مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

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Information Journal Paper

Title

DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF 4-BENZAMIDOBENZOIC ACID HYDRAZIDE DERIVATIVES AS NOVEL SOLUBLE EPOXIDE HYDROLASE INHIBITORS

Pages

  51-59

Abstract

 Inhibitors of SOLUBLE EPOXIDE HYDROLASE (sEH) represent one of the novel pharmaceutical approaches for treating hypertension, vascular inflammation, pain and other cardiovascular related diseases. Most of the potent sEH inhibitors reported in literature often suffer from poor solubility and bioavailability. Toward improving pharmacokinetic profile beside favorable potency, two series of 4-benzamidobenzoic acid hydrazide derivatives with hydrazide group as a novel secondary pharmacophore against sEH enzyme were developed. The designed compounds were synthesized in acceptable yield and their in vitro assay was determined. Most of the synthesized compounds have appropriate PHYSICAL PROPERTIES and exhibited considerable in-vitro sEH inhibitory activity in comparison with 12- (3-Adamantan-1-yl-ureido) -dodecanoicacid (AUDA), a potent urea-based sEH inhibitor.4- (2- (4- (4-chlorobenzamido) benzoyl) hydrazinyl) -4-oxobutanoic acid 6c was found to be the most potent inhibitor with inhibitory activity of 72% targeting sEH enzyme.

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    APA: Copy

    REZAEE ZAVAREH, ELHAM, HEDAYATI, MAHDI, HOGHOOGHI RAD, LALEH, SHAHHOSSEINI, SORAYA, FAIZI, MEHRDAD, & TABATABAI, SAYYED ABBAS. (2014). DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF 4-BENZAMIDOBENZOIC ACID HYDRAZIDE DERIVATIVES AS NOVEL SOLUBLE EPOXIDE HYDROLASE INHIBITORS. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 13(SUPPL), 51-59. SID. https://sid.ir/paper/288425/en

    Vancouver: Copy

    REZAEE ZAVAREH ELHAM, HEDAYATI MAHDI, HOGHOOGHI RAD LALEH, SHAHHOSSEINI SORAYA, FAIZI MEHRDAD, TABATABAI SAYYED ABBAS. DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF 4-BENZAMIDOBENZOIC ACID HYDRAZIDE DERIVATIVES AS NOVEL SOLUBLE EPOXIDE HYDROLASE INHIBITORS. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2014;13(SUPPL):51-59. Available from: https://sid.ir/paper/288425/en

    IEEE: Copy

    ELHAM REZAEE ZAVAREH, MAHDI HEDAYATI, LALEH HOGHOOGHI RAD, SORAYA SHAHHOSSEINI, MEHRDAD FAIZI, and SAYYED ABBAS TABATABAI, “DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF 4-BENZAMIDOBENZOIC ACID HYDRAZIDE DERIVATIVES AS NOVEL SOLUBLE EPOXIDE HYDROLASE INHIBITORS,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 13, no. SUPPL, pp. 51–59, 2014, [Online]. Available: https://sid.ir/paper/288425/en

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