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- Title
Synthesis of diindolylmethane (DIM) bearing thiadiazole derivatives as a potent urease inhibitor.
- Authors
Taha, Muhammad; Rahim, Fazal; Khan, Aftab Ahmad; Anouar, El Hassane; Ahmed, Naveed; Shah, Syed Adnan Ali; Ibrahim, Mohamed; Zakari, Zainul Amiruddin
- Abstract
The current study describes synthesis of diindolylmethane (DIM) derivatives based-thiadiazole as a new class of urease inhibitors. Diindolylmethane is natural product alkaloid reported to use in medicinal chemistry extensively. Diindolylmethane-based-thiadiazole analogs (1–18) were synthesized and characterized by various spectroscopic techniques 1HNMR, 13C-NMR, EI-MS and evaluated for urease (jack bean urease) inhibitory potential. All compounds showed excellent to moderate inhibitory potential having IC50 value within the range of 0.50 ± 0.01 to 33.20 ± 1.20 µM compared with the standard thiourea (21.60 ± 0.70 µM). Compound 8 (IC50 = 0.50 ± 0.01 µM) was the most potent inhibitor amongst all derivatives. Structure-activity relationships have been established for all compounds. The key binding interactions of most active compounds with enzyme were confirmed through molecular docking studies.
- Subjects
DIINDOLYLMETHANE; THIADIAZOLES; ALKALOIDS; MOLECULAR docking; THIOUREA
- Publication
Scientific Reports, 2020, Vol 10, Issue 1, p1
- ISSN
2045-2322
- Publication type
Academic Journal
- DOI
10.1038/s41598-020-64729-3