140439-35-6Relevant articles and documents
Identification of inhibitors targeting polyketide synthase 13 of Mycobacterium tuberculosis as antituberculosis drug leads
Wang, Xiao,Zhao, Wenting,Wang, Bin,Ding, Wei,Guo, Hao,Zhao, Hongyi,Meng, Jianzhou,Liu, Sihan,Lu, Yu,Liu, Yishuang,Zhang, Dongfeng
, (2021/06/30)
Polyketide synthase 13 (Pks13) is an essential enzyme in the synthesis of mycolic acids in Mtb. Therefore, Pks13 is a promising drug target for tuberculosis treatment. We used a structure-guided approach to identify novel chemotype inhibitors of Pks13 and assessed them using a Pks13 enzymatic assay and surface plasmon resonance. The structure–activity relationships (SAR) results demonstrated that the substituents at the 2, 5, and 6 positions of the 4H-chromen-4-one scaffold are critical for maintaining the MIC. Compound 6e with 2-hydroxyphenyl at the 2 position of the 4H-chromen-4-one scaffold, exhibited potent activity against Mtb H37Rv (MIC = 0.45 μg/mL) and displayed good Pks13 affinity and inhibition (IC50 = 14.3 μM). This study described here could provide an avenue to explore a novel inhibitor class for Pks13 and aid the further development of antituberculosis drugs.
(Aminoalkoxy)chromones. Selective ? Receptor Ligands
Erickson, Ronald H.,Natalie, Kenneth J.,Bock, William,Lu, Zhijian,Farzin, Farzaneh,et al.
, p. 1526 - 1535 (2007/10/02)
A series of (aminoalkoxy)chromones has been prepared, members of which bind potently (16-100 nM) at the ? binding site and bind weakly (>1000 nm) at the dopamine D2 receptor and 33 other receptors, second messenger systems, and ion channels.At
