Novel amide derivatives of pyrimidine piperidine; Design, synthesis and In-vitro anti-tubercular activity

Tuberculosis (TB) caused by M. tuberculosis, continues?to be a global threat, with the growing emergence of multidrug-resistant strains. A novel class of amide derivatives of?pyrimidine piperidine were designed. Molecular docking studies was performed through Schrodinger software against protein receptor (PDB ID-7F72) using Ethionamide as reference drug. Docking study represented that the SB-7, SB-14 and SB-15 had the maximum binding affinities i.e., -6.292, -6.443 and -7.556 respectively, to the protein receptor and considered as promising candidates for further synthesis. The synthesized compounds were characterized by Infra-red, NMR and Mass spectrometry and them in-vitro antimycobacterial activity was tested by Microplate Alamar Blue Assay (MABA) method. The minimum inhibitory concentration was?found significant for some derivatives, SB-7: 6.25 µg/ml and SB-14: 3.12 µg/ml, while it was more significant with SB-15 (1.6 µg/ml) against M. tuberculosis H37Rv strain, indicating their potential as promising antimycobacterial agent.

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Publication Details

Journal
The Pharma Innovation
Published
2025-01-01
DOI
https://doi.org/10.22271/tpi.2025.v14.i2a.26164
Primary Topic
Synthesis and biological activity
Type
article
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article

Novel amide derivatives of pyrimidine piperidine; Design, synthesis and In-vitro anti-tubercular activity

Tanuj Hooda, Shailja, Bhagwati Devi, Pawan Jalwal et al.
The Pharma Innovation
Synthesis and biological activity
article

Novel amide derivatives of pyrimidine piperidine; Design, synthesis and In-vitro anti-tubercular activity

Tanuj Hooda, Shailja, Bhagwati Devi, Pawan Jalwal, Aarti Bhoria
article en

Abstract

Tuberculosis (TB) caused by M. tuberculosis, continues?to be a global threat, with the growing emergence of multidrug-resistant strains. A novel class of amide derivatives of?pyrimidine piperidine were designed. Molecular docking studies was performed through Schrodinger software against protein receptor (PDB ID-7F72) using Ethionamide as reference drug. Docking study represented that the SB-7, SB-14 and SB-15 had the maximum binding affinities i.e., -6.292, -6.443 and -7.556 respectively, to the protein receptor and considered as promising candidates for further synthesis. The synthesized compounds were characterized by Infra-red, NMR and Mass spectrometry and them in-vitro antimycobacterial activity was tested by Microplate Alamar Blue Assay (MABA) method. The minimum inhibitory concentration was?found significant for some derivatives, SB-7: 6.25 µg/ml and SB-14: 3.12 µg/ml, while it was more significant with SB-15 (1.6 µg/ml) against M. tuberculosis H37Rv strain, indicating their potential as promising antimycobacterial agent.

The Pharma InnovationVol. 14(2)
Openalex Percentile: Top 89%
Synthesis and biological activity
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Novel amide derivatives of pyrimidine piperidine; Design, synthesis and In-vitro anti-tubercular activity — Tanuj Hooda, Shailja, et al. · The Pharma Innovation (2025) | TGRS Research Map | TGRS