| Title: |
A New Class of Linezolid‐Based Molecules as Potential Antimicrobial and Antitubercular Agents: A Rational Approach |
| Authors: |
Kushwaha, Babita; Kushwaha, Narva Deshwar; Parish, Tanya; Guzman, Junitta; Kajee, Afsana; Shaikh, Mahamadhanif S.; Kehinde, Idowu; Obakachi, Vincent A.; Pathan, Tabasum Khan; Shinde, Suraj Raosaheb; Karpoormath, Rajshekhar |
| Source: |
ChemistrySelect ; volume 6, issue 13, page 3065-3074 ; ISSN 2365-6549 2365-6549 |
| Publisher Information: |
Wiley |
| Publication Year: |
2021 |
| Collection: |
Wiley Online Library (Open Access Articles via Crossref) |
| Description: |
A total of 19 linezolid‐based novel molecules ( 6 a – d , 8 a – d and 10 a – k ) were synthesized by utilizing a simple and convenient synthetic method. Structures of all the novel derivatives were established by 1 H, 13 C NMR, FT‐IR and mass spectroscopic methods. In addition, structural elucidation of some representative compounds by 19 F, 2D NMR and single crystal X‐ray experiment's ( 6 d and 8 b ) further confirmed the structures of the desired compounds. All the final compounds were evaluated for their in vitro antitubercular ( Mycobacterium tuberculosis H 37 RV strain), antibacterial ( S. aureus , B. subtilis , E. coli and P. aeruginosa ) and antifungal ( C. neoformans , C. albicans and A. niger ) activities. The docking study of most active compounds were also performed towards 50S ribosomal unit of Haloarcula marismortui . The Lipinski's rule of five and significant ADME pharmacokinetic parameters were also analysed indicating potential to develop good oral antimicrobial and antitubercular drug candidates. |
| Document Type: |
article in journal/newspaper |
| Language: |
English |
| DOI: |
10.1002/slct.202100493 |
| Availability: |
https://doi.org/10.1002/slct.202100493; https://onlinelibrary.wiley.com/doi/pdf/10.1002/slct.202100493; https://onlinelibrary.wiley.com/doi/full-xml/10.1002/slct.202100493 |
| Rights: |
http://onlinelibrary.wiley.com/termsAndConditions#vor |
| Accession Number: |
edsbas.CF28C94A |
| Database: |
BASE |