Design, Synthesis, and Biological Evaluation of 3,5‐Disubstituted 2‐Pyrazineamide Derivatives as Antitubercular Agents

A novel series of 3,5‐disubstituted‐2‐pyrazineamide derivatives (5a–5o) were synthesized and studied for their potential as antitubercular agents. Among them, the compounds 5a, 5g, and 5m showed the good minimal inhibitory concentration of 20, 25, and 25 μg/mL, respectively. The compound 5a displaye...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Journal of heterocyclic chemistry 2019-03, Vol.56 (3), p.1117-1126
Hauptverfasser: Gangarapu, Nagaraja Reddy, Ranganatham, A., Reddy, Eeda Koti, Surendra, H. D., Sajith, Ayyiliath M., Yellappa, Shivaraj, Chandrasekhar, Kothapalli Bannoth
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:A novel series of 3,5‐disubstituted‐2‐pyrazineamide derivatives (5a–5o) were synthesized and studied for their potential as antitubercular agents. Among them, the compounds 5a, 5g, and 5m showed the good minimal inhibitory concentration of 20, 25, and 25 μg/mL, respectively. The compound 5a displayed excellent minimum inhibitory concentration of 10 μg/mL and is four times more potent compared with the standard drug, rifampicin concentration. In silico docking studies revealed that the compounds 5a and 5c can bind strongly in the active site of 2FUM enzyme and prevent enzyme–substrate interactions. In addition, in silico docking studies were calculated, and based on the data obtained, compound 5a displayed excellent drug‐like properties.
ISSN:0022-152X
1943-5193
DOI:10.1002/jhet.3461