Article (Scientific journals)
Synthesis of linear and cyclic guazatine derivatives endowed with antibacterial activity
Maccari, G.; Sanfilippo, S.; De Luca, F. et al.
2014In Bioorganic and Medicinal Chemistry Letters, 24 (23), p. 5525-5529
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Keywords :
Antibacterial; Drug resistant bacteria; Guanidinic compounds; Macrocycles; Achromobacter xylosoxidans; Acinetobacter baumannii; Aeromonas hydrophila; Alcaligenes faecalis; Article; Bacillus subtilis; Elizabethkingia meningoseptica; Enterobacter cloacae; Enterococcus faecalis; Escherichia coli; Klebsiella pneumoniae; Pseudomonas aeruginosa; Staphylococcus aureus; Staphylococcus epidermidis; Staphylococcus haemolyticus; Staphylococcus hominis; Staphylococcus warneri; Stenotrophomonas maltophilia; Streptococcus pyogenes; Anti-Bacterial Agents; Drug Resistance, Microbial; Guanidines; Humans; Microbial Sensitivity Tests
Abstract :
[en] Antibiotic resistance has reached alarming levels in many clinically-relevant human pathogens, and there is an increasing clinical need for new antibiotics active on drug-resistant Gram-negative pathogens who rapidly evolve towards pandrug resistance phenotypes. Here, we report on two related classes of guanidinic compounds endowed with antibacterial activity. The two best compounds (9a and 13d) exhibited the most potent antibacterial activity with MIC values ranging 0.12-8 μg/ml with most tested pathogens, including both Gram-positive and Gram-negative bacteria. Interestingly, MIC values were not affected (1-8 μg/ml) when measured using recent clinical isolates with various antibiotic resistance determinants. The results reported herein identify guazatine derivatives as an interesting starting point for the optimization of a potentially novel class of antibacterial agents. © 2014 Elsevier Ltd. All rights reserved.
Disciplines :
Chemistry
Microbiology
Author, co-author :
Maccari, G.;  Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Siena, I-53100, Italy
Sanfilippo, S.;  Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Siena, I-53100, Italy
De Luca, F.;  Department of Medical Biotechnology, University of Siena, Siena, I-53100, Italy
Deodato, D.;  Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Siena, I-53100, Italy
Casian, A.;  Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Siena, I-53100, Italy
Dasso Lang, M. C.;  Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Siena, I-53100, Italy
Zamperini, C.;  Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Siena, I-53100, Italy
Dreassi, E.;  Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Siena, I-53100, Italy
Rossolini, G. M.;  Department of Medical Biotechnology, University of Siena, Siena, I-53100, Italy
Docquier, Jean-Denis ;  Université de Liège - ULiège > Département des sciences de la vie > Centre d'ingénierie des protéines
Botta, M.;  Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Siena, I-53100, Italy, Sbarro Institute for Cancer Research and Molecular Medicine, College of Science and Technology, Temple University, 1900 N 12th Street, Philadelphia, PA 19122, United States, Lead Discovery Siena S.r.l, Via Vittorio Alfieri 31, Castelnuovo Berardenga, I-53019, Italy
Language :
English
Title :
Synthesis of linear and cyclic guazatine derivatives endowed with antibacterial activity
Publication date :
2014
Journal title :
Bioorganic and Medicinal Chemistry Letters
ISSN :
0960-894X
eISSN :
1464-3405
Publisher :
Elsevier Ltd
Volume :
24
Issue :
23
Pages :
5525-5529
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 19 November 2020

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