1395493-30-7Relevant articles and documents
Novel SAR for quinazoline inhibitors of EHMT1 and EHMT2
Leenders, Ruben,Zijlmans, Remco,van Bree, Bart,van de Sande, Marc,Trivarelli, Federica,Damen, Eddy,Wegert, Anita,Müller, Daniel,Ehlert, Jan Erik,Feger, Daniel,Heidemann-Dinger, Carolin,Kubbutat, Michael,Sch?chtele, Christoph,Lenstra, Danny C.,Mecinovi?, Jasmin,Müller, Gerhard
, p. 2516 - 2524 (2019)
Detailed structure activity relationship of two series of quinazoline EHMT1/EHMT2 inhibitors (UNC0224 and UNC0638) have been elaborated. New and active alternatives are presented for the ubiquitous substitution patterns found in literature for the linker to the lysine mimicking region and the lysine mimic itself. These findings could allow for advancing EHMT1/EHMT2 inhibitors of that type beyond tool compounds by fine-tuning physicochemical properties making these inhibitors more drug-like.
Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria
Skepper, Colin K.,Armstrong, Duncan,Balibar, Carl J.,Bauer, Daniel,Bellamacina, Cornelia,Benton, Bret M.,Bussiere, Dirksen,De Pascale, Gianfranco,De Vicente, Javier,Dean, Charles R.,Dhumale, Bhavesh,Fisher, L. Mark,Fuller, John,Fulsunder, Mangesh,Holder, Lauren M.,Hu, Cheng,Kantariya, Bhavin,Lapointe, Guillaume,Leeds, Jennifer A.,Li, Xiaolin,Lu, Peichao,Lvov, Anatoli,Ma, Sylvia,Madhavan, Shravanthi,Malekar, Swapnil,McKenney, David,Mergo, Wosenu,Metzger, Louis,Moser, Heinz E.,Mutnick, Daniel,Noeske, Jonas,Osborne, Colin,Patel, Ashish,Patel, Darshit,Patel, Tushar,Prajapati, Krunal,Prosen, Katherine R.,Reck, Folkert,Richie, Daryl L.,Rico, Alice,Sanderson, Mark R.,Satasia, Shailesh,Sawyer, William S.,Selvarajah, Jogitha,Shah, Nirav,Shanghavi, Kartik,Shu, Wei,Thompson, Katherine V.,Traebert, Martin,Vala, Anand,Vala, Lakhan,Veselkov, Dennis A.,Vo, Jason,Wang, Michael,Widya, Marcella,Williams, Sarah L.,Xu, Yongjin,Yue, Qin,Zang, Richard,Zhou, Bo,Rivkin, Alexey
, p. 7773 - 7816 (2020/07/21)
Since their discovery over 5 decades ago, quinolone antibiotics have found enormous success as broad spectrum agents that exert their activity through dual inhibition of bacterial DNA gyrase and topoisomerase IV. Increasing rates of resistance, driven lar
CARBOXYLIC DIARYTHIAZEPINEAMINES AS MIXED MU-AND DELTA-OPIOID RECEPTOR AGONISTS
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Page/Page column 84; 86-87, (2018/10/19)
The present invention provides a compound having the structure:, or a pharmaceutically acceptable salt or ester thereof, and a method of treating a subject afflicted with a pain, a depressive disorder, a mood disorder, an anxiety disorder, borderline personality disorder, opioid addiction, or opioid withdrawal symptoms by administering the compound to the subject.