In vitro assays identified thiohydantoins with anti-trypanosomatid activity and molecular modelling studies indicated possible selective CYP51 inhibition [PDF]
This work investigates the anti-trypanosomal activities of ten thiohydantoin derivatives against the parasite Trypanosoma cruzi. Compounds with aliphatic chains (THD1, THD3, and THD5) exhibited the most promising IC50 against the epimastigote form of T ...
Priscila Goes Camargo +9 more
doaj +2 more sources
A Plausible Prebiotic One-Pot Synthesis of Orotate and Pyruvate Suggestive of Common Protometabolic Pathways. [PDF]
A prebiotic synthesis of the nucleobase orotate, and the citric acid cycle intermediate pyruvate, proceeds in a single pot from two small glycine derivatives, hydantoin and glyoxylate, under mild aqueous conditions. These findings support a co‐evolution of pathways to core protometabolites and nucleic acid building blocks in a common environment ...
Clay AP +5 more
europepmc +3 more sources
Aldol Reactions of Conformationally Stable Axially Chiral Thiohydantoin Derivatives [PDF]
Sevgi Sarigul Ozbek +2 more
doaj +2 more sources
Synthesis and biological activity of novel zingerone-thiohydantoin hybrids [PDF]
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 were structurally characterized by IR and
Virijević Katarina D. +6 more
doaj +1 more source
Synthesis and Identification of Heterobivalent Anticancer Compounds Containing Urea and 5-Arylidene-2-Thiohydantoin Motifs. [PDF]
A synthetic approach to the synthesis of novel heterobivalent compounds containing urea and 5‐arylthiohydantoin groups was developed for the preparation of a mixture‐based library. Through the screening and deconvolution of the library, six hits with βC branched residues at R1 and imidazyl residue at R3 were identified exhibiting moderate inhibitory ...
Whitely C, Winburn H, Li Y.
europepmc +2 more sources
One-Pot Gateway to Quinazoline–Thiohydantoin Fused Scaffolds and Discovery of Their Antileukemic Activity [PDF]
Lena Kersting +13 more
doaj +2 more sources
Reactions of Nitrile Imines with Thiohydantoin Derivatives: Unexpected Chemoselectivity of the 1,3-Dipolar Cycloaddition: Preferential Addition of C=C rather than C=S Bonds [PDF]
Maria E. Filkina +6 more
doaj +2 more sources
The title molecule, C23H26N2O4S, adopts a cup-shaped conformation. In the crystal, layers lying parallel to the ab plane are formed by C—H...O hydrogen bonds and C—H...π(ring) interactions.
Walid Guerrab +4 more
doaj +1 more source
Efforst are described for developing Brønsted base‐catalyzed, site‐ and stereoselective α‐functionalization of a variety of unsaturated enolizable carbonyl compounds via transient enolates featuring an extended π‐system. Abstract Chiral Brønsted base (BB) catalyzed asymmetric transformations constitute an important tool for synthesis.
Mikel Oiarbide, Claudio Palomo
wiley +1 more source
A new strategy has been proposed for the synthesis of an array of imidazo[5,1‐c][1,4]oxazine chemotypes by using a planned aza‐Michael addition in a 3‐CR heteroring‐forming, post‐cyclization transformation followed by an intramolecular fused‐heterocycles formation process.
Giacomo Mari +4 more
wiley +1 more source

