Characterization of the Oral Absorption of Some β-Lactams Effect of the α-Amino Side Chain Group

1993 ◽  
Vol 82 (9) ◽  
pp. 897-900 ◽  
Author(s):  
Doo‐Man oh ◽  
Patrick J. Sinko ◽  
Gordon L. Amidon
Keyword(s):  
Oral Absorption ◽  
Side Chain ◽  
Chain Group

Implicit Side-Chain Model and Experimental Characterization of Bottlebrush Block Copolymer Solution Assembly

2021 ◽  
Author(s):  
Tianyuan Pan ◽  
Bijal B. Patel ◽  
Dylan J. Walsh ◽  
Sarit Dutta ◽  
Damien Guironnet ◽  
...  
Keyword(s):  
Block Copolymer ◽  
Side Chain ◽  
Chain Model ◽  
Experimental Characterization ◽  
Copolymer Solution

Characterization of the Side Chain Steric Structures in the Various Lignins

Holzforschung ◽  
1989 ◽  
Vol 43 (3) ◽  
pp. 187-190 ◽  
Author(s):  
H. Taneda ◽  
N. Habu ◽  
J. Nakano
Keyword(s):  
Side Chain

Characterization of squalene epoxidase activity from the dermatophyte Trichophyton rubrum and its inhibition by terbinafine and other antimycotic agents.

1996 ◽  
Vol 40 (2) ◽  
pp. 443-447 ◽  
Author(s):  
B Favre ◽  
N S Ryder
Keyword(s):  
Biochemical Characterization ◽  
Trichophyton Rubrum ◽  
Side Chain ◽  
Ergosterol Biosynthesis ◽  
Squalene Epoxidase ◽  
High Potency ◽  
Whole Cells ◽  
Absolute Requirement ◽  
Tertiary Amino

Squalene epoxidase (SE) is the primary target of the allylamine antimycotic agents terbinafine and naftifine and also of the thiocarbamates. Although all of these drugs are employed primarily in dermatological therapy, SE from dermatophyte fungi has not been previously investigated. We report here the biochemical characterization of SE activity from Trichophyton rubrum and the effects of terbinafine and other inhibitors. Microsomal SE activity from T. rubrum was not dependent on soluble cytoplasmic factors but had an absolute requirement for NADPH or NADH and was stimulated by flavin adenine dinucleotide. Kinetic analyses revealed that under optimal conditions the Km for squalene was 13 microM and its Vmax was 0.71 nmol/h/mg of protein. Terbinafine was the most potent inhibitor tested, with a 50% inhibitory concentration (IC50) of 15.8 nM. This inhibition was noncompetitive with regard to the substrate squalene. A structure-activity relationship study with some analogs of terbinafine indicated that the tertiary amino structure of terbinafine was crucial for its high potency, as well as the tert-alkyl side chain. Naftifine had a lower potency (IC50, 114.6 nM) than terbinafine. Inhibition was also demonstrated by the thiocarbamates tolciclate (IC50, 28.0 nM) and tolnaftate (IC50, 51.5 nM). Interestingly, the morpholine amorolfine also displayed a weak but significant effect (IC50, 30 microM). T. rubrum SE was only slightly more sensitive (approximately twofold) to terbinafine inhibition than was the Candida albicans enzyme. Therefore, this difference cannot fully explain the much higher susceptibility (> or = 100-fold) of dermatophytes than of yeasts to this drug. The sensitivity to terbinafine of ergosterol biosynthesis in whole cells of T. rubrum (IC50, 1.5 nM) is 10-fold higher than that of SE activity, suggesting that the drug accumulates in the fungus.

Synthesis and Characterization of a Regioregular Side‐Chain Semifluorinated Polythiophene

2019 ◽  
Vol 216 (12) ◽  
pp. 1800747 ◽  
Author(s):  
Christoph Horn ◽  
Doris Pospiech ◽  
Johanna Zessin ◽  
Sebastian Stein ◽  
Dieter Jehnichen ◽  
...  
Keyword(s):  
Side Chain ◽  
Synthesis And Characterization
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