Novel 3‐Arylamino‐ and 3‐Cycloalkylamino‐5, 6‐diphenyl‐pyridazines Active as ACAT Inhibitors

Abstract

A new series of pyridazine derivatives, structurally related to the previously reported ACAT inhibitors 3-(cyclo)alkylamino-5, 6-diphenyl-pyridazines, were synthesized and tested for their inhibitory properties. Substitution of the 3-alkylamino chain with a phenylamino group maintains activity. In contrast, the presence of either substituents on the phenylamino group or aliphatic rings having more or less than six carbon atoms lowers it.

Mono- or Diphenylpyridazines Connected to N-(2,4-Difluorophenyl)-N‘-heptylurea as Acyl-CoA:Cholesterol Acyltransferase Inhibitors

“…These compounds retained several main features of ACAT inhibitors, such as a long alkyl side chain linked to a heterocycle by a heteroatom of different nature and the o -diphenyl system . To better define the structural requirements of this class, a series of derivatives with different substituents both on the o -diphenyl system and the side-chain were also synthesized. − …”

Synthesis and Antimicrobial Activity of 4-aryl furo Pyridazines

“…Besides they exhibit antiviral activity against the replication of human immunodeficiency virus, inhibit human picornaviruses, protein kinase and acyl coenzyme A: cholesterol acyltransferase. [1][2][3][4][5][6][7][8][9] In recent years , a substantial number of pyridazines have been reported to possess antimicrobial, antitubercular, antifungal, potent analgesic and anti-inflammatory .phosphodiesterase 4 (PDE4) inhibitors are effective anti-inflammatory drugs as potent and selective COX-2 inhibitors , antipyretic activities ,antidiabetic, antifeedant , insecticidal activities , antihypertensive and antiplatelet activities 10 .…”