Formula: C4H7NO2SIn 2021 ,《Structure-activity relationship studies in substituted sulfamoyl benzamidothiazoles that prolong NF-κB activation》 was published in Bioorganic & Medicinal Chemistry. The article was written by Shukla, Nikunj M.; Chan, Michael; Lao, Fitzgerald S.; Chu, Paul J.; Belsuzarri, Masiel; Yao, Shiyin; Nan, Jason; Sato-Kaneko, Fumi; Saito, Tetsuya; Hayashi, Tomoko; Corr, Maripat; Carson, Dennis A.; Cottam, Howard B.. The article contains the following contents:
In the face of emerging infectious diseases, there remains an unmet need for vaccine development where adjuvants that enhance immune responses to pathogenic antigens are highly desired. Using high-throughput screens with a cell-based nuclear factor κB (NF-κB) reporter assay, we identified a sulfamoyl benzamidothiazole bearing compound 1 that demonstrated a sustained activation of NF-κB after a primary stimulus with a Toll-like receptor (TLR)-4 agonist, lipopolysaccharide (LPS). Here, we explore systematic structure-activity relationship (SAR) studies on compound 1 that indicated the sites on the scaffold that tolerated modification and yielded more potent compounds compared to 1. The selected analogs enhanced release of immunostimulatory cytokines in the human monocytic cell line THP-1 cells and murine primary dendritic cells. In murine vaccination studies, select compounds were used as co-adjuvants in combination with the Food and Drug Administration approved TLR-4 agonistic adjuvant, monophosphoryl lipid A (MPLA) that showed significant enhancement in antigen-specific antibody titers compared to MPLA alone. Addnl., our SAR studies led to identification of a photoaffinity probe which will aid the target identification and mechanism of action studies in the future. In the experiment, the researchers used Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Formula: C4H7NO2S)
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Formula: C4H7NO2S
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