id	author	title	date	pages	extension	mime	words	sentences	flesch	summary	cache	txt
cord-327946-mqakaisa	Massari, Serena	Synthesis and Characterization of 1,2,4-Triazolo[1,5-a]pyrimidine-2-carboxamide-based Compounds Targeting the PA-PB1 Interface of Influenza A Virus Polymerase	2020-10-16		.txt	text/plain	3467	205	48	title: Synthesis and Characterization of 1,2,4-Triazolo[1,5-a]pyrimidine-2-carboxamide-based Compounds Targeting the PA-PB1 Interface of Influenza A Virus Polymerase In search for new anti-Flu drugs, our group has focused on viral RNA-dependent RNA polymerase (RdRP) developing disruptors of PA-PB1 subunits interface with the best compounds characterized by cycloheptathiophene-3-carboxamide and 1,2,4-triazolo[1,5-a]pyrimidine-2-carboxamide scaffolds. In particular, a thorough exploration of the cycloheptathiophene-3-carboxamide moiety led to acquire important SAR insight and identify new active compounds showing both the ability to inhibit PA-PB1 interaction and viral replication in the micromolar range and at non-toxic concentrations. Finally, with the aim to gain information on how two different moieties, such as the cHTC and the 2-carbamoylphenyl, showed a favorable ability to disrupt PA-PB1 interaction, computational studies were performed to predict the binding mode of benzamide derivative 23 within the PA cavity with respect to hit compound 4.	./cache/cord-327946-mqakaisa.txt	./txt/cord-327946-mqakaisa.txt