AI Article Synopsis

  • This text discusses a new group of compounds called 3,5-diaryl-1H-pyrazoles, which are designed to specifically inhibit certain enzymes in bacteria known as arylamine N-acetyltransferases.
  • The research mentions that one of these compounds was discovered during a previous high-throughput screening process and has shown effectiveness in stopping the growth of Mycobacterium tuberculosis, the bacteria responsible for tuberculosis.
  • The overall goal of this study is to develop potential treatments against tuberculosis by targeting these specific enzymes with the new pyrazole compounds.

Article Abstract

The synthesis and inhibitory potencies of a novel series of 3,5-diaryl-1H-pyrazoles as specific inhibitors of prokaryotic arylamine N-acetyltransferase enzymes is described. The series is based on hit compound 1 3,5-diaryl-1H-pyrazole identified from a high-throughout screen that has been carried out previously and found to inhibit the growth of Mycobacterium tuberculosis.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2013.02.052DOI Listing

Publication Analysis

Top Keywords

arylamine n-acetyltransferase
8
design synthesis
4
synthesis structure-activity
4
structure-activity relationships
4
relationships 35-diaryl-1h-pyrazoles
4
35-diaryl-1h-pyrazoles inhibitors
4
inhibitors arylamine
4
n-acetyltransferase synthesis
4
synthesis inhibitory
4
inhibitory potencies
4

Similar Publications

Novel inhibitors of the (VIBVN) NAT protein identified through pharmacophore modeling.

Sci Rep

January 2025

Key Laboratory of Marine Drugs, School of Medicine and Pharmacy, Ministry of Education, Ocean University of China, Qingdao, 266071, China.

Arylamine N-acetyltransferases (NATs, E.C. 2.

View Article and Find Full Text PDF

Effect of Genetic Variants on Rosuvastatin Pharmacokinetics in Healthy Volunteers: Involvement of , and .

Int J Mol Sci

December 2024

Clinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto de Investigación Sanitaria La Princesa (IIS-Princesa), 28006 Madrid, Spain.

Statins are the primary drugs used to prevent cardiovascular disease by inhibiting the HMG-CoA reductase, an enzyme crucial for the synthesis of LDL cholesterol in the liver. A significant number of patients experience adverse drug reactions (ADRs), particularly musculoskeletal problems, which can affect adherence to treatment. Recent clinical guidelines, such as those from the Clinical Pharmacogenetics Implementation Consortium (CPIC) in 2022, recommend adjusting rosuvastatin doses based on genetic variations in the and genes to minimize ADRs and improve treatment efficacy.

View Article and Find Full Text PDF

One of the functions of placenta is to protect the fetus against harmful xenobiotics. Protective mechanisms of placenta are based on enzymes, e.g.

View Article and Find Full Text PDF

3,4-Dimethylaniline (3,4-DMA) is present in cigarette smoke and widely used as an intermediate in dyes, drugs, and pesticides. Nucleotide excision repair-deficient Chinese hamster ovary (CHO) cells stably transfected with human CYP1A2 and N-acetyltransferase 1 (NAT1) alleles: (reference allele) or (the most common variant allele) were utilized to assess 3,4-DMA -acetylation and hypoxanthine phosphoribosyl transferase (HPRT) mutations, double-strand DNA breaks and reactive oxygen species (ROS). CHO cells expressing exhibited significantly ( < 0.

View Article and Find Full Text PDF

Introduction: Tuberculosis (TB) is the leading infectious cause of death globally. Despite WHO recommendations for TB preventive therapy (TPT), challenges persist, including incompletion of treatment and adverse drug reactions (ADRs). There is limited data on the 3-month isoniazid and rifapentine (3HP) pharmacokinetics, pharmacogenomics and their relation with ADRs.

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!