Structure-Activity Relationship Studies To Identify Affinity Probes in Bis-aryl Sulfonamides That Prolong Immune Stimuli was written by Chan, Michael;Lao, Fitzgerald S.;Chu, Paul J.;Shpigelman, Jonathan;Yao, Shiyin;Nan, Jason;Sato-Kaneko, Fumi;Li, Vicky;Hayashi, Tomoko;Corr, Maripat;Carson, Dennis A.;Cottam, Howard B.;Shukla, Nikunj M.. And the article was included in Journal of Medicinal Chemistry in 2019.Category: chlorides-buliding-blocks This article mentions the following:
Agents that safely induce, enhance, or sustain multiple innate immune signaling pathways could be developed as potent vaccine adjuvants or coadjuvants. Using high-throughput screens with cell-based nuclear factor 魏B (NF-魏B) and interferon stimulating response element (ISRE) reporter assays, we identified a bis-aryl sulfonamide bearing compound 1 that demonstrated sustained NF-魏B and ISRE activation after a primary stimulus with lipopolysaccharide or interferon-伪, resp. Here, we present systematic structure-activity relationship (SAR) studies on the two Ph rings and amide nitrogen of the sulfonamide group of compound 1 focused toward identification of affinity probes. The murine vaccination studies showed that compounds 1 and 33 when used as coadjuvants with monophosphoryl lipid A (MPLA) showed significant enhancement in antigen ovalbumin-specific Ig responses compared to MPLA alone. SAR studies pointed to the sites on the scaffold that can tolerate the introduction of aryl azide, biotin, and fluorescent rhodamine substituents to obtain several affinity and photoaffinity probes which will be utilized in concert for future target identification and mechanism of action studies. In the experiment, the researchers used many compounds, for example, 4-Butoxybenzene-1-sulfonyl chloride (cas: 1138-56-3Category: chlorides-buliding-blocks).
4-Butoxybenzene-1-sulfonyl chloride (cas: 1138-56-3) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.Category: chlorides-buliding-blocks
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics