Design, synthesis, and biological evaluation of novel 4-hydro-quinoline-3-carboxamide derivatives as an immunomodulator.
A series of novel quinoline-3-carboxamide derivatives were synthesized and evaluated for their immunomodulatory activity. The compounds were tested in vitro for effects on spleen lymphocyte proliferation and TNF-alpha production by macrophage. Three compounds showed immunomodulatory profiles similar to and more potent than those of linomide and FR137316 and were selected for further pharmacological studies in vivo.
He
Jun-Feng
JF
Beijing Institute of Pharmacology and Toxicology, Department of Medicinal Chemistry, 27 Taiping Road, Beijing 100850, China. hjf3770@yahoo.com
Yun
Liu-Hong
LH
Yang
Ri-Fang
RF
Xiao
Zhi-Yong
ZY
Cheng
Jun-Ping
JP
Zhou
Wen-Xia
WX
Zhang
Yong-Xiang
YX
D000818:Animals; D049109:Cell Proliferation / Q000187:drug effects*; D002478:Cells, Cultured; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006912:Hydroxyquinolines / Q000494:pharmacology; D007155:Immunologic Factors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008214:Lymphocytes / Q000187:drug effects / Q000276:immunology; D008264:Macrophages / Q000187:drug effects / Q000276:immunology / Q000378:metabolism*; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013154:Spleen / Q000187:drug effects / Q000276:immunology; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
D006912:Hydroxyquinolines; D007155:Immunologic Factors; D011804:Quinolines; D014409:Tumor Necrosis Factor-alpha; C045282:roquinimex