101258-12-2Relevant articles and documents
Discovery of mercaptopropanamide-substituted aryl tetrazoles as new broad-spectrum metallo-β-lactamase inhibitors
Yan, Yu-Hang,Chen, Jian,Zhan, Zhen,Yu, Zhu-Jun,Li, Gen,Guo, Li,Li, Guo-Bo,Wu, Yong,Zheng, Yongxiang
, p. 31377 - 31384 (2020)
β-Lactam antibiotic resistance mediated by metallo-β-lactamases (MBL) has threatened global public health. There are currently no available inhibitors of MBLs for clinical use. We previously reported the ruthenium-catalyzed meta-selective C-H nitration synthesis method, leading to some meta-mercaptopropanamide substituted aryl tetrazoles as new potent MBL inhibitors. Here, we described the structure-activity relationship of meta- and ortho-mercaptopropanamide substituted aryl tetrazoles with clinically relevant MBLs. The resulting most potent compound 13a showed IC50 values of 0.044 μM, 0.396 μM and 0.71 μM against VIM-2, NDM-1 and IMP-1 MBL, respectively. Crystallographic analysis revealed that 13a chelated to active site zinc ions via the thiol group and interacted with the catalytically important residues Asn233 and Tyr67, providing further structural information for the development of thiol based MBL inhibitors. This journal is
SUBSTITUTED SPIRO AZABICYCLICS AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
-
Page/Page column 69-70, (2008/06/13)
The present application describes modulators of CCR3 of formula (Ia) and (Ib): (I) or pharmaceutically acceptable salt forms thereof, wherein Z, R1, R2, R3, R4, R5, R5', R6, a, b
N-substituted heterocyclic amines as modulators of chemokine receptor activity
-
Page/Page column 28, (2010/02/06)
The present application describes modulators of chemokine receptors of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.