Condensation of this thiohydantoin derivative with benzaldehyde and subsequent treatment with alkali yields benzal thiohydantoin (D), and the formation of this product demonstrates5 the presence in the original peptide of a glycine group with free carboxyl. Other considerations, not yet ripe for discussion here, suggest that a free carboxyl group belonging to eysteine is not also present. The f...

W. S. REITH AND N. M. WALDRON I954 DDPT is thus a suitable reagent for the determination of the amino-acid sequence in peptides by a process of step-wise degradation from the Nterminal end of the chain, and has in fact been successfully applied for this purpose. The conditions under which the N-terminal amino acid splits off as a substituted DDP-thiohydantoin are so mild that other peptide bond...

A series of zingerone?thiohydantoin hybrids were synthesized from O-alkyl zingerone derivatives by cyclocondensation with thiosemicarbazide in a two-step reaction. The obtained new potentially bioactive compounds structurally characterized IR and NMR spectroscopy, as well elemental HRMS analysis. In addition, their antimicrobial vitro anticancer activities tested. tested showed low to moderate ...

A high throughput screening and subsequent hit validation identified compound 1 as an inhibitor of Trypanosoma brucei parasite growth. Extensive structure-activity relationship optimization based on antiparasitic activity led to the highly potent compounds, 1-(4-fluorobenzyl)-3-(4-dimethylamino-3-chlorophenyl)-2-thiohydantoin (68) and 1-(2-chloro-4-fluorobenzyl)-3-(4-dimethylamino-3-methoxyphen...

This paper presents a method for synthesis and cytotoxicity of new platinum(II) complexes of (9'-fluorene)-spiro-5-hydantoin (L1) and (9'-fluorene)-spiro-5-(2-thiohydantoin) (L2). The new obtained complexes were studied by elemental analysis: ultraviolet-visible, attenuated total reflection Fourier transform infrared (ATR-FTIR), and 1H- and 13C-NMR for Pt(II) compounds and additionally Raman sp...

Two series of fused tetrahydro-β-carboline hydantoin and tetrahydro-β-carboline thiohydantoin derivatives with a pendant 2,4-dimethoxyphenyl at position 5 were synthesized, and chiral carbons at positions 5 and 11a swing from R,R to R,S, S,R, and S,S. The prepared analogues were evaluated for their capacity to inhibit phosphodiesterase 5 (PDE5) isozyme. The R absolute configuration of C-5 in th...

A new naked-eye chromogenic chemosensor based on 2-thiohydantoin shows high selectivity for fluoride ions and is used to develop a test paper for detection of fluoride ions in the solid state.

2-Thiohydantoin derivatives are produced by heating a mixture of thiourea and an alpha-amino acid. The method described offers the advantages of simplicity, low cost, easy work-up and scalability.

Changes in high localised concentrations of Ca2+ ions are fundamental to cell signalling. The synthesis of a dual excitation, ratiometric calcium ion sensor with a Kd of 90 μM, is described. It is tagged with an azido group for bioconjugation, and absorbs in the blue/green and emits in the red region of the visible spectrum with a large Stokes shift. The binding modulating nitro group is introd...

A novel and practical two-step approach to an intriguing class of imidazo[1,5-a]pyrazines with exocyclic C=X (X = CH2, O) bonds is described. The process utilizes a sequential three-component reaction of propargyl amine or aminoester, 1,2-diaza-1,3-dienes and isothiocyanates to furnish functionalized 2-thiohydantoins which are transformed into thiohydantoin-fused tetrahydropyrazines by subseque...