New Arene and/or Heteroarene‐Linked 1,3,4‐Oxadiazoles: Synthesis of Potential Methicillin‐Resistant Staphylococcus aureus and Vancomycin‐Resistant Enterococcus Inhibitors

ChemistrySelect, Journal Year: 2024, Volume and Issue: 9(36)

Published: Sept. 19, 2024

Abstract Bacterial infections, particularly those associated with methicillin‐resistant Staphylococcus aureus (MRSA) and vancomycin‐resistant Enterococcus (VRE), threaten public health economies, rising antibiotic resistance resulting in more deaths yearly. In this study, we investigated the bacterial inhibitory activity of some new 1,3,4‐oxadiazoles prepared, good yields, using a two‐step tandem protocol. Therefore, appropriate N ‐benzoylhydrazones were prepared first, then, without isolation, underwent oxidative‐cyclization presence chloramine trihydrate. More 4‐acyloxyphenyl‐linked by pyridine‐mediated acylation 2‐(4‐hydroxyphenyl)‐1,3,4‐oxadiazoles acyl chlorides. Some products demonstrated activity, against S. faecalis strains. The 4‐(5‐(furan‐2‐yl)‐1,3,4‐oxadiazol‐2‐yl)phenyl acetate showed comparable antibacterial to ciprofloxacin, MIC/MBC values up 3.6/7.2 µM previous Moreover, it different MRSA VRE strains when compared linezolid. It had 7.2/14.4 14.4/57.8 strains, respectively.

Language: Английский

2-Aminothiophene Derivatives—New Drug Candidates Against Leishmaniasis: Drug Design, Synthesis, Pharmacomodulation, and Antileishmanial Activity

Pharmaceuticals, Journal Year: 2025, Volume and Issue: 18(1), P. 125 - 125

Published: Jan. 17, 2025

Background/Objectives: Leishmaniasis is one of the 20 Neglected Tropical Diseases according to WHO, affecting approximately 12 million people in four continents, generating serious public health problems. The lack therapeutic options, associated with toxicity and emergence resistance few available drugs, makes it urgent develop new drug options. In this context, aims work are expand knowledge about pharmacophore group responsible for antileishmanial potential 2-aminothiophene derivatives. Thus, compounds were synthesized containing chemical modifications at C-3, C-4, C-5 positions ring, addition S-Se bioisosterism. Methods: Dozens 2-AT 2-aminoselenophen (2-AS) derivatives sequentially through applications Gewald reaction then evaluated vitro their activities against L. amazonensis cytotoxicity macrophages. Results: Several series synthesized, was possible identify some substitution patterns favorable activity IC50 values below 10 µM, such as non-essentiality presence a carbonitrile C-3; importance size cycloalkyl/piperidinyl chains C-4 modulating activity; increase without safety S/Se bioisosteric substitution. Conclusions: Taken together, these findings reaffirm great 2-aminothiophenes generate candidates offers contributions design an even more promising profile problem leishmaniasis.

Language: Английский

Synthesis and Cytostatic Activity of Substituted Derivatives of Sodium 1-Amino-2-cyano-1,6-dioxo-4-{[3-(ethoxycarbonyl)thiophen-2-yl]amino}hexa-2,4-dien-3-olates

Russian Journal of General Chemistry, Journal Year: 2024, Volume and Issue: 94(12), P. 3140 - 3148

Published: Dec. 1, 2024

Language: Английский