Structure-Activity Studies of Pyrrolnitrin Analogues

Synthesis and structure–activity relationship studies of teixobactin analogues

A new series of teixobactin analogues were synthesized via an oxidative cyclative cleavage approach using aryl hydrazide resin as the solid support. Structure–activity relationship studies revealed that the guanidine or amine group at position 10, the hydroxyl group of Ser7 residue and the NH proton of the N-terminal Phe1 residue are critical to the antibacterial activities, while side chain si...

Synthesis and Characterization of Quinazolinone-hydrazide Analogues: Structure Activity Relationship (sar) Studies of Anti- Microbial Activity

Antinociceptive activity of structural analogues of rotundifolone: structure-activity relationship.

Rotundifolone, a monoterpene isolated from the essential oil of the leaves of Mentha x villosa, is a constituent of several essential oils and known to have antinociceptive activity. Our recent study demonstrated that the analogues of rotundifolone showed also a significant antinociceptive effect. In the present report, to investigate the correlation between the structure and antinociceptive ac...

Choleretic activity of phloracetophenone in rats: structure-function studies using acetophenone analogues.

The relationship between the chemical structure and choleretic activity of phloracetophenone (2,4,6-trihydroxyacetophenone) was investigated in adult male rats. Fourteen acetophenone analogues, with different substituents on the benzene nucleus, were intraduodenally administered and bile samples were collected via a bile fistula. All of the compounds tested immediately induced choleresis. For t...

Quantitative structure-antitumor activity relationships of camptothecin analogues: cluster analysis and genetic algorithm-based studies.

Topoisomerase 1 (top1) inhibitors are proving useful against a range of refractory tumors, and there is considerable interest in the development of additional top1 agents. Despite crystallographic studies, the binding site and ligand properties that lead to activity are poorly understood. Here we report a unique approach to quantitative structure-activity relationship (QSAR) analysis based on t...