2,5,6-trisubstituted imidazo[2,1-b][1,3,4]thiadiazoles: search for antihyperlipidemic agents.
作者： Harun M. Patel , Malleshappa N. Noolvi , Anjali Goyal , B.S. Thippeswamy
DOI: 10.1016/J.EJMECH.2013.04.020
关键词:
摘要: Abstract A novel series of 2,5,6-trisubstituted imidazo[2,1- b ][1,3,4]thiadiazoles 4 ( a – d ) and 7 i were rationally designed through QSAR based pharmacophore approach synthesized from 5-(1,3-benzodioxol-5-yl)-[1,3,4]thiadiazol-2-amine 1 ). The structures these compounds established by IR, H NMR, 13 C HRMS technique. All the evaluated for their in vitro antihyperlipidemic activity using trition induced hyperlipidemic model. newly title compound 7d , 7e 7h showed significant decrease in serum, TCH, TG LDL VLDL values along with an increase serum HDL levels as compared to standard drug Fenofibrate. treated groups also atherogenic index, LDL:HDL risk ratios level SGOT, SGPT ALP activities cholesterol control group.
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John D. Bancroft, Marilyn Gamble, Theory and Practice of Histological Techniques ,(1990)
Hans Ulrich Bergmeyer, Methods of Enzymatic Analysis ,(1963)
Albert Zlatkis, Albert Zlatkis, Albert J. Boyle, Albert J. Boyle, Bennie Zak, Bennie Zak, A new method for the direct determination of serum cholesterol. Journal of Laboratory and Clinical Medicine. ,vol. 41, pp. 486- 492 ,(1953) , 10.5555/URI:PII:0022214353901255
Andanappa K Gadad, Chanabasappa S Mahajanshetti, Sudarshan Nimbalkar, Anandkumar Raichurkar, Synthesis and antibacterial activity of some 5-guanylhydrazone/thiocyanato-6-arylimidazo[2,1-b]-1,3, 4-thiadiazole-2-sulfonamide derivatives. European Journal of Medicinal Chemistry. ,vol. 35, pp. 853- 857 ,(2000) , 10.1016/S0223-5234(00)00166-5
Lisa Shewchuk, Anne Hassell, Bruce Wisely, Warren Rocque, William Holmes, James Veal, Lee F. Kuyper, Binding mode of the 4-anilinoquinazoline class of protein kinase inhibitor: X-ray crystallographic studies of 4-anilinoquinazolines bound to cyclin-dependent kinase 2 and p38 kinase. Journal of Medicinal Chemistry. ,vol. 43, pp. 133- 138 ,(2000) , 10.1021/JM990401T
GuoGang Tu, ShaoHua Li, HuiMing Huang, Gang Li, Fang Xiong, Xi Mai, HuaWei Zhu, BinHai Kuang, Wen Fang Xu, Novel aminopeptidase N inhibitors derived from 1,3,4-thiadiazole scaffold. Bioorganic & Medicinal Chemistry. ,vol. 16, pp. 6663- 6668 ,(2008) , 10.1016/J.BMC.2008.05.081
Haregewein Assefa, Shantaram Kamath, John K. Buolamwini, 3D-QSAR and docking studies on 4-anilinoquinazoline and 4-anilinoquinoline epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors Journal of Computer-Aided Molecular Design. ,vol. 17, pp. 475- 493 ,(2003) , 10.1023/B:JCAM.0000004622.13865.4F
Hicham Harnafi, Nour el Houda Bouanani, Mohammed Aziz, Hana Serghini Caid, Noreddine Ghalim, Souliman Amrani, The hypolipidaemic activity of aqueous Erica multiflora flowers extract in Triton WR-1339 induced hyperlipidaemic rats: a comparison with fenofibrate. Journal of Ethnopharmacology. ,vol. 109, pp. 156- 160 ,(2007) , 10.1016/J.JEP.2006.09.017
Andanappa K. Gadad, Malleshappa N. Noolvi, Rajshekhar V. Karpoormath, Synthesis and anti-tubercular activity of a series of 2-sulfonamido/trifluoromethyl-6-substituted imidazo[2,1-b]-1,3,4-thiadiazole derivatives. Bioorganic & Medicinal Chemistry. ,vol. 12, pp. 5651- 5659 ,(2004) , 10.1016/J.BMC.2004.07.060
Gundurao Kolavi, Vinayak Hegde, Imtiyaz ahmed Khazi, Pramod Gadad, Synthesis and evaluation of antitubercular activity of imidazo[2,1-b][1,3,4]thiadiazole derivatives Bioorganic & Medicinal Chemistry. ,vol. 14, pp. 3069- 3080 ,(2006) , 10.1016/J.BMC.2005.12.020