On October 5, 2021, Sui, Yan-Fei; Ansari, Mohammad Fawad; Fang, Bo; Zhang, Shao-Lin; Zhou, Cheng-He published an article.Formula: C5H5NOS The title of the article was Discovery of novel purinylthiazolylethanone derivatives as anti-Candida albicans agents through possible multifaceted mechanisms. And the article contained the following:
Novel purinylthiazolylethanone derivatives, I [R = H, Et, allyl, 2-chlorophenylmethyl, etc], II [R1 = hydroxyl, hydroxyimino, methoxyimino]which were expected to combat the fungal drug resistance was developed. Some prepared purinylthiazolylethanone derivatives I and II possessed satisfactory inhibitory action towards the tested fungi, among which compound I [R = 2-ethoxyoxoethyl] gave a MIC value of 1μg/mL against C. albicans. The active mol. I [R = 2-ethoxyoxoethyl] was able to kill C. albicans with undetectable resistance as well as low hematotoxicity and cytotoxicity. Furthermore, it could hinder the growth of C. albicans biofilm, thus avoiding the occurrence of drug resistance. Mechanism research manifested that purinylthiazolylethanone derivative I [R = 2-ethoxyoxoethyl] led to damage of cell wall and membrane disruption, so protein leakage and the cytoplasmic membrane depolarization were observed On this account, the activity of fungal lactate dehydrogenase was reduced and metabolism was impeded. Meanwhile, the increased levels of reactive oxygen species (ROS) and reactive nitrogen species (RNS) disordered redox equilibrium, giving rise to oxidative damage to fungal cells and fungicidal effect. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Formula: C5H5NOS
The Article related to purinylthiazolylethanone preparation antifungal sar drug resistance, antifungal, drug resistance, purine, thiazole, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Formula: C5H5NOS
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica