Results 31 to 40 of about 130,911 (332)
Correlation between the lipophilicity and antifungal activity of some benzoxazole derivatives [PDF]
In the present work, a quantitative relationship between the lipophilicity and antifungal activity of some benzoxazole derivatives against Candida albicans was investigated by using QSAR (quantitative structure-activity relationship) analyses.
Podunavac-Kuzmanović Sanja O. +1 more
doaj +1 more source
Providing the ‘Best’ Lipophilicity Assessment in a Drug Discovery Environment
Lipophilicity is a fundamental structural property that influences almost every aspect of drug discovery. Within Pfizer, we have two complementary high-throughput screens for measuring lipophilicity as a distribution coefficient (LogD) – a miniaturized ...
Nathaniel, Woody +2 more
core +1 more source
Lipophilicity of morphine microspecies and their contribution to the lipophilicity profile
The complete set of experimental microscopic partition coefficients of morphine was determined for the first time for any compound. The acid-base microequilibria were characterized by combining pH-potentiometry and deductive methods using auxiliary compounds of reduced complexity.
Károly, Mazák, Béla, Noszál
openaire +2 more sources
In this study, eco-friendly microwave-assisted esterification reactions of chenodeoxycholic acid with medium-chain diols (1,2-ethanediol, 1,4-butanediol, 1,6-hexanediol, 1,8-octanediol, and 1,10-decanediol) or tetraethylene glycol were accomplished. The
Ksenija Pavlović +6 more
doaj +1 more source
Drug-like properties in macrocycles above MW 1000: Backbone rigidity vs. side-chain lipophilicity
Large, macrocyclic peptides can achieve surprisingly high membrane permeability, although the properties that govern permeability in this chemical space are only beginning to come into focus. We generated two libraries of cyclic decapeptides with stable,
A. Furukawa +9 more
semanticscholar +1 more source
Systematic Investigation of Lipophilicity Modulation by Aliphatic Fluorination Motifs
Optimization of compound lipophilicity is a key aspect of drug discovery. The aim of this work was to compare the lipophilicity modulations induced by 16 distinct known and novel fluoroalkyl motifs on three parent models.
Jérôme Graton +15 more
core +2 more sources
Lipophilicity trends upon fluorination of isopropyl, cyclopropyl and 3-oxetanyl groups
A systematic comparison of lipophilicity modulations upon fluorination of isopropyl, cyclopropyl and 3-oxetanyl substituents, at a single carbon atom, is provided using directly comparable, and easily accessible model compounds.
Benjamin Jeffries +9 more
doaj +1 more source
Sulfonamides are a classic group of chemotherapeutic drugs with a broad spectrum of pharmacological action, including anticancer activity. In this work, reversed-phase high-performance liquid chromatography and biomimetic chromatography were applied to ...
Monika Pastewska +8 more
doaj +1 more source
The subject of the study was 11 new synthetized tetracyclic diazaphenothiazine derivatives. Using thin-layer chromatography in a reverse phase system (RP-TLC), their RM0 lipophilicity parameter was determined.
Anna Nycz–Empel +4 more
doaj +1 more source
Quantitative structure-toxicity relationship study of some natural and synthetic coumarins using retention parameters [PDF]
Four lipophilicity descriptors (RM0, b, C0, PC1) for twelve coumarine derivatives were determined by reversed-phase thin-layer chromatography in order to analyze which descriptor best describes the lipophilicity of coumarines investigated.
Rabtti El Hadi M.A. +7 more
doaj +1 more source

