Synthesis and biological evaluation of novel pyrazoline derivatives as potent anti-inflammatory agents. 2015

Jiqiang He, and Liang Ma, and Zhe Wei, and Jun Zhu, and Fei Peng, and Mingfeng Shao, and Lei Lei, and Lin He, and Minghai Tang, and Linhong He, and Yuzhe Wu, and Lijuan Chen
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu 610041, China.

Twenty-eight pyrazoline derivatives, which originated from pyranochalcones, have been synthesized and evaluated for their inhibitory potency on the production of inflammatory mediator nitric oxide (NO) in LPS-stimulated RAW 264.7 cells. Among them, three compounds (1c, 11c, and 15c) exhibited potent inhibitory effects on NO production and iNOS activity superior to positive control Indomethacin, with 1c being most efficacious. Furthermore, 1c could suppress the progress of carrageenan-induced hind paw edema at a dosage of 50 mg/kg/day and dose-dependently ameliorate the development of adjuvant-induced arthritis (AIA). Docking study confirmed that 1c was an iNOS inhibitor with good binding into the active site of murine iNOS.

UI MeSH Term Description Entries
D007249 Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function. Innate Inflammatory Response,Inflammations,Inflammatory Response, Innate,Innate Inflammatory Responses
D008070 Lipopolysaccharides Lipid-containing polysaccharides which are endotoxins and important group-specific antigens. They are often derived from the cell wall of gram-negative bacteria and induce immunoglobulin secretion. The lipopolysaccharide molecule consists of three parts: LIPID A, core polysaccharide, and O-specific chains (O ANTIGENS). When derived from Escherichia coli, lipopolysaccharides serve as polyclonal B-cell mitogens commonly used in laboratory immunology. (From Dorland, 28th ed) Lipopolysaccharide,Lipoglycans
D008264 Macrophages The relatively long-lived phagocytic cell of mammalian tissues that are derived from blood MONOCYTES. Main types are PERITONEAL MACROPHAGES; ALVEOLAR MACROPHAGES; HISTIOCYTES; KUPFFER CELLS of the liver; and OSTEOCLASTS. They may further differentiate within chronic inflammatory lesions to EPITHELIOID CELLS or may fuse to form FOREIGN BODY GIANT CELLS or LANGHANS GIANT CELLS. (from The Dictionary of Cell Biology, Lackie and Dow, 3rd ed.) Bone Marrow-Derived Macrophages,Monocyte-Derived Macrophages,Macrophage,Macrophages, Monocyte-Derived,Bone Marrow Derived Macrophages,Bone Marrow-Derived Macrophage,Macrophage, Bone Marrow-Derived,Macrophage, Monocyte-Derived,Macrophages, Bone Marrow-Derived,Macrophages, Monocyte Derived,Monocyte Derived Macrophages,Monocyte-Derived Macrophage
D008813 Mice, Inbred ICR An inbred strain of mouse that is used as a general purpose research strain, for therapeutic drug testing, and for the genetic analysis of CARCINOGEN-induced COLON CANCER. Mice, Inbred ICRC,Mice, ICR,Mouse, ICR,Mouse, Inbred ICR,Mouse, Inbred ICRC,ICR Mice,ICR Mice, Inbred,ICR Mouse,ICR Mouse, Inbred,ICRC Mice, Inbred,ICRC Mouse, Inbred,Inbred ICR Mice,Inbred ICR Mouse,Inbred ICRC Mice,Inbred ICRC Mouse
D008958 Models, Molecular Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures. Molecular Models,Model, Molecular,Molecular Model
D002351 Carrageenan A water-soluble extractive mixture of sulfated polysaccharides from RED ALGAE. Chief sources are the Irish moss CHONDRUS CRISPUS (Carrageen), and Gigartina stellata. It is used as a stabilizer, for suspending COCOA in chocolate manufacture, and to clarify BEVERAGES. Carrageenin,iota-Carrageenan,kappa-Carrageenan,lambda-Carrageenan,iota Carrageenan,kappa Carrageenan,lambda Carrageenan
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000893 Anti-Inflammatory Agents Substances that reduce or suppress INFLAMMATION. Anti-Inflammatory Agent,Antiinflammatory Agent,Agents, Anti-Inflammatory,Agents, Antiinflammatory,Anti-Inflammatories,Antiinflammatories,Antiinflammatory Agents,Agent, Anti-Inflammatory,Agent, Antiinflammatory,Agents, Anti Inflammatory,Anti Inflammatories,Anti Inflammatory Agent,Anti Inflammatory Agents
D001168 Arthritis Acute or chronic inflammation of JOINTS. Oligoarthritis,Polyarthritis,Arthritides,Oligoarthritides,Polyarthritides

