56570-66-2Relevant academic research and scientific papers
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria
Lapointe, Guillaume,Skepper, Colin K.,Holder, Lauren M.,Armstrong, Duncan,Bellamacina, Cornelia,Blais, Johanne,Bussiere, Dirksen,Bian, Jianwei,Cepura, Cody,Chan, Helen,Dean, Charles R.,De Pascale, Gianfranco,Dhumale, Bhavesh,Fisher, L. Mark,Fulsunder, Mangesh,Kantariya, Bhavin,Kim, Julie,King, Sean,Kossy, Lauren,Kulkarni, Upendra,Lakshman, Jay,Leeds, Jennifer A.,Ling, Xiaolan,Lvov, Anatoli,Ma, Sylvia,Malekar, Swapnil,McKenney, David,Mergo, Wosenu,Metzger, Louis,Mhaske, Keshav,Moser, Heinz E.,Mostafavi, Mina,Namballa, Sunil,Noeske, Jonas,Osborne, Colin,Patel, Ashish,Patel, Darshit,Patel, Tushar,Piechon, Philippe,Polyakov, Valery,Prajapati, Krunal,Prosen, Katherine R.,Reck, Folkert,Richie, Daryl L.,Sanderson, Mark R.,Satasia, Shailesh,Savani, Bhautik,Selvarajah, Jogitha,Sethuraman, Vijay,Shu, Wei,Tashiro, Kyuto,Thompson, Katherine V.,Vaarla, Krishniah,Vala, Lakhan,Veselkov, Dennis A.,Vo, Jason,Vora, Bhavesh,Wagner, Trixie,Wedel, Laura,Williams, Sarah L.,Yendluri, Satya,Yue, Qin,Yifru, Aregahegn,Zhang, Yong,Rivkin, Alexey
supporting information, p. 6329 - 6357 (2021/06/01)
Herein, we describe the discovery and optimization of a novel series that inhibits bacterial DNA gyrase and topoisomerase IV via binding to, and stabilization of, DNA cleavage complexes. Optimization of this series led to the identification of compound 25
A Method for the Preparation of β-Amino-α,β-unsaturated Carbonyl Compounds: Study of Solvent Effect and Mechanism
R. S., Reyno,Sugunan, Akash,S., Ranganayakulu,Suresh, Cherumuttathu H.,Rajendar, Goreti
supporting information, p. 1040 - 1045 (2020/02/15)
An efficient method for the preparation of β-amino-α,β-unsaturated carbonyl compounds is demonstrated. Bench-stable sodium 3-oxo-enolates were prepared from carbonyl compounds, and reacted with amines in the presence of an acid and a desiccant. DFT studie
Relay Catalysis to Synthesize β-Substituted Enones: Organocatalytic Substitution of Vinylogous Esters and Amides with Organoboronates
Sundstrom, Sasha,Nguyen, Thien S.,May, Jeremy A.
supporting information, p. 1355 - 1359 (2020/02/13)
Organocatalysis was shown to facilitate conjugate additions to vinylogous esters and amides for the first time. Subsequent elimination of a β-alcohol or amine provided π-conjugated β-substituted enones. Remarkably, nucleophile addition to the electron-rich vinylogous substrates is more rapid than classical enones, forming monosubstituted products. A doubly organocatalytic (organic diol and methyl aniline) conjugate addition synthesized the products directly from alkynyl ketones. Both of these catalytic transformations are orthogonal to transition metal catalysis, allowing for good yields, easily accessible or commercially available reagents, high selectivity, reagent recovery and recyclability, facile scalability, and exceptional functional group tolerance.
Scalable synthesis of highly reactive 1,3-diamino dienes from vinamidinium salts and their use in Diels-Alder reactions
Zhou, Sida,Sanchez-Larios, Eduardo,Gravel, Michel
scheme or table, p. 3576 - 3582 (2012/06/15)
A practical and chromatography-free synthesis of vinamidinium salts and their use as diene precursors in Diels-Alder reactions is reported. Additionally, 1,3-dipyrrolidino-1,3-butadiene was shown to be significantly more reactive than Rawal's diene in a c
