Thiazolidine formation from L-cysteine and formaldehyde

Cyclic peptides from linear unprotected peptide precursors through thiazolidine formation.

This has been largely discussed under synthesis.

Aliphatic nitro compounds are synthesised by;
This commercial free radical process involves the NO2 radical;
The use of the enolate active methylenes forms a stable product dueto the chelation of the counter ion;Two products, a nitro compound and a nitrite ester, are produced dueto the sodium nitrate acting as an ambident nucleophile, either a N orO nucleophile;The use of silver nitrate produces only the nitro compound as it isnot an ambident nucleophile.

Design and synthesis of novel thiazolidine-2,4-diones …

The promising and broad biological activity of the heterocyclic pharmacophore has sparked our interests in the design and synthesis of such novel pseudodisaccharide derivatives for drug discovery.The thiazolidin-4-one ring is a core substructure in various synthetic pharmaceuticals that are associated with diverse biological activities, such as antibacterial, anti-fungal, anti-cancer, antiviral, anti-inflammatory and analgesic, and calcium antagonistic activities among others.

The promising and broad biological activity of the heterocyclic pharmacophore has sparked our interests in the design and synthesis of such novel pseudodisaccharide derivatives for drug discovery.The thiazolidin-4-one ring is a core substructure in various synthetic pharmaceuticals that are associated with diverse biological activities, such as antibacterial, anti-fungal, anti-cancer, antiviral, anti-inflammatory and analgesic, and calcium antagonistic activities among others.


Design and Synthesis of novel Thiazolidine-2,4 …

N2 - A new series of thiazolidine derivatives with an adamantyl group was synthesized and evaluated for their ability to inhibit 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1). Our initial compound 5a showed a weak inhibitory activity. Significant improvements in potency were achieved by substituent modification. The potent compound 8g (E) showed good in vitro inhibitory activity toward human 11β-HSD1, selectivity toward 11β-HSD2, metabolic stability, pharmacokinetic, and safety profile. Furthermore, this compound significantly inhibited 11β-HSD1 activity in rat and monkey models, and showed improved glycemic control in KKAy mice.

L(-)-Thiazolidine-4-carboxylic acid | 34592-47-7

AB - A new series of thiazolidine derivatives with an adamantyl group was synthesized and evaluated for their ability to inhibit 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1). Our initial compound 5a showed a weak inhibitory activity. Significant improvements in potency were achieved by substituent modification. The potent compound 8g (E) showed good in vitro inhibitory activity toward human 11β-HSD1, selectivity toward 11β-HSD2, metabolic stability, pharmacokinetic, and safety profile. Furthermore, this compound significantly inhibited 11β-HSD1 activity in rat and monkey models, and showed improved glycemic control in KKAy mice.

Synthesis and biological evaluation of thiazolidine …

Thiazolidine thioester peptides were synthesized by reacting bis(2-sulfanylethyl)amido peptides with glyoxylic acid at pH 1. A significant increase in Native Chemical Ligation (NCL) rate was observed with thiazolidine thioesters compared to 3-mercaptopropionic acid-thioester analogues. The method is of particular interest for accelerating valine-cysteine peptide bond formation.

A convenient synthesis of novel thiazolidin-4 ..

A new series of thiazolidine derivatives with an adamantyl group was synthesized and evaluated for their ability to inhibit 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1). Our initial compound 5a showed a weak inhibitory activity. Significant improvements in potency were achieved by substituent modification. The potent compound 8g (E) showed good in vitro inhibitory activity toward human 11β-HSD1, selectivity toward 11β-HSD2, metabolic stability, pharmacokinetic, and safety profile. Furthermore, this compound significantly inhibited 11β-HSD1 activity in rat and monkey models, and showed improved glycemic control in KKAy mice.