The copper-catalyzed multicomponent cyclization reaction, which combined aldehydes, hydrazines, and alkynylesters, was applied in the synthesis of pyridazinones. The reaction was regioselective and gave only six-membered pyridazinones in the complete absence of five-membered pyrazoles or a regioisomeric mixture. During this investigation, the use of 2-halobenzaldehyde as the starting material, under identical reaction conditions, gave 6-(2-ethoxyphenyl)pyridazinones after sequential Michael addition/1,2-addition/Ullmann cross-coupling reactions.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1002/chem.201403873 | DOI Listing |
Bioorg Chem
January 2025
Chemistry Department, Faculty of Science, Ain Shams University, Cairo 11566, Egypt. Electronic address:
A new series of benzo[h]quinoline-containing heterocycles was synthesized via reactions of benzo[h]quinolinyl-2(3H)-furanone with some nitrogen bidentate nucleophiles, leading to the formation of pyridazinone, pyrrolinone, benzimidazole, and benzoxazinone derivatives. The synthesized compounds were evaluated for their insecticidal activity against Culex pipiens L. larvae.
View Article and Find Full Text PDFSci Rep
November 2024
Pharmaceutical organic chemistry department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
People of all age categories and lifestyles suffer to different extents from hypertension. Accordingly, this necessitates the rise of new ways to defeat this enemy. Vasodilators exert a principal portion of highly effectual antihypertensive agents; our research is focused on the design, synthesis and biological evaluation of a new series of 6-(4-substitutedphenyl)-3-pyridazinones as potential hydralazine vasodilator analogues implementing both in vitro and in silico approaches.
View Article and Find Full Text PDFSci Rep
October 2024
Department of Chemistry, Faculty of Science, Ain Shams University, Abbassia, Cairo, 11566, Egypt.
As a result of its high reactivity, furan-2(3H)-one derivative 2 can be selected as a versatile and suitable candidate for building of novel nitrogen heterocyclic compounds. Consequently, furan-2(3H)-one derivative 2 and some nitrogen nucleophiles were utilized as starting materials for the formation of new pyridazinone and pyrrolone derivatives bearing naphthalene moiety. The continuous buildup of insecticide resistance is the main obstacle facing pest control measures.
View Article and Find Full Text PDFRSC Med Chem
August 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams University Abbassia Cairo 11566 Egypt
Cancer patients undergoing chemotherapy are highly susceptible to infections owing to their compromised immune system, which also promotes cancer progression through inflammation. Thus, this study aimed to develop novel chemotherapeutic agents with both anticancer and antimicrobial properties. A series of diarylurea derivatives based on pyridazinone scaffolds were designed, synthesized, and characterized as surrogates for sorafenib.
View Article and Find Full Text PDFEur J Med Chem
November 2024
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China. Electronic address:
Pyridazinone derivatives have been extensively used as anticancer agents. IMB5036 is a structure specific pyridazinone compound with potential antitumor activity via targeting KSRP protein which controls gene expression at multiple levels. In this study, fifteen IMB5036 analogues were synthesized and preliminary structure-activity relationships were explored.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!