ",

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T1 - Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates

AU - Panda, Siva S.

N1 - Funding Information: We thank the University of Florida and the Kenan Foundation for financial support. This paper was also funded in part by generous support from King Abdulaziz University, under grant No. (D-006/431). The authors, therefore, acknowledge the technical and financial support of KAU. We also thank to Dr. C.D. Hall for helpful suggestions.

PY - 2014/4/1

Y1 - 2014/4/1

N2 - Amino acid conjugates of quinolone, metronidazole and sulfadiazine antibiotics were synthesized in good yields using benzotriazole methodology. All the conjugates were screened for their antibacterial activity using methods adapted from the Clinical and Laboratory Standards Institute. Antibiotic conjugates were tested for activity in four medically relevant organisms; Staphylococcus aureus (RN4220), Escherichia coli (DH5α), Pseudomonas aeruginosa (PAO1), and Bacillus subtilis (168). Several antibiotic conjugates show promising results against several of the strains screened.

AB - Amino acid conjugates of quinolone, metronidazole and sulfadiazine antibiotics were synthesized in good yields using benzotriazole methodology. All the conjugates were screened for their antibacterial activity using methods adapted from the Clinical and Laboratory Standards Institute. Antibiotic conjugates were tested for activity in four medically relevant organisms; Staphylococcus aureus (RN4220), Escherichia coli (DH5α), Pseudomonas aeruginosa (PAO1), and Bacillus subtilis (168). Several antibiotic conjugates show promising results against several of the strains screened.

KW - Antibacterial

KW - Antibiotics

KW - Benzotriazole

KW - Conjugates

KW - Lipophilicity

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JO - Bioorganic and Medicinal Chemistry Letters

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ER -

Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates

Abstract

Keywords

ASJC Scopus subject areas

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