Nguyen, William; Jacobson, Jonathan; Jarman, Kate E.; Jousset Sabroux, Helene; Harty, Leigh; McMahon, James; Lewin, Sharon R.; Purcell, Damian F.; Sleebs, Brad E. published the artcile< Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models>, COA of Formula: C6H10N2S, the main research area is acylaminothiazole TAT transcription HIV1 latency antiretroviral agent HIV infection.
The persistent reservoir of cells latently infected with human immunodeficiency virus (HIV)-integrated proviral DNA necessitates lifelong suppressive antiretroviral therapy (ART). Epigenetic targeted compounds have shown promise as potential latency-reversing agents; however, these drugs have undesirable toxicity and lack specificity for HIV. We utilized a novel HEK293-derived FlpIn dual-reporter cell line, which quantifies specific HIV provirus reactivation (LTR promoter) relative to nonspecific host cell gene expression (CMV promoter), to identify the 5-substituted 2-acylaminothiazole hit class. Here, we describe the optimization of the hit class, defining the functionality necessary for HIV gene activation and for improving in vitro metabolism and solubility The optimized compounds displayed enhanced HIV gene expression in HEK293 and Jurkat 10.6 latency cellular models and increased unspliced HIV RNA in resting CD4+ T cells isolated from HIV-infected individuals on ART, demonstrating the potential of the 2-acylaminothiazole class as latency-reversing agents.
Journal of Medicinal Chemistry published new progress about Anti-HIV agents. 101080-15-3 belongs to class thiazole, and the molecular formula is C6H10N2S, COA of Formula: C6H10N2S.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica