Activity and Quantitative Structure Activity Analysis of ƒ ¿ - Isopropyl - α - [ 3 - [ 3 - ( 3 - methoxyphenoxy ) propylamino ] propyl ] - α - phenylacetonitrile
نویسندگان
چکیده
prepared, and their Ca2+ -antagonistic activity was evaluated. Among these compounds, the N-Me derivatives with m-OMe, p-F, p-Cl, 3,4-(OM4 and 3,5-(OMe)2 substituents on the A ring were found to show higher Ca2+ -antagonistic activity than verapamil . The effect of substituents on the A ring was examined quantitatively using physicochemical substituent parameters and regression analysis. The analysis showed that substituents with a n value close to zero are favorable to the activity and that optimum steric conditions exist for mand p-substituents, corresponding to those of m-OMe and p-F or p-Cl. The analysis for the whole series of analogs where substituents on the A ring, the benzene ring (B ring) at the phenoxy moiety and the quaternary carbon atom are simultaneously varied suggested that there is an optimum molecular hydrophobicity , perhaps participating in the transport process to the site of action, besides position-specific steric and hydrophobic effects.
منابع مشابه
Synthesis and Cytotoxicity Evaluation of C4‐ and C5‐Modified Analogues of the α,β‐Unsaturated Lactone of Pironetin
Pironetin is a natural product with potent antiproliferative activity that forms a covalent adduct with α-tubulin via conjugate addition into the natural product's α,β-unsaturated lactone. Although pironetin's α,β-unsaturated lactone is involved in its binding to tubulin, the structure-activity relationship at different positions of the lactone have not been thoroughly evaluated. For a systemat...
متن کاملSynthesis and Biological Evaluation of 2-Hydroxy-3-[(2-aryloxyethyl)amino]propyl 4-[(Alkoxycarbonyl)amino]benzoates
A series of twenty substituted 2-hydroxy-3-[(2-aryloxyethyl)amino]propyl 4-[(alkoxycarbonyl)amino]benzoates were prepared and characterized. As similar compounds have been described as potential antimycobacterials, primary in vitro screening of the synthesized carbamates was also performed against two mycobacterial species. 2-Hydroxy-3-[2-(2,6-dimethoxyphenoxy)ethylamino]-propyl 4-(butoxycarbon...
متن کاملEnhanced Phtocatalytic Activity of α-Fe2O3 Nanoparticles Using 2D MoS2 Nanosheets
α‒Fe2O3/MoS2 nanocomposites were synthesized via hydrothermal method and characterized in terms of crystal structure, particle size and morphology, elemental purity and optical properties. Results confirmed the formation of α‒Fe2O3/MoS2 nanocomposites containing hematite nanoparticles with average diameter of 40 nm and MoS2 nanosheets with hexagonal crystal structure and sheet thickness o...
متن کاملConvenient synthesis of 4-thiolactose, 3,4-dithiolactose and related thiooligosaccharides and disulfides. Inhibitory activity of the glycomimetics against a β-galactosidase.
The ring-opening reaction of sugar 3,4-epoxides by 2,3,4,6-tetra-O-acetyl-1-thio-β-D-galactopyranose (7) as a nucleophile led to (1 → 3)- and (1 → 4)-thiodisaccharides. High regio- and diastereoselectivities were achieved in the synthesis of the per-O-acetyl derivative of the β-D-Galp-S-(1 → 4)-4-thio-α-D-Glcp-O-iPr (10). Analogues of the 4-thiolactoside 10 have been prepared, with the β-D-Galp...
متن کاملEvaluation of Novel α-(Acyloxy)-α-(Quinolin-4-yl) Acetamides as Antiplasmodial Agents
Because of expanding resistance to efficient and affordable antimalarial drugs likechloroquine, the search is continuing for more effective drugs against this disease. In-vitroantiplasmodial activity and cytotoxicity of α-(acyloxy)-α-(quinolin-4-yl) acetamides onPlasmodium falciparum and structure-activity relationships of this new class of Passeriniadducts is described. The in-vitro antiplasmo...
متن کامل