Synthesis, in Vitro Biological Screening and Molecular Docking Studies of Novel Camphor-based Thiazoles
Overview
Authors
Affiliations
Synthesis, characterization and investigation of antibacterial and antifungal activities of twelve camphor based 2,4-disubstituted 1,3-thiazoles is presented. Their structures were determined using NMR, IR, FAB MS and HRMS analyses. Among the derivatives, 3i and 5 were found to exhibit antifungal and antibacterial activities comparable to that of fluconazole and ciprofloxacin against yeast belonging to Candida spp., MIC 0.12-0.98 μg/ml and Gram-positive bacteria including both pathogenic S. aureus and opportunistic S. epidermidis, MIC 0.98-7.81 μg/ml, B. subtilis and B. cereus, MIC 3.91-31.25 μg/ml, and M. luteus, MIC 0.98 μg/ml species, respectively. Molecular docking studies of all compounds into the active sites of microbial enzymes indicated a possible targets SAP and NMT, thiazoles 3a-j, 4, 5 showed more favourable affinity than the native ligand.
Antibiofilm and Antimicrobial Potentials of Novel Synthesized Sulfur Camphor Derivatives.
Duda-Madej A, Viscardi S, Pacyga K, Kupczynski R, Maczka W, Grabarczyk M Int J Mol Sci. 2024; 25(20).
PMID: 39456678 PMC: 11507198. DOI: 10.3390/ijms252010895.
Is Camphor the Future in Supporting Therapy for Skin Infections?.
Duda-Madej A, Viscardi S, Grabarczyk M, Topola E, Kozlowska J, Maczka W Pharmaceuticals (Basel). 2024; 17(6).
PMID: 38931382 PMC: 11206849. DOI: 10.3390/ph17060715.
Donarska B, Switalska M, Wietrzyk J, Plazinski W, Mizerska-Kowalska M, Zdzisinska B Int J Mol Sci. 2022; 23(14).
PMID: 35886913 PMC: 9321231. DOI: 10.3390/ijms23147566.
Sokolova A, Yarovaya O, Bormotov N, Shishkina L, Salakhutdinov N Medchemcomm. 2018; 9(10):1746-1753.
PMID: 30429979 PMC: 6194496. DOI: 10.1039/c8md00347e.
Laczkowski K, Konklewska N, Biernasiuk A, Malm A, Salat K, Furgala A Med Chem Res. 2018; 27(9):2125-2140.
PMID: 30220831 PMC: 6133161. DOI: 10.1007/s00044-018-2221-x.