Imidazole Biochem/physiol Actions: Imidazole derivatives have antibacterial, antifungal and anticancer functionality. It interacts with DNA and also binds to protein and stops cell division. 10111-08-7, formula is C4H4N2O, Name is 1H-Imidazole-2-carbaldehyde. It also acts as a microtubule destabilizing agents and inhibits topoisomerase and Cytochrome P450 Family 26 Subfamily A Member 1 (CYP26A1) enzymes. Application In Synthesis of 10111-08-7.
Sestito, Simona;Bacci, Andrea;Chiarugi, Sara;Runfola, Massimiliano;Gado, Francesca;Margheritis, Eleonora;Gul, Sheraz;Riveiro, Maria E.;Vazquez, Ramiro;Huguet, Samuel;Manera, Clementina;Rezai, Keyvan;Garau, Gianpiero;Rapposelli, Simona research published 《 Development of potent dual PDK1/AurA kinase inhibitors for cancer therapy: Lead-optimization, structural insights, and ADME-Tox profile》, the research content is summarized as follows. We report the synthesis of novel first-in-class I as dual PDK1-AurA kinase inhibitors as a novel strategy to treat Ewing sarcoma. The most potent compound I [R1 = H, R2 = phenyl] is suitable for progression to in vivo studies. The specific attributes of I [R1 = H, R2 = phenyl] included nanomolar inhibitory potency against both phosphoinositide-dependent kinase-1 (PDK1) and Aurora A (AurA) kinase, with acceptable in vitro ADME-Tox properties (cytotoxicity in 2 healthy and 14 hematol. and solid cancer cell-lines; inhibition of PDE4C1, SIRT7, HDAC4, HDAC6, HDAC8, HDAC9, AurB, CYP1A2, CYP2C9, CYP2C19, CYP2D6, and hERG). X-ray crystallog. and docking studies led to the identification of the key AurA and PDK1/I [R1 = H, R2 = phenyl] interactions. Finally, in vitro drug-intake kinetics and in vivo PK appear to indicate that these compounds are attractive lead-structures for the design and synthesis of PDK1/AurA dual-target mols. to further investigate the in vivo efficacy against Ewing Sarcoma.
Application In Synthesis of 10111-08-7, 1H-Imidazole-2-carbaldehyde, also known as 1H-Imidazole-2-carbaldehyde, is a useful research compound. Its molecular formula is C4H4N2O and its molecular weight is 96.09 g/mol. The purity is usually 95%.
1H-Imidazole-2-carboxaldehyde is a novel PTP1b inhibitor with potential application to treat type 2 diabetes.
1H-Imidazole-2-carboxaldehyde is a broad-spectrum antimicrobial that has been shown to inhibit the growth of bacteria by interfering with protein synthesis. It binds to the cytosolic protein and receptor molecule, which are involved in the activation of bacterial enzymes. Imidazole-2-carboxaldehyde reacts with anhydrous sodium and copper complex to produce hydrogen bonds, which prevent the formation of the nitrogen atoms necessary for cellular processes. This chemical also has biological properties such as glyoxal, which inhibits bacterial growth by reacting with amino groups on proteins., 10111-08-7.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem