82859-77-6Relevant academic research and scientific papers
Analgesic and anti-inflammatory activities of salicylaldehyde 2-chlorobenzoyl hydrazone (H2LASSBio-466), salicylaldehyde 4-chlorobenzoyl hydrazone (H2LASSBio-1064) and their zinc(II) complexes
Junior, Walfrido Bispo,Alexandre-Moreira, Magna S.,Alves, Marina A.,Perez-Rebolledo, Anayive,Parrilha, Gabrieli L.,Castellano, Eduardo E.,Piro, Oscar E.,Barreiro, Eliezer J.,Lima, Lidia Moreira,Beraldo, Heloisa
, p. 6902 - 6915 (2011)
Salicylaldehyde 2-chlorobenzoyl hydrazone (H2LASSBio-466), salicylaldehyde 4-chlorobenzoyl hydrazone (H2LASSBio-1064) and their complexes [Zn(LASSBio- 466)H2O]2 (1) and [Zn(HLASSBio-1064)Cl]2 (2) were
Modulation of estrogen-related receptors subtype selectivity: Conversion of an ERRβ/γ selective agonist to ERRα/β/γ pan agonists
Avdagic, Amer,Billon, Cyrielle,Burris, Sheryl L.,Burris, Thomas P.,Elagawany, Mohamed,Elgendy, Bahaa,Goher, Shaimaa S.,Hegazy, Lamees,Sanders, Ryan,Shahien, Mohamed,Sitaula, Sadichha
, (2020/07/21)
Estrogen Related Receptors (ERRs) are key regulators of energy homeostasis and play important role in the etiology of metabolic disorders, skeletal muscle related disorders, and neurodegenerative diseases. Among the three ERR isoforms, ERRα emerged as a potential drug target for metabolic and neurodegenerative diseases. Although ERRβ/γ selective agonist chemical tools have been identified, there are no chemical tools that effectively target ERRα agonism. We successfully engineered high affinity ERRα agonism into a chemical scaffold that displays selective ERRβ/γ agonist activity (GSK4716), providing novel ERRα/β/γ pan agonists that can be used as tools to probe the physiological roles of these nuclear receptors. We identified the structural requirements to enhance selectivity toward ERRα. Molecular modeling shows that our novel modulators have favorable binding modes in the LBP of ERRα and can induce conformational changes where Phe328 that originally occupies the pocket is dislocated to accommodate the ligands in a rather small cavity. The best agonists up-regulated the expression of target genes PGC-1α and PGC-1β, which are necessary to achieve maximal mitochondrial biogenesis. Moreover, they increased the mRNA levels of PDK4, which play an important role in energy homeostasis.
Oxomolybdenum(V) Complexes of Some Multidentate N-O Donors
Poddar, S. N.,Samanta, G. C.,Mukherjee, G.,Ghosh, S.
, p. 7 - 10 (2007/10/02)
A number of oxomolybdenum(V) complexes of some multidentate N-O donors in the form of Schiff bases have been synthesised and studied.The Schiff bases were obtained by condensing aromatic acid hydrazides with salicyladehyde (ligands designated as L1H2) and with biacetylmonoxyme (ligands designated as L2H2).All these ligands exhibit tridentate fuction in forming the complexes.The ligands L1H2 formed complexes of the type MoO(L1H)Cl2 (Type A), whereas L2H2 yielded complexes of the type Mo2O3(L2H)2Cl2 (Type B).All the type A complexes are mononuclear, while the type B complexes are binuclear with oxygen-bridging between two Mo atoms.The isolated complexes were characterised by elemental analysis, spectroscopic (uv-visible, ir), magnetic and conductance data.
