88460-72-4Relevant academic research and scientific papers
Identification, synthesis and evaluation of SARS-CoV and MERS-CoV 3C-like protease inhibitors
Kumar, Vathan,Tan, Kian-Pin,Wang, Ying-Ming,Lin, Sheng-Wei,Liang, Po-Huang
, p. 3035 - 3042 (2016/06/13)
Severe acute respiratory syndrome (SARS) led to a life-threatening form of atypical pneumonia in late 2002. Following that, Middle East Respiratory Syndrome (MERS-CoV) has recently emerged, killing about 36% of patients infected globally, mainly in Saudi Arabia and South Korea. Based on a scaffold we reported for inhibiting neuraminidase (NA), we synthesized the analogues and identified compounds with low micromolar inhibitory activity against 3CLpro of SARS-CoV and MERS-CoV. Docking studies show that a carboxylate present at either R1 or R4 destabilizes the oxyanion hole in the 3CLpro. Interestingly, 3f, 3g and 3m could inhibit both NA and 3CLpro and serve as a starting point to develop broad-spectrum antiviral agents.
Identification, synthesis, and evaluation of new neuraminidase inhibitors
Kumar, Vathan,Chang, Chih-Kang,Tan, Kian-Pin,Jung, Young-Sik,Chen, Shih-Hsun,Cheng, Yih-Shyun E.,Liang, Po-Huang
supporting information, p. 5060 - 5063 (2015/01/08)
High-throughput screening was performed on ～6800 compounds to identify KR-72039 as an inhibitor of H1N1 and H5N1 neuraminidases (NAs). Structure-activity relationship studies led to 3e, which inhibited H5N1 NA with an IC50 of 2.8 μM and blocked viral replication. Docking analysis shows that compounds bind to loop-430 around the NA active site. Compound 3l additionally inhibited H7N9 NA, making it a dual inhibitor of N1- and N2-type NAs.
Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase γ
Pomel, Vincent,Klicic, Jasna,Covini, David,Church, Dennis D.,Shaw, Jeffrey P.,Roulin, Karen,Burgat-Charvillon, Fabienne,Valognes, Delphine,Camps, Montserrat,Chabert, Christian,Gillieron, Corinne,Fran?on, Bernard,Perrin, Dominique,Leroy, Didier,Gretener, Denise,Nichols, Anthony,Vitte, Pierre Alain,Carboni, Susanna,Rommel, Christian,Schwarz, Matthias K.,Rückle, Thomas
, p. 3857 - 3871 (2007/10/03)
Class I phosphoinositide 3-kinases (PI3Ks), in particular PI3Kγ, have become attractive drug targets for inflammatory and autoimmune diseases. Here, we disclose a novel series of furan-2-ylmethylene thiazolidinediones as selective, ATP-competitive PI3Kγ i
