Molecules, Vol. 28, Pages 5479: Synthesis, Biological, Spectroscopic and Computational Investigations of Novel N-Acylhydrazone Derivatives of Pyrrolo[3,4-d]pyridazinone as Dual COX/LOX Inhibitors
Molecules, Vol. 28, Pages 5479: Synthesis, Biological, Spectroscopic and Computational Investigations of Novel N-Acylhydrazone Derivatives of Pyrrolo[3,4-d]pyridazinone as Dual COX/LOX Inhibitors
Molecules doi: 10.3390/molecules28145479
Authors:
Jakub Mikus
Piotr Świątek
Patrycja Przybyła
Edward Krzyżak
Aleksandra Marciniak
Aleksadra Kotynia
Aleksandra Redzicka
Benita Wiatrak
Paulina Jawień
Tomasz Gębarowski
Łukasz Szczukowski
Secure and efficient treatment of diverse pain and inflammatory disorders is continually challenging. Although NSAIDs and other painkillers are well-known and commonly available, they are sometimes insufficient and can cause dangerous adverse effects. As yet reported, derivatives of pyrrolo[3,4-d]pyridazinone are potent COX-2 inhibitors with a COX-2/COX-1 selectivity index better than meloxicam. Considering that N-acylhydrazone (NAH) moiety is a privileged structure occurring in many promising drug candidates, we decided to introduce this pharmacophore into new series of pyrrolo[3,4-d]pyridazinone derivatives. The current paper presents the synthesis and in vitro, spectroscopic, and in silico studies evaluating the biological and physicochemical properties of NAH derivatives of pyrrolo[3,4-d]pyridazinone. Novel compounds 5a-c–7a-c were received with high purity and good yields and did not show cytotoxicity in the MTT assay. Their COX-1, COX-2, and 15-LOX inhibitory activities were estimated using enzymati...
Source: Molecules - Category: Chemistry Authors: Jakub Mikus Piotr Świątek Patrycja Przyby ła Edward Krzy żak Aleksandra Marciniak Aleksadra Kotynia Aleksandra Redzicka Benita Wiatrak Paulina Jawie ń Tomasz G ębarowski Łukasz Szczukowski Tags: Article Source Type: research