In 2020.0 EUR J MED CHEM published article about THERMAL SHIFT ASSAYS; CYCLOPHILIN-A; REPLICATION; INFECTION; PROTEIN; ROLES; INHIBITION; DISCOVERY; POTENT; CELLS in [Wang, Lei; Vernekar, Sanjeev Kumar V.; Do, Ha T.; Sahani, Rajkumar Lalji; Xie, Jiashu; Wang, Zhengqiang] Univ Minnesota, Coll Pharm, Ctr Drug Design, Minneapolis, MN 55455 USA; [Casey, Mary C.] Univ Missouri, Christopher S Bond Life Sci Ctr, Dept Mol Microbiol & Immunol, Sch Med, Columbia, MO 65211 USA; [Kirby, Karen A.; Du, Haijuan; Zhang, Huanchun; Tedbury, Philip R.; Sarafianos, Stefan G.] Emory Univ, Dept Pediat, Lab Biochem Pharmacol, Sch Med, Atlanta, GA 30322 USA; [Hachiya, Atsuko] Natl Hosp Org, Clin Res Ctr, Nagoya Med Ctr, Nagoya, Aichi 4600001, Japan; [Wang, Lei] Dalian Univ Technol, Sch Chem Engn, Dept Pharm, Dalian 116024, Peoples R China in 2020.0, Cited 51.0. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9. Formula: C13H13N
The capsid protein (CA) of HIV-1 plays essential roles in multiple steps of the viral replication cycle by assembling into functional capsid core, controlling the kinetics of uncoating and nuclear entry, and interacting with various host factors. Targeting CA represents an attractive yet underexplored antiviral approach. Of all known CA-targeting small molecule chemotypes, the peptidomimetic PF74 is particularly interesting because it binds to the same pocket used by a few important host factors, resulting in highly desirable antiviral phenotypes. However, further development of PF74 entails understanding its pharmacophore and mitigating its poor metabolic stability. We report herein the design, synthesis, and evaluation of a large number of PF74 analogs aiming to provide a comprehensive chemical profiling of PF74 and advance the understanding on its detailed binding mechanism and pharmacophore. The analogs, containing structural variations mainly in the aniline domain and/or the indole domain, were assayed for their effect on stability of CA hexamers, antiviral activity, and cytotoxicity. Selected analogs were also tested for metabolic stability in liver microsomes, alone or in the presence of a CYP3A inhibitor. Collectively, our studies identified important pharmacophore elements and revealed additional binding features of PF74, which could aid in future design of improved ligands to better probe the molecular basis of CA-host factor interactions, design strategies to disrupt them, and ultimately identify viable CA-targeting antiviral leads. (C) 2020 Elsevier Masson SAS. All rights reserved.
Formula: C13H13N. About Diphenylmethanamine, If you have any questions, you can contact Wang, L; Casey, MC; Vernekar, SKV; Do, HT; Sahani, RL; Kirby, KA; Du, HJ; Hachiya, A; Zhang, HC; Tedbury, PR; Xie, JS; Sarafianos, SG; Wang, ZQ or concate me.
Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics