Suzuki, Takayoshi; Khan, Mohammed Naseer Ahmed; Sawada, Hideyuki; Imai, Erika; Itoh, Yukihiro; Yamatsuta, Katsura; Tokuda, Natsuko; Takeuchi, Jun; Seko, Takuya; Nakagawa, Hidehiko; Miyata, Naoki published the artcile< Design, Synthesis, and Biological Activity of a Novel Series of Human Sirtuin-2-Selective Inhibitors>, COA of Formula: C8H8BrCl, the main research area is anilinobenzamide preparation selective sirtuin inhibitor; phenethyloxyanilinobenzamide preparation selective inhibition SIRT2; structure anilinobenzamide inhibition selectivity human sirtuin isoform.
Anilinobenzamides such as I [R = H, PhNHCO, PhNMeCO, PhCH2NHCO, PhCH2NMeCO, PhCH2CONH, PhCH2CONMe, cyclohexylmethoxy, Me2CHCH2O, PhCH2O, PhCH2CH2O, R2CH2CH2O, PhCH2CH2CH2O; R2 = 2-MeC6H4, 3-MeC6H4, 4-MeC6H4, 2-F3CC6H4, 3-F3CC6H4, 4-F3CC6H4, 2-FC6H4, 3-FC6H4, 4-FC6H4, 2-ClC6H4, 3-ClC6H4, 4-ClC6H4, 2-BrC6H4, 3-BrC6H4, 4-BrC6H4; R1 = H, (E)-PhCH:CH, (Z)-PhCH:CH, PhCH2CH2, PhNMeCO, PhNHCO, PhCONMe, PhCONH, R3CONH; R3 = Me, Me2CH, cyclohexyl, 4-piperidinyl, 2-pyridinyl, 3-pyridinyl, 4-pyridinyl] were prepared as selective inhibitors of human sirtuin 2 (SIRT2), a deacetylase with potential involvement in neurodegenerative diseases such as Parkinson’s and Huntington’s diseases. In particular, phenethyloxyanilinobenzamides such as I (R = R2CH2CH2O; R1 = H; R2 = Ph, 3-FC6H4) were potent and selective SIRT2 inhibitors, with 3.5-fold greater SIRT2 inhibition and more than 35-fold greater selectivity for SIRT2 over SIRT1 and SIRT3 than the previously known dichlorophenylfuranylpropenamide SIRT2 inhibitor AGK2. I (R = PhCH2CH2; R1 = H) dose-dependently inhibited SIRT2 in human colon cancer HCT116 cells.
Journal of Medicinal Chemistry published new progress about Aromatic amides Role: PAC (Pharmacological Activity), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, COA of Formula: C8H8BrCl.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics