Zhong, Ying-Ying; Chen, Hui-Sheng; Wu, Pan-Pan; Zhang, Bing-Jie; Yang, Yang; Zhu, Qiu-Yan; Zhang, Chun-Guo; Zhao, Su-Qing published an article about the compound: 5-Chloropicolinaldehyde( cas:31181-89-2,SMILESS:O=CC1=NC=C(Cl)C=C1 ).COA of Formula: C6H4ClNO. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:31181-89-2) through the article.
Considerable interest has been attracted in oleanolic acid and its analogs because of their hypoglycemic activity. In this study, a series of novel oleanolic acid analogs against α-glucosidase were synthesized and their biol. activities were evaluated in vitro and in vivo. In vitro α-glucosidase inhibition activity results indicated that most of the designed analogs exhibited prominent inhibition activities, especially compounds I [R = 4-MeC6H4, 2,4-(MeO)2C6H3, 4-MeOC6H4, 3-ClC6H4] (II) which have IC50 values of 0.33 ± 0.01, 0.98 ± 0.06, 0.69 ± 0.01 and 0.72 ± 0.21 μM, resp. Enzyme kinetic studies on the most potent compounds reveled that derivatives II were noncompetitive inhibitors. Moreover, the docking studies were carried out to prove that the four compounds could interact with the hydrophobic region of the active pocket and form hydrogen bonds to enhance the binding affinity of them with the α-glucosidase. The cytotoxicity evaluation assay demonstrated a high level of safety profile of the active compounds II against normal 3T3 cell line. Furthermore, the in vivo actual pharmacol. potential studies on derivatives II showed that the hypoglycemic effects of them were comparable to that of pos. control, acarbose.
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Reference:
Phosphine ligand,
Chiral phosphine ligands in asymmetric synthesis. Molecular structure and absolute configuration of (1,5-cyclooctadiene)-(2S,3S)-2,3-bis(diphenylphosphino)butanerhodium(I) perchlorate tetrahydrofuran solvate