69491-58-3Relevant academic research and scientific papers
SARS-COV-2 INHIBITORS HAVING COVALENT MODIFICATIONS FOR TREATING CORONAVIRUS INFECTIONS
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, (2021/11/06)
Provided herein are compounds, pharmaceutical compositions and methods for treating a SARS-CoV-2 infection.
PURINE DIONES AS WNT PATHWAY MODULATORS
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Paragraph 000109, (2014/12/12)
The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway [Formula should be inserted here] wherein R1, R2, R3, R4 and R5 are each, independently, H or an
Synthesis and methemoglobinemia-inducing properties of benzocaine isosteres designed as humane rodenticides
Conole, Daniel,Beck, Thorsten M.,Jay-Smith, Morgan,Tingle, Malcolm D.,Eason, Charles T.,Brimble, Margaret A.,Rennison, David
, p. 2220 - 2235 (2014/04/17)
A number of isosteres (oxadiazoles, thiadiazoles, tetrazoles and diazines) of benzocaine were prepared and evaluated for their capacity to induce methemoglobinemia - with a view to their possible application as humane pest control agents. It was found that an optimal lipophilicity for the formation of methemoglobin (metHb) in vitro existed within each series, with 1,2,4-oxadiazole 3 (metHb% = 61.0 ± 3.6) and 1,3,4-oxadiazole 10 (metHb% = 52.4 ± 0.9) demonstrating the greatest activity. Of the 5 candidates (compounds 3, 10, 11, 13 and 23) evaluated in vivo, failure to induce a lethal end-point at doses of 120 mg/kg was observed in all cases. Inadequate metabolic stability, particularly towards hepatic enzymes such as the CYPs, was postulated as one reason for their failure.
