Bioorganic & medicinal chemistry

Substituted 1, 2, 3, 4-tetrahydroquinolin-6-yloxypropanes as β 3-adrenergic receptor agonists: Design, synthesis, biological evaluation and pharmacophore modeling

N Shakya, KK Roy, AK Saxena

Index: Shakya, Neeraj; Roy, Kuldeep K.; Saxena, Anil K. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 2 p. 830 - 847

Full Text: HTML

Citation Number: 21

Abstract

In search of potent β3-adrenergic receptor agonists, a series of novel substituted 1, 2, 3, 4- tetrahydroquinolin-6-yloxypropanes has been synthesized and evaluated for their β3- adrenergic receptor agonistic activity (ranging from− 17.73% to 90.64% inhibition at 10μM) using well established Human SK-N-MC neuroblastoma cells model. Four molecules viz. 11, 15, 22 and 23 showed β3-AR agonistic IC50 value of 0.55, 0.59, 1.18 and 1.76 μM, ...

Related Articles:

A novel and efficient catalytic epoxidation of olefins and monoterpenes with microencapsulated Lewis base adducts of methyltrioxorhenium

[Tetrahedron, , vol. 61, # 5 p. 1069 - 1075]

(N, N-Diisopropylcarbamoyloxy)-methyl p-tolyl sulfone: preparation and application for the syntheses of 1, 2-diols

[Ma, Lu; Zhao, Dongmei; Chen, Lin; Wang, Xin; Chen, Yue-Lei; Shen, Jingkang Tetrahedron, 2012 , vol. 68, # 42 p. 8704 - 8711]

One-pot synthesis of enantiomerically pure 1, 2-diols: asymmetric reduction of aromatic α-oxoaldehydes catalysed by Candida parapsilosis ATCC 7330

[Mahajabeen, Pula; Chadha, Anju Tetrahedron Asymmetry, 2011 , vol. 22, # 24 p. 2156 - 2160]

Synthesis, characterization, catalytic and antiamoebic activity of vanadium complexes of binucleating bis (dibasic tridentate ONS donor) ligand systems

[European Journal of Inorganic Chemistry, , # 15 p. 2560 - 2577]

Mn (III) complexes of the monoprotic tridentate ONN donor 2-[2-(1H-(benzo [d] imidazol-2-yl) ethylimino) methyl] phenol as a functional mimic of haloperoxidase

[Polyhedron, , vol. 46, # 1 p. 33 - 40]

More Articles...