Structure-activity relationships of novel potent MurF inhibitors.

Bioorg Med Chem Lett

Infectious Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 200 Abbott Park Road, Abbott Park, IL 60064, USA.

Published: January 2004

A novel class of MurF inhibitors was discovered and structure-activity relationship studies have led to several potent compounds with IC(50)=22 approximately 70 nM. Unfortunately, none of these potent MurF inhibitors exhibited significant antibacterial activity even in the presence of bacterial cell permeabilizers.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2003.09.073DOI Listing

Publication Analysis

Top Keywords

murf inhibitors
12
potent murf
8
structure-activity relationships
4
relationships novel
4
novel potent
4
inhibitors novel
4
novel class
4
class murf
4
inhibitors discovered
4
discovered structure-activity
4

Similar Publications

[Effect of electroacupuncture on denervated skeletal muscle atrophy in rats based on p38 MAPK signaling pathway].

Zhongguo Zhen Jiu

January 2025

College of TCM, Chongqing Medical University, Chongqing Key Laboratory of TCM for Prevention and Treatment of Metabolic Diseases, Chongqing 410007, China.

Objective: To assess the impacts of electroacupuncture (EA) on the gait, oxidative stress, inflammatory reaction, and protein degradation in the rats of denervated skeletal muscle atrophy, and explore the potential mechanism of EA for alleviating denervated skeletal muscle atrophy.

Methods: Forty male SD rats, 8 weeks old, were randomly assigned to a sham-surgery group, a model group, an EA group, and a p38 MAPK inhibitor group, with 10 rats in each group. The right sciatic nerve was transected to establish a rat model of denervated skeletal muscle atrophy in the model group, the EA group and the p38 MAPK inhibitor group.

View Article and Find Full Text PDF

Daidzein improves muscle atrophy caused by lovastatin by regulating the AMPK/FOXO3a axis.

Chin Med

December 2024

State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.

Background: Lovastatin, the main lipid-lowering component in red yeast rice, is a golden anti-lipid drug, but its long-term application is continuously challenged by potential skeletal muscle atrophy. Daidzein, an isoflavone derived from soybeans and many Chinese medicines, shows therapeutic potential in treating muscle-related diseases and metabolic disorders. However, whether daidzein can improve lovastatin-induced muscle atrophy and the specific mechanism needs to further study.

View Article and Find Full Text PDF

Tetrandrine induces muscle atrophy involving ROS-mediated inhibition of Akt and FoxO3.

Mol Med

November 2024

The Jiangsu Key Laboratory for Molecular and Medical Biotechnology, School of Life Sciences, Nanjing Normal University, Nanjing, 210023, China.

Tetrandrine (Tet), a well-known drug of calcium channel blocker, has been broadly applied for anti-inflammatory and anti-fibrogenetic therapy. However, due to the functional diversity of ubiquitous calcium channels, potential side-effects may be expected. Our previous report revealed an inhibitory effect of Tet on myogenesis of skeletal muscle.

View Article and Find Full Text PDF

Background: Sarcopenia is a muscle disease characterized by reduction of muscle strength and muscle mass. In RA, 25.9 to 43.

View Article and Find Full Text PDF
Article Synopsis
  • - Chemobrain is a negative cognitive effect linked to doxorubicin (DOX) chemotherapy, caused by oxidative stress that leads to inflammation and cell death, affecting cancer survivors' mental functions.
  • - The study explored the neuroprotective potential of empagliflozin (EMPA) against DOX-induced chemobrain in rats, showcasing that higher doses of EMPA improved memory, motor skills, and reduced anxiety while preserving neurons in key brain regions.
  • - Biochemical analyses indicated that EMPA treated rats exhibited lower inflammatory and apoptotic signals, increased SIRT-1 protein, and changes in gene expression, suggesting that EMPA could effectively mitigate the cognitive impairments associated with DOX, possibly through specific cellular
View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!