Untersuchungen zur Eiweißbindung von Arzneistoffen durch kontinuierliche Ultrafiltration, 3. Mitt.⁵⁾ Eiweißbindung von blutgerinnungshemmenden Tetronsäuren

Abstract

Die EiweiSbindung von funf blutgerinnungshemmenden Tetronsauren an menschliches Serumalbumin wurde durch kontinuierliche Ultrafiltration bestimmt. Die wirkungsstarksten Substanzen zeigten auch die starkste EiweiSbindung, wobei 5 in der GroSenordnung von Phenprocoumon gebunden wird. Trotz der starken Proteinbindung zeigen die Tetronsauren raschen Wirkungseintritt und relative kurze Wirkungsdauer.

Synthesis of New and Highly Functionalized 1,4‐Dihydropyridines and Spirooxindole Dihydropyridines Using L‐Proline as Efficient Catalyst

“…[20,21] Due to some features of these compounds such as antibiotic, HIV-1 protease inhibitors, antiepileptic, anticoagulant, antibacterial, antifungal, analgesic, anti-inflammatory, and anticancer, could be considered as interesting templates for medicinal chemistry. [22][23][24][25][26][27] Regarded to mentioned significances, an efficient procedure for the synthesis of 1,4-DHP derivatives containing tetronic acid moiety was presented through a three-component reaction.…”

“…Among the dicarbonyl compounds, tetronic acid can be mentioned as a structural moiety in some of the natural compounds such as muconolactones, acetogenins, strigol and leptosfaerin . Due to some features of these compounds such as antibiotic, HIV‐1 protease inhibitors, antiepileptic, anticoagulant, antibacterial, antifungal, analgesic, anti‐inflammatory, and anticancer, could be considered as interesting templates for medicinal chemistry . Regarded to mentioned significances, an efficient procedure for the synthesis of 1,4‐DHP derivatives containing tetronic acid moiety was presented through a three‐component reaction.…”

Microwave-assisted multi-component reaction in water leading to highly regioselective formation of benzo[f]azulen-1-ones

“…1h-i In addition, some of these compounds also possess bioactivities on analgesic, sedative ans antidepressive as well as hypnotic activities. 2 On the other hand, the derivatives of tetronic acid (tetrahydrofuran-2,4-dione) play an essential role in medicinal chemistry 3 by serving as HIV-1 protease inhibiting 4 , anti-inflammatory, 5 antifungal, 6 antibiotic, 7 insecticidal, 8 analgesic, 9 anticoagulant 10 and antiepileptic 11 agents. Consequently, benzoazulen-1-one derivatives containing both benzodiazepine and tetronic acid motifs would provide novel leading structures for combinatorial drug-discovery research.…”