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Synthesis of diindolylmethane (DIM) bearing thiadiazole derivatives as a potent urease inhibitor.

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.

SUBMITTER: Taha M

PROVIDER: S-EPMC7224224 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature

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Synthesis of diindolylmethane (DIM) bearing thiadiazole derivatives as a potent urease inhibitor.

Taha Muhammad M Rahim Fazal F Khan Aftab Ahmad AA Anouar El Hassane EH Ahmed Naveed N Shah Syed Adnan Ali SAA Ibrahim Mohamed M Zakari Zainul Amiruddin ZA

Scientific reports 20200514 1

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 <sup>1</sup>HNMR, <sup>13</sup>C-NMR, EI-MS and evaluated for urease (jack bean urease) inhibitory potential. All compounds showed excellent to moderat ...[more]

PMID: 32409737

Dataset Information

Synthesis of diindolylmethane (DIM) bearing thiadiazole derivatives as a potent urease inhibitor.

Publications

Synthesis of diindolylmethane (DIM) bearing thiadiazole derivatives as a potent urease inhibitor.

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