In 2022,Han, Sang Hoon; Goins, Christopher M.; Arya, Tarun; Shin, Woo-Jin; Maw, Joshua; Hooper, Alice; Sonawane, Dhiraj P.; Porter, Matthew R.; Bannister, Breyanne E.; Crouch, Rachel D.; Lindsey, A. Abigail; Lakatos, Gabriella; Martinez, Steven R.; Alvarado, Joseph; Akers, Wendell S.; Wang, Nancy S.; Jung, Jae U.; Macdonald, Jonathan D.; Stauffer, Shaun R. published an article in Journal of Medicinal Chemistry. The title of the article was 《Structure-based optimization of ML300-derived, noncovalent inhibitors targeting the severe acute respiratory syndrome coronavirus 3CL protease (SARS-CoV-2 3CLpro)》.Reference of 2-Pyridinylboronic acid The author mentioned the following in the article:
Starting from the MLPCN probe compound ML300, a structure-based optimization campaign was initiated against the recent severe acute respiratory syndrome coronavirus (SARS-CoV-2) main protease (3CLpro). X-ray structures of SARS-CoV-1 and SARS-CoV-2 3CLpro enzymes in complex with multiple ML300-based inhibitors, including the original probe ML300, were obtained and proved instrumental in guiding chem. toward probe compound 41 (I)(CCF0058981). The disclosed inhibitors utilize a noncovalent mode of action and complex in a noncanonical binding mode not observed by peptidic 3CLpro inhibitors. In vitro DMPK profiling highlights key areas where further optimization in the series is required to obtain useful in vivo probes. Antiviral activity was established using a SARS-CoV-2-infected Vero E6 cell viability assay and a plaque formation assay. I demonstrates nanomolar activity in these resp. assays, comparable in potency to remdesivir. These findings have implications for antiviral development to combat current and future SARS-like zoonotic coronavirus outbreaks. In addition to this study using 2-Pyridinylboronic acid, there are many other studies that have used 2-Pyridinylboronic acid(cas: 197958-29-5Reference of 2-Pyridinylboronic acid) was used in this study.
2-Pyridinylboronic acid(cas: 197958-29-5) belongs to pyridine. When pyridine is adsorbed on oxide surfaces or in porous materials, the following species are commonly observed: (i) pyridine coordinated to Lewis acid sites, (ii) pyridine H-bonded to weakly acidic hydroxyls, and (iii) protonated pyridine. At high coverage, physisorbed pyridine and protonated dimers can also be observed.Reference of 2-Pyridinylboronic acid