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- Title
Design, Synthesis, and in vitro antitubercular activity of 1,2,3‐triazolyl‐dihydroquinoline derivatives.
- Authors
Banu, Saleha; Bollu, Rajitha; Nagarapu, Lingaiah; Nanubolu, Jagadeesh Babu; Yogeswari, Perumal; Sriram, Dharmarajan; Gunda, Shravan Kumar; Vardhan, Divyasphoorthi
- Abstract
In the quest for new active molecules against Mycobacterium tuberculosis, a series of dihydroquinoline derivatives possessing triazolo substituents were efficiently synthesized using click chemistry. The structure of 6l was evidenced by X‐ray crystallographic study. The newly synthesized compounds were evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv (ATCC27294). The compounds 6a, 6g, and 6j (MIC: 3.13 μg/ml) showed promising activity when compared to the first‐line drug such as ethambutol. In addition, the structure and antitubercular activity relationship were further supported by in silico molecular docking studies of the active compounds against 3IVX.PDB (crystal structure of pantothenate synthetase in complex with 2‐(2‐(benzofuran‐2‐ylsulfonylcarbamoyl)‐5‐methoxy‐1H‐indol‐1‐yl)acetic acid).
- Subjects
MYCOBACTERIUM tuberculosis; DOPAMINE receptors; STRUCTURE-activity relationship in pharmacology; ANTITUBERCULAR agents; CLICK chemistry; X-ray crystallography; ETHAMBUTOL; THERAPEUTICS
- Publication
Chemical Biology & Drug Design, 2018, Vol 92, Issue 1, p1315
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.13196