نتایج جستجو برای: lipophilicity

تعداد نتایج: 5219  

2013
Gerhard Sandmann Peter Böger

New 2-phenylpyridazinones, analogs o f 4-chloro-5-methylamino-2-phenylpyridazin-3(2H)ones, were assayed for their phytotoxic activity to interfere with plant pigment formation. Six derivatives with — SCF3, — OCF2CH FCF3, — O CH F2, — CN, or — Br in meta position o f the phenyl ring exhibited similar or better bleaching activity than the m -CF3 analog (norflurazon). The activity is predominantly...

Journal: :Molecules 2010
Robert Musiol Josef Jampilek Jacek E Nycz Matus Pesko James Carroll Katarina Kralova Marcela Vejsova Jim O'Mahony Aidan Coffey Anna Mrozek Jaroslaw Polanski

In this study, a series of fourteen ring-substituted 8-hydroxyquinoline derivatives were prepared. The synthesis procedures are presented. The compounds were analyzed using RP-HPLC to determine lipophilicity. They were tested for their activity related to inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the synth...

2002
Peter Liljeroth Bernadette M. Quinn osti Kontturi

A novel method to readily determine the lipophilicity of electrogenerated charged species is reported. This is achieved by local electrolysis at a Pt coated micropipette and, subsequently, driving the electrogenerated species to transfer across the liquid–liquid interface supported at the tip of the micropipette under potential control. The formal potential of ion transfer can then be used to g...

Journal: :European journal of medicinal chemistry 2003
Nellie Gulyaeva Alexander Zaslavsky Pamela Lechner Michael Chlenov Oliver McConnell Arnon Chait Victor Kipnis Boris Zaslavsky

Relative hydrophobicity and lipophilicity of 63 compounds with known permeability through the blood-brain barrier (BBB) was examined by partitioning in aqueous dextran-poly(ethylene glycol) two-phase system and octanol-buffer system, and by gradient RP-HPLC at pH 7.4. Combination of the relative hydrophobicity estimates, N(CH(2)) obtained by aqueous two-phase partitioning and the lipophilicity ...

2017
Peter J. Choi Hamish S. Sutherland Amy S.T. Tong Adrian Blaser Scott G. Franzblau Christopher B. Cooper Manisha U. Lotlikar Anna M. Upton Jerome Guillemont Magali Motte Laurence Queguiner Koen Andries Walter Van den Broeck William A. Denny Brian D. Palmer

Analogues of bedaquiline where the phenyl B-unit was replaced with monocyclic heterocycles of widely differing lipophilicity (thiophenes, furans, pyridines) were synthesised and evaluated. While there was an expected broad positive correlation between lipophilicity and anti-TB activity, the 4-pyridyl derivatives appeared to have an additional contribution to antibacterial potency. The majority ...

Journal: :Molecules 2016
Pavlina Marvanova Tereza Padrtova Klara Odehnalova Ondrej Hosik Michal Oravec Petr Mokry

Nine new dihydrochloride salts of 3-(4-arylpiperazin-1-yl)-2-hydroxypropyl 4-alkoxyethoxybenzoates were designed and synthesized. The physicochemical properties such as lipophilicity index (log kw) and dissociation constant (pKa) were experimentally determined and compared to the software calculated data. The lipophilicity index was determined by means of reversed-phase high performance liquid ...

Journal: :Molecules 2009
Josef Jampilek Robert Musiol Matus Pesko Katarina Kralova Marcela Vejsova James Carroll Aidan Coffey Jacek Finster Dominik Tabak Halina Niedbala Violetta Kozik Jaroslaw Polanski Jozef Csollei Jiri Dohnal

In the study, a series of twelve ring-substituted 4-hydroxy-1H-quinolin-2-one derivatives were prepared. The procedures for synthesis of the compounds are presented. The compounds were analyzed using RP-HPLC to determine lipophilicity and tested for their photosynthesis-inhibiting activity using spinach (Spinacia oleracea L.) chloroplasts. All the synthesized compounds were also evaluated for a...

Journal: :Avicenna journal of medical biochemistry 2023

Background: The skin is the largest organ of body and provides main barrier between internal external environment. Assessment permeability critical importance for understanding predicting in vivo efficacy bioavailability bioactive phenolic compounds. Objectives: This study investigated relationship compounds using silico methods. Methods: Screening was performed on 475 randomly selected Molecul...

Journal: :Current Topics in Medicinal Chemistry 2019

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