1147-84-8Relevant academic research and scientific papers
NOVEL BENZAMIDE DERIVATIVE AND USE THEREOF
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, (2014/10/16)
Disclosed are a novel benzamide derivative and pharmaceutical use thereof, and more particularly, a novel benzamide derivative having a structure of Formula 1 or pharmaceutically acceptable salts thereof, and a composition for prevention or treatment of pain or itching including the above material. The novel benzamide derivative and pharmaceutically acceptable salt thereof according to the present invention exhibit excellent pain-suppressive effect and, in particular, pain-suppressive effect in not only a neuropathic animal model but also other models such as a formalin model, and therefore, may be used in suppression of different pains such as nociceptive pain, chronic pain, etc. Further, since it was demonstrated that the present invention displays anti-pruritic efficacy even in an itching model, to which a mechanism and treatment concept established with respect to pain is applied, the present invention may also be effectively used in radical treatment of atopic dermatitis by applying the inventive product to an anti-pruritic composition in order to suppress an initial itching stage and treat symptoms thereof, thus preventing skin damage or inflammation after the scratching stage.
NOVEL BENZAMIDE DERIVATIVE AND USE THEREOF
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, (2014/11/27)
Disclosed are a novel benzamide derivative and pharmaceutical use thereof, and more particularly, a novel benzamide derivative having a structure of Formula 1 or pharmaceutically acceptable salts thereof, and a composition for prevention or treatment of pain or itching including the above material. The novel benzamide derivative and pharmaceutically acceptable salt thereof according to the present invention exhibit excellent pain-suppressive effect and, in particular, pain-suppressive effect in not only a neuropathic animal model but also other models such as a formalin model, and therefore, may be used in suppression of different pains such as nociceptive pain, chronic pain, etc. Further, since it was demonstrated that the present invention displays anti-pruritic efficacy even in an itching model, to which a mechanism and treatment concept established with respect to pain is applied, the present invention may also be effectively used in radical treatment of atopic dermatitis by applying the inventive product to an anti-pruritic composition in order to suppress an initial itching stage and treat symptoms thereof, thus preventing skin damage or inflammation after the scratching stage.
Development of a Novel Series of Trialkoxyaryl Derivatives as Specific and Competitive Antagonists of Platelet Activating Factor
Sawyer, David A.,Beams, Richard M.,Blackwell, Geoffrey, J.,Brockwell, Michael A.,Cheesman, Neil J.,et al.
, p. 2130 - 2137 (2007/10/02)
The synthesis and structure-activity relationship (SAR) analysis of a novel series of trialkoxyaryl derivatives as specific and competetive inhibitors of platelet activating factor (PAF), are described.Molecular modeling comparisons of PAF with the known antagonists Ginkgolide B and L-652731 led to the selection of N-ethyl>-N,N,N-trimethylammonium iodide (1) from the Wellcome registry of compounds and to the synthesis of the lead compound N-oxy>ethyl>-N,N,N-trimethylammonium iodide (3, pKb 5.43).Furth er SAR considerations directed the design to 2-(hexyloxy)-1,3-dimethoxy-5-benzene (38) (pKb 7.14), a novel, specific, and competitive inhibitor of the PAF receptor in rabbit-washed platelets.
