F. Monforte

TL;DR: It was found that the substitution pattern on the 5-benzylidene moiety markedly influenced the activity of N-unsubstituted 2,4-thiazolidinediones 2, compounds with substituents at the meta position being generally more effective than the para-subst ituted ones; however, this SAR was not evidenced in acetates 3 and acids 4.

TL;DR: Mesono isomers showed better pharmacological profiles than corresponding racemates and Methoxy substitution patterns of the aryls on stereogenic carbons are generally the most favorable on the pharmacological profile.

TL;DR: Their antimycobacterial in vitro activity was evaluated against Mycobacterium tuberculosis H37Rv in comparison with the ligands and displayed MIC values < or = 0.2 microg/mL.

TL;DR: Within the series of chiral 3,3'-(1,2-ethanediyl)bis[2-arylthiazolidin-4-ones], the 3,4-dimethoxyphenyl substituted derivative was found in the primary anti-inflammatory screening to be endowed with superior in vivo properties and good safety profile.

TL;DR: Interestingly, selected compounds 1 to 3, mostly hydrazides (compounds 2), were effective in killing M. tuberculosis growing within macrophages at concentrations in culture medium which were much lower than the corresponding MICs.