112136-00-2Relevant academic research and scientific papers
BIOISPIRED PROTEASOME ACTIVATORS WITH ANTIAGEING ACTIVITY
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, (2019/10/01)
The present invention relates to novel bio-inspired hybrid compounds of formula I which act as proteasome activators and exhibit anti-ageing activity, as well as methods for their synthesis. These hybrid compounds combine the structural features of hydroxytyrosol and the natural antioxidant vitamin E or its bioisosteres in one molecular scaffold. The compounds of formula I, which include structural proteasome activators (activation by stereochemical interaction), can be used in the production of anti-ageing products, such as cosmetic preparations. Additionally, they can be used in conditions and diseases where the proteasome is down-regulated, as well as proteasome-activation control compounds.
A straightforward hetero-diels-alder approach to (2-ambo,4′R, 8′R)-α/β/γ/δ-4-thiatocopherol
Menichetti, Stefano,Amorati, Riccardo,Bartolozzi, Maria Grazia,Pedulli, Gian Franco,Salvini, Antonella,Viglianisi, Caterina
supporting information; experimental part, p. 2218 - 2225 (2010/07/03)
A simple and original inverse electron demand hetero-Diels-Alder reaction has been successfully applied to the synthesis of (2-ambo,4′R,8′R)- α/β/γ/δ-4-thiatocopherol. Commercially available methyl hydroquinones and. (2E,7R,11R)-(+)-phytol were exploited for the preparation of the ortho-thioquinones, acting as electron-poor dienes, and of the proper 1,3-diene used as dienophile, respectively. The benzoxathiine cycloadducts, with the required tocopherol-like skeleton, were obtained with complete control, of regio and chemoselectivity. The antioxidant activity of 4-thiatocopherols was measured and rationalized in comparison with that of the corresponding natural components of Vitamin E.
[3H,7H]thiazole[3,4-a]pyridines having antiasthmatic and antiinflammatory activities on the respiratory tract
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, (2008/06/13)
STR1 Compounds of formula (I), having antiasthmatic and antiinflammatory actions on the respiratory tract, processes for the preparation thereof and pharmaceutical compositions containing them.
Studies on hindered phenols and analogues. 1. Hypolipidemic and hypoglycemic agents with ability to inhibit lipid peroxidation
Yoshioka,Fujita,Kanai,Aizawa,Kurumada,Hasegawa,Horikoshi
, p. 421 - 428 (2007/10/02)
A series of hindered phenols were investigated as hypolipidemic and/or hypoglycemic agents with ability to inhibit lipid peroxidation. 1,3-Benzoxathioles (9 and 22), phenoxypentanoic acid (34), phenoxypentanol (35a), phenoxynonanol (35b), phenylchloropropionic acid having a chromanyl group (25), and a thiazolidine compound (27) derived from 25, all having a hindered phenol group, were prepared and examined. Compound 27 showed the expected biological properties in vivo and in vitro without any liver weight increase. Biological activities of the analogous thiazolidine compounds, 43-58, were compared. Thus, roxy-2,5,7,8-tetramethylchroman-2-yl(methoxy]-benzyl]-2,4-thiazolidinedione (27) (CS-045) was found to have all our expected properties and was selected as a candidate for further development as a hypoglycemic and hypolipidemic agent.
