Synthesis of benzimidazole derivatives as antiallergic agents with 5-lipoxygenase inhibiting action.
نویسندگان
چکیده
Syntheses were conducted of novel benzimidazole derivatives that suppress histamine release from mast cells, inhibit 5-lipoxygenase, and possess antioxidative action. Among the compounds synthesized, 1-[2-[2-(4-hydroxy- 2,3,5-trimethylphenoxy)ethoxy]ethyl]-2-(4-methyl-1- homopiperazino)benzimidazole (22) potently suppressed histamine release from rat peritoneal mast cells triggered by the antigen-antibody reaction, inhibited 5-lipoxygenase in rat basophilic leukemia-1 (RBL-1) cells, and prevented the NADPH-dependent lipid peroxidation induced by Fe(3+)-ADP in rat liver microsomes, in addition to an antagonizing the contraction of guinea pig ileum caused by histamine.
منابع مشابه
Design and Synthesis of New Benzimidazole and Pyrimidine Derivatives as α-glucosidase Inhibitor
In an endeavor to find a novel series of antihyperglycemic agents, new benzimidazole and pyrimidine derivatives were successfully synthesized efficiently in high yield with high purity, starting from amino acids in the presence of phosphorus oxychloride (POCl3). The synthesized compounds were identified by 1H-NMR, 13C-NMR, FT-IR spectroscopic techniques and elemental analysis. All products were...
متن کاملDesign and Synthesis of New Benzimidazole and Pyrimidine Derivatives as α-glucosidase Inhibitor
In an endeavor to find a novel series of antihyperglycemic agents, new benzimidazole and pyrimidine derivatives were successfully synthesized efficiently in high yield with high purity, starting from amino acids in the presence of phosphorus oxychloride (POCl3). The synthesized compounds were identified by 1H-NMR, 13C-NMR, FT-IR spectroscopic techniques and elemental analysis. All products were...
متن کاملSynthesis and biological evaluation of N-(5-(pyridin-2-yl)-1,3,4-thiadiazol-2-yl)benzamide derivatives as lipoxygenase inhibitor with potential anticancer activity
In the recent years, the role of LOX enzymes in the cause of neoplastic diseases such as colorectal, skin, pancreatic and renal cancers has been confirmed. A new series of 1,3,4-thiadiazole derivatives bearing 2-pyridyl moiety was synthesized and their cytotoxicity was assessed using MTT protocol. Enzyme inhibitory activity of prepared compounds was also tested against 15-lipoxygenase-1 as nove...
متن کاملSynthesis and biological evaluation of N-(5-(pyridin-2-yl)-1,3,4-thiadiazol-2-yl)benzamide derivatives as lipoxygenase inhibitor with potential anticancer activity
In the recent years, the role of LOX enzymes in the cause of neoplastic diseases such as colorectal, skin, pancreatic and renal cancers has been confirmed. A new series of 1,3,4-thiadiazole derivatives bearing 2-pyridyl moiety was synthesized and their cytotoxicity was assessed using MTT protocol. Enzyme inhibitory activity of prepared compounds was also tested against 15-lipoxygenase-1 as nove...
متن کاملSynthesis of Some 4-Thiazolidinone Derivatives as Antitubercular Agents
Substituted Schiff's bases 2a-o prepared by the treatment of 2-amino-4-(?-methoxyiminocarbomethoxymethyl)-thiazole 1 with different aromatic aldehydes, on cyclocondensation with mercaptoaceticacid and mercaptopropionicacid in dry benzene furnished desired thiazolidinones of type 3a-o and 4a-j, respectively. The structure of the compounds have been assigned on the basis of elemental analyses and...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Chemical & pharmaceutical bulletin
دوره 47 11 شماره
صفحات -
تاریخ انتشار 1999