475489-78-2Relevant academic research and scientific papers
Discovery of Sisunatovir (RV521), an Inhibitor of Respiratory Syncytial Virus Fusion
Cockerill, G. Stuart,Angell, Richard M.,Bedernjak, Alexandre,Chuckowree, Irina,Fraser, Ian,Gascon-Simorte, Jose,Gilman, Morgan S. A.,Good, James A. D.,Harland, Rachel,Johnson, Sara M.,Ludes-Meyers, John H,Littler, Edward,Lumley, James,Lunn, Graham,Mathews, Neil,McLellan, Jason S.,Paradowski, Michael,Peeples, Mark E.,Scott, Claire,Tait, Dereck,Taylor, Geraldine,Thom, Michelle,Thomas, Elaine,Villalonga Barber, Carol,Ward, Simon E.,Watterson, Daniel,Williams, Gareth,Young, Paul,Powell, Kenneth
, p. 3658 - 3676 (2021/04/12)
RV521 is an orally bioavailable inhibitor of respiratory syncytial virus (RSV) fusion that was identified after a lead optimization process based upon hits that originated from a physical property directed hit profiling exercise at Reviral. This exercise encompassed collaborations with a number of contract organizations with collaborative medicinal chemistry and virology during the optimization phase in addition to those utilized as the compound proceeded through preclinical and clinical evaluation. RV521 exhibited a mean IC50 of 1.2 nM against a panel of RSV A and B laboratory strains and clinical isolates with antiviral efficacy in the Balb/C mouse model of RSV infection. Oral bioavailability in preclinical species ranged from 42 to >100% with evidence of highly efficient penetration into lung tissue. In healthy adult human volunteers experimentally infected with RSV, a potent antiviral effect was observed with a significant reduction in viral load and symptoms compared to placebo.
Understanding corrosion inhibition of mild steel in acid medium by new benzonitriles: Insights from experimental and computational studies
Chaouiki,Lgaz,Chung, Ill-Min,Ali,Gaonkar,Bhat,Salghi,Oudda,Khan
, p. 603 - 616 (2018/07/13)
Two benzonitrile derivatives, namely 4-(isopentylamino)-3-nitrobenzonitrile (PANB) and 3-amino-4-(isopentylamino)benzonitrile(APAB) have been synthesized and evaluated as corrosion inhibitors for mild steel (MS) in 1 M HCl solution at 303 K by gravimetric
BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS ANTIVARAL AGENTS
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Page/Page column 94, (2010/10/03)
The invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined in the specification, and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together
Respiratory syncytial virus fusion inhibitors. Part 5: Optimization of benzimidazole substitution patterns towards derivatives with improved activity
Wang, Xiangdong Alan,Cianci, Christopher W.,Yu, Kuo-Long,Combrink, Keith D.,Thuring, Jan W.,Zhang, Yi,Civiello, Rita L.,Kadow, Kathleen F.,Roach, Julia,Li, Zhufang,Langley, David R.,Krystal, Mark,Meanwell, Nicholas A.
, p. 4592 - 4598 (2008/02/11)
Extensive SAR studies and optimization of ADME properties of benzimidazol-2-one derivatives led to the identification of BMS-433771 (3) as an orally active RSV fusion inhibitor. In order to extend the structure-activity relationships for this compound ser
Synthesis of some new 2-substituted-phenyl-1H-benzimidazole-5-carbonitriles and their potent activity against Candida species
G?ker, Hakan,Ku?, Canan,Boykin, David W.,Yildiz, Sulhiye,Altanlar, Nurten
, p. 2589 - 2596 (2007/10/03)
New 2-substituted-phenyl-1H-benzimidazole-5-carboxylic acids (35, 38), ethyl-5-carboxylate (36), -5-carboxamides (37, 39),-5-carboxaldehyde (42), -5-chloro (40), -5-trifluoromethyl (41), and -5-carbonitriles (44-53, 55-67), -6-carbonitrile (54) were prepa
