872044-70-7Relevant articles and documents
Design, Synthesis and Evaluation of Oxazaborine Inhibitors of the NLRP3 Inflammasome
Baldwin, Alex G.,Tapia, Victor S.,Swanton, Tessa,White, Claire S.,Beswick, James A.,Brough, David,Freeman, Sally
, p. 312 - 320 (2018/02/09)
The NLRP3 inflammasome is an important regulator of the sterile inflammatory response, and its activation by host-derived sterile molecules leads to the intracellular activation of caspase-1, processing of the pro-inflammatory cytokines interleukin-1β (IL-1β)/IL-18, and pyroptotic cell death. Inappropriate activation of NLRP3 drives a chronic inflammatory response and is implicated in several non-communicable diseases, including gout, atherosclerosis, type II diabetes and Alzheimer's disease. In this study, we report the design, synthesis and biological evaluation of novel boron compounds (NBCs) as NLRP3 inflammasome inhibitors. Structure–activity relationships (SAR) show that 4-fluoro substituents on the phenyl rings retain NLRP3 inhibitory activity, whereas more steric and lipophilic substituents diminish activity. Loss of inhibitory activity is also observed if the CCl3 group on the oxazaborine ring is replaced by a CF3 group. These findings provide additional understanding of the NBC series and will aid in the development of these NLRP3 inhibitors as tool compounds or therapeutic candidates for sterile inflammatory diseases.
Identification of a novel boron-containing antibacterial agent (AN0128) with anti-inflammatory activity, for the potential treatment of cutaneous diseases
Baker, Stephen J.,Akama, Tsutomu,Zhang, Yong-Kang,Sauro, Vittorio,Pandit, Chetan,Singh, Rajeshwar,Kully, Maureen,Khan, Jehangir,Plattner, Jacob J.,Benkovic, Stephen J.,Lee, Ving,Maples, Kirk R.
, p. 5963 - 5967 (2007/10/03)
A series of borinic acid picolinate esters were synthesized and screened for their minimum inhibitory concentration (MIC) against Gram-positive and -negative bacteria. Our lead compounds were then screened for anti-inflammatory activity. From these studie
Topical formulations of borinic acid antibiotics and their methods of use
-
Page/Page column 11, (2008/06/13)
Disclosed are topical formulations, for example, creams, gels, or lotions, of borinic acid antibiotic compounds active against acne vulgaris or secondarily infected skin conditions.