Synthesis and antitubercular evaluation of reduced lipophilic imidazo[1,2-a]pyridine-3-carboxamide derivatives
Wang H, Wang A, Gu J, Fu L, Lv K, Ma C, Tao Z, Wang B, et al. (11 authors)
European journal of medicinal chemistry · 2018-12
Abstract
A series of reduced lipophilic N-benzylic imidazo[1,2-a]pyridine carboxamides (IPAs) with various side chains were designed and synthesized as new anti-TB agents in this work. Five derivatives A2, A3, A4, B1 and B9 exhibit excellent in vitro activity (MIC: 0-∞ and C max than Q203 and PBTZ169, suggesting its promising potential to be a lead compound for future antitubercular drug discovery.
MeSH terms
- Mycobacterium tuberculosis
- Imidazoles
- Piperazines
- Pyridines
- Thiazines
- Antitubercular Agents
- Area Under Curve
- Drug Resistance, Multiple
- Structure-Activity Relationship
- Hydrophobic and Hydrophilic Interactions
- Piperazine