2016
DOI: 10.3390/molecules21020241
|View full text |Cite
|
Sign up to set email alerts
|

Discovery of a New Class of Sortase A Transpeptidase Inhibitors to Tackle Gram-Positive Pathogens: 2-(2-Phenylhydrazinylidene)alkanoic Acids and Related Derivatives

Abstract: A FRET-based random screening assay was used to generate hit compounds as sortase A inhibitors that allowed us to identify ethyl 3-oxo-2-(2-phenylhydrazinylidene)butanoate as an example of a new class of sortase A inhibitors. Other analogues were generated by changing the ethoxycarbonyl function for a carboxy, cyano or amide group, or introducing substituents in the phenyl ring of the ester and acid derivatives. The most active derivative found was 3-oxo-2-(2-(3,4dichlorophenyl)hydrazinylidene)butanoic acid (2… Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
3
1
1

Citation Types

0
21
0

Year Published

2016
2016
2024
2024

Publication Types

Select...
9

Relationship

0
9

Authors

Journals

citations
Cited by 33 publications
(21 citation statements)
references
References 37 publications
(49 reference statements)
0
21
0
Order By: Relevance
“…The effort to discover a Sortase A inhibitor has identified various structural scaffolds as potentially clinical useful solutions. These include: 2-phenylbenzofuran-3-carboxamide [ 18 ], 2-phenylbenzo[ d ]oxazole-7-carboxamide [ 19 ], 2-(2-phenylhydrazinylidene)alkanoic acids [ 20 ], benzisothiazolinone [ 21 ], indolethiazolidine [ 22 ], rhodanines [ 23 ], diarylacrylonitriles, triazolo-thiadiazole [ 24 ], and other structures as presented in the reviews of these fields [ 16 , 25 , 26 ].…”
Section: Introductionmentioning
confidence: 99%
“…The effort to discover a Sortase A inhibitor has identified various structural scaffolds as potentially clinical useful solutions. These include: 2-phenylbenzofuran-3-carboxamide [ 18 ], 2-phenylbenzo[ d ]oxazole-7-carboxamide [ 19 ], 2-(2-phenylhydrazinylidene)alkanoic acids [ 20 ], benzisothiazolinone [ 21 ], indolethiazolidine [ 22 ], rhodanines [ 23 ], diarylacrylonitriles, triazolo-thiadiazole [ 24 ], and other structures as presented in the reviews of these fields [ 16 , 25 , 26 ].…”
Section: Introductionmentioning
confidence: 99%
“…Several significant small organic molecules have been designed and synthesized, as shown in Figure 2 , with promising IC 50 values. Herein, the concrete synthetic features and the analytic properties for structural identification are described in the order of diarylacrylonitriles [ 38 ], pyridazinones [ 39 ], aryl 3-acryloamides [ 40 ], dihydro-β-carboline [ 41 ], benzisothiazolinones [ 42 ], triazolothiadiazoles [ 43 ], 2-(2-phenylhydrazinylidene)alkanoates [ 44 ], 2-phenyl-benzo[ d ]oxazole-7-carboxamide [ 45 ], 2-phenyl-benzofuran-7-carboxamide [ 46 ], 2-phenylthiazoles [ 47 ], 2, 5-disubstitued thiadiazole [ 48 ], and thiadiazolidinedione [ 49 ].…”
Section: Resultsmentioning
confidence: 99%
“…As expected, MC-RL was as active as MC-L against S. aureus, since RSV did not synergistically contribute to the antimicrobial activity. Notwithstanding, the loading of RSV into the MC-RL might be useful, since better antibacterial properties were reported for RSV in respect to benzoyl peroxide, which is conventionally used to treat acne [6], and the procedures of loading could be optimized to increase RSV amount. Since LIM and RSV are known for inhibiting bacterial growth [6][7][8][9][10][11][12][13], the MC-E, MC-RL, MC-R, and MC-L were analyzed for their antibacterial activity against S. aureus by microbiological assays (Figure 8).…”
Section: Antibacterial Activity Against Staphylococcus Aureus Atcc 25923mentioning
confidence: 99%
“…Even though they are widely used, the prolonged use of chemotherapeutics is the main cause of the spread of antibacterial resistance phenomena in microorganisms, leading to infectious-disease-treatment failure worldwide [4,5]. As a consequence, an additional strategy to contrast antibiotic resistance is the research of new molecules targeting biofilm formation [6,7]. During the last few years, the attention toward the Resveratrol (RSV) has been increasing considerably, due to its proven beneficial properties on human health [8].…”
Section: Introductionmentioning
confidence: 99%