AI Medical Compendium Journal:
RSC medicinal chemistry

Showing 1 to 5 of 5 articles

Scaffold hopping based designing of selective ALDH1A1 inhibitors to overcome cyclophosphamide resistance: synthesis and biological evaluation.

RSC medicinal chemistry
Aldehyde dehydrogenase 1A1 (ALDH1A1) is an isoenzyme that catalyzes the conversion of aldehydes to acids. However, the overexpression of ALDH1A1 in a variety of malignancies is the major cause of resistance to an anti-cancer drug, cyclophosphamide (C...

A scaffold hopping strategy to generate new aryl-2-amino pyrimidine MRSA biofilm inhibitors.

RSC medicinal chemistry
Infections that stem from bacterial biofilms are difficult to eradicate. Within a biofilm state, bacteria are upwards of 1000-fold more resistant to conventional antibiotics, necessitating the development of alternative approaches to treat biofilm-ba...

Structure-activity relationship studies on 2,5,6-trisubstituted benzimidazoles targeting -FtsZ as antitubercular agents.

RSC medicinal chemistry
Filamenting temperature sensitive protein Z (FtsZ) is an essential bacterial cell division protein and a promising target for the development of new antibacterial therapeutics. As a part of our ongoing SAR studies on 2,5,6-trisubstituted benzimidazol...

Rational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 2.

RSC medicinal chemistry
Building on our previously-reported novel tricyclic topoisomerase inhibitors (NTTIs), we disclose the discovery of REDX07965, which has an MIC of 0.5 μg mL against , favourable pharmacokinetic properties, selectivity human topoisomerase II and an a...

Rational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 1.

RSC medicinal chemistry
The alarming reduction in drug effectiveness against bacterial infections has created an urgent need for the development of new antibacterial agents that circumvent bacterial resistance mechanisms. We report here a series of DNA gyrase and topoisomer...