227935-30-0Relevant articles and documents
Structure-activity relationship studies in substituted sulfamoyl benzamidothiazoles that prolong NF-κB activation
Belsuzarri, Masiel,Carson, Dennis A.,Chan, Michael,Chu, Paul J.,Corr, Maripat,Cottam, Howard B.,Hayashi, Tomoko,Lao, Fitzgerald S.,Nan, Jason,Saito, Tetsuya,Sato-Kaneko, Fumi,Shukla, Nikunj M.,Yao, Shiyin
, (2021/07/19)
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. Additionally, our SAR studies led to identification of a photoaffinity probe which will aid the target identification and mechanism of action studies in the future.
VACCINE ADJUVANT
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Page/Page column 78, (2020/06/10)
Compounds useful as an adjuvant, e.g., formulas (I)-(VI) and uses thereof, for example, with immunogenic moieties or other adjuvants, are provided.
AMIDO-BENZYL SULFONE AND SULFOXIDE DERIVATIVES
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Page/Page column 146, (2013/09/12)
The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5- carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT)
Zheng, Xiaozhang,Bair, Kenneth W.,Bauer, Paul,Baumeister, Timm,Bowman, Krista K.,Buckmelter, Alexandre J.,Caligiuri, Maureen,Clodfelter, Karl H.,Feng, Yezhen,Han, Bingsong,Ho, Yen-Ching,Kley, Nikolai,Li, Hong,Liang, Xiaorong,Liederer, Bianca M.,Lin, Jian,Ly, Justin,O'Brien, Thomas,Oeh, Jason,Oh, Angela,Reynolds, Dominic J.,Sampath, Deepak,Sharma, Geeta,Skelton, Nicholas,Smith, Chase C.,Tremayne, Jarrod,Wang, Leslie,Wang, Weiru,Wang, Zhongguo,Wu, Hongxing,Wu, Jiansheng,Xiao, Yang,Yang, Guangxing,Yuen, Po-Wai,Zak, Mark,Dragovich, Peter S.
supporting information, p. 5488 - 5497 (2013/10/01)
Potent, 1H-pyrazolo[3,4-b]pyridine-containing inhibitors of the human nicotinamide phosphoribosyltransferase (NAMPT) enzyme were identified using structure-based design techniques. Many of these compounds exhibited nanomolar antiproliferation activities a
Preparation of arylsulfonyl chlorides by chlorosulfonylation of in situ generated diazonium salts using a continuous flow reactor
Malet-Sanz, Laia,Madrzak, Julia,Ley, Steven V.,Baxendale, Ian R.
experimental part, p. 5324 - 5332 (2011/01/12)
A new flow procedure for the preparation of arylsulfonyl chlorides from aniline starting materials is described. The reaction conditions are mild, requiring no added acid and are amenable to continuous flow processing, in a safe, easily scalable and less labour intensive way than the corresponding batch method.
Method for Preparing Halogenated Amines
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Page/Page column 12, (2008/12/07)
This invention relates to methods for preparing halogenated amines.
Triazine angiogenesis inhibitors
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, (2008/06/13)
Compounds having Formula I STR1 or pharmaceutically acceptable salts or prodrugs thereof, are useful for treating pathological states which arise from or are exacerbated by angiogenesis. The invention also relates to pharmaceutical compositions comprising these compounds and to methods of inhibiting anglogenesis in a mammal.