Related Publications

Jiqiang He, and Liang Ma, and Zhe Wei, and Jun Zhu, and Fei Peng, and Mingfeng Shao, and Lei Lei, and Lin He, and Minghai Tang, and Linhong He, and Yuzhe Wu, and Lijuan Chen
June 2012, Archives of pharmacal research,
Jiqiang He, and Liang Ma, and Zhe Wei, and Jun Zhu, and Fei Peng, and Mingfeng Shao, and Lei Lei, and Lin He, and Minghai Tang, and Linhong He, and Yuzhe Wu, and Lijuan Chen
December 2014, Bioorganic & medicinal chemistry letters,
Jiqiang He, and Liang Ma, and Zhe Wei, and Jun Zhu, and Fei Peng, and Mingfeng Shao, and Lei Lei, and Lin He, and Minghai Tang, and Linhong He, and Yuzhe Wu, and Lijuan Chen
June 2013, Drug research,
Jiqiang He, and Liang Ma, and Zhe Wei, and Jun Zhu, and Fei Peng, and Mingfeng Shao, and Lei Lei, and Lin He, and Minghai Tang, and Linhong He, and Yuzhe Wu, and Lijuan Chen
January 2014, Medicinal chemistry (Shariqah (United Arab Emirates)),
Jiqiang He, and Liang Ma, and Zhe Wei, and Jun Zhu, and Fei Peng, and Mingfeng Shao, and Lei Lei, and Lin He, and Minghai Tang, and Linhong He, and Yuzhe Wu, and Lijuan Chen
April 2012, European journal of medicinal chemistry,
Jiqiang He, and Liang Ma, and Zhe Wei, and Jun Zhu, and Fei Peng, and Mingfeng Shao, and Lei Lei, and Lin He, and Minghai Tang, and Linhong He, and Yuzhe Wu, and Lijuan Chen
February 2008, Bioorganic & medicinal chemistry letters,
Jiqiang He, and Liang Ma, and Zhe Wei, and Jun Zhu, and Fei Peng, and Mingfeng Shao, and Lei Lei, and Lin He, and Minghai Tang, and Linhong He, and Yuzhe Wu, and Lijuan Chen
June 2016, Chemical & pharmaceutical bulletin,
Jiqiang He, and Liang Ma, and Zhe Wei, and Jun Zhu, and Fei Peng, and Mingfeng Shao, and Lei Lei, and Lin He, and Minghai Tang, and Linhong He, and Yuzhe Wu, and Lijuan Chen
March 2009, Medicinal chemistry (Shariqah (United Arab Emirates)),
Jiqiang He, and Liang Ma, and Zhe Wei, and Jun Zhu, and Fei Peng, and Mingfeng Shao, and Lei Lei, and Lin He, and Minghai Tang, and Linhong He, and Yuzhe Wu, and Lijuan Chen
June 2013, European journal of medicinal chemistry,
Jiqiang He, and Liang Ma, and Zhe Wei, and Jun Zhu, and Fei Peng, and Mingfeng Shao, and Lei Lei, and Lin He, and Minghai Tang, and Linhong He, and Yuzhe Wu, and Lijuan Chen
June 2023, International journal of molecular sciences,
Copied contents to your clipboard!