Imidazole–Thiazole Hybrid: Synthesis, Brain Penetration, Cytochrome P450 Enzyme and Gastrointestinal Absorption Study

An Overview of the Structure–Activity Relationship in Novel Antimicrobial Thiazoles Clubbed with Various Heterocycles (2017–2023)

“…Regarding the antifungal activity, the compounds were tested against C. albicans and A. niger strains, using clotrimazole as reference [ 39 ]. Only compound 132 showed superior activity against C. albicans (IZ = 25 mm) compared to clotrimazole (IZ = 22 mm) [ 39 ].…”

“…SAR studies of this series showed that dichloro substitution (R 1 = R 2 = Cl) increased antifungal activity against C. albicans , as seen in compound 132 ( Figure 25 ) [ 39 ]. The substitution of both points of variation with large electron-withdrawing substituents, such as bromo and nitro in 130 , increased antibacterial activity against S. aureus .…”

“…Mono-substitution with an electron-withdrawing substituent (R 1 = Cl in 131 ) decreased the activity against S. aureus but slightly increased antibacterial activity against E. coli , compared to compound 130 ( Figure 25 ). No potential target was reported by the authors [ 39 ].…”

“… SAR studies of antimicrobial 2-(iminobenzylidenel)-5-(imidazole-2-yl)-thiazole derivatives, reported by Dekate et al [ 39 ]. …”

“…Regarding the antifungal activity, the compounds were tested against C. albicans and A. niger strains, using clotrimazole as reference [39]. Only compound 132 showed superior activity against C. albicans (IZ = 25 mm) compared to clotrimazole (IZ = 22 mm) [39]. The antifungal activity of these compounds can be attributed to their capacity to target lanosterol 14α-demethylase, based on molecular docking studies.…”