Transporter-Mediated Drug–Drug Interactions Involving OATP Substrates: Predictions Based on In Vitro Inhibition Studies

2012 ◽  
Vol 91 (6) ◽  
pp. 1053-1064 ◽  
Author(s):  
K Yoshida ◽  
K Maeda ◽  
Y Sugiyama
Keyword(s):  
Drug Interactions ◽  
In Vitro Inhibition ◽  
Inhibition Studies

scholarly journals Application of Static Modeling ­­in the Prediction of In Vivo Drug–Drug Interactions between Rivaroxaban and Antiarrhythmic Agents Based on In Vitro Inhibition Studies

2017 ◽  
Vol 45 (3) ◽  
pp. 260-268 ◽  
Author(s):  
Eleanor Jing Yi Cheong ◽  
Janice Jia Ni Goh ◽  
Yanjun Hong ◽  
Gopalakrishnan Venkatesan ◽  
Yuanjie Liu ◽  
...  
Keyword(s):  
Drug Interactions ◽  
Antiarrhythmic Agents ◽  
Static Modeling ◽  
In Vitro Inhibition ◽  
Inhibition Studies

scholarly journals In vitro inhibition of human CYP2D6 by the chiral pesticide fipronil and its metabolite fipronil sulfone: Prediction of pesticide-drug interactions

2019 ◽  
Vol 313 ◽  
pp. 196-204 ◽  
Author(s):  
Daniel Blascke Carrão ◽  
Maísa Daniela Habenchus ◽  
Nayara Cristina Perez de Albuquerque ◽  
Rodrigo Moreira da Silva ◽  
Norberto Peporine Lopes ◽  
...  
Keyword(s):  
Drug Interactions ◽  
In Vitro Inhibition

SAR directed design and synthesis of novel β(1-4)-Glucosyltransferase inhibitors and Their In vitro inhibition studies

2002 ◽  
Vol 10 (4) ◽  
pp. 1129-1136 ◽  
Author(s):  
Asish K Bhattacharya ◽  
Florian Stolz ◽  
Jürgen Kurzeck ◽  
Wolfgang Rüger ◽  
Richard R Schmidt
Keyword(s):  
Design And Synthesis ◽  
In Vitro Inhibition ◽  
Directed Design ◽  
Inhibition Studies

Characterization and in Vitro Inhibition Studies of Bacillus anthracis FtsZ: A Potential Antibacterial Target

2014 ◽  
Vol 172 (6) ◽  
pp. 3263-3270 ◽  
Author(s):  
Hae-Chul Park ◽  
Vinayakumar Gedi ◽  
June-Haeng Cho ◽  
Jae-Wook Hyun ◽  
Kwang-Jick Lee ◽  
...  
Keyword(s):  
Bacillus Anthracis ◽  
In Vitro Inhibition ◽  
Antibacterial Target ◽  
Inhibition Studies

scholarly journals Prediction of seriniquinone-drug interactions by in vitro inhibition of human cytochrome P450 enzymes

2020 ◽  
Vol 65 ◽  
pp. 104820
Author(s):  
Rodrigo Moreira da Silva ◽  
Daniel Blascke Carrão ◽  
Maísa Daniela Habenschus ◽  
Paula Christine Jimenez ◽  
Norberto Peporine Lopes ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interactions ◽  
Cytochrome P450 Enzymes ◽  
Human Cytochrome ◽  
In Vitro Inhibition

scholarly journals Synthesis and Inhibition Activity Study of Triazinyl-Substituted Amino(alkyl)-benzenesulfonamide Conjugates with Polar and Hydrophobic Amino Acids as Inhibitors of Human Carbonic Anhydrases I, II, IV, IX, and XII

2021 ◽  
Vol 22 (20) ◽  
pp. 11283
Author(s):  
Mária Bodnár Mikulová ◽  
Dáša Kružlicová ◽  
Daniel Pecher ◽  
Andrea Petreni ◽  
Claudiu T. Supuran ◽  
...  
Keyword(s):  
Amino Acids ◽  
Side Chain ◽  
Carbonic Anhydrases ◽  
Inhibition Activity ◽  
Short Reaction Time ◽  
High Affinity ◽  
Hydrophobic Amino Acids ◽  
In Vitro Inhibition ◽  
Inhibition Studies

Primary sulfonamide derivatives with various heterocycles represent the most widespread group of potential human carbonic anhydrase (hCA) inhibitors with high affinity and selectivity towards specific isozymes from the hCA family. In this work, new 4-aminomethyl- and aminoethyl-benzenesulfonamide derivatives with 1,3,5-triazine disubstituted with a pair of identical amino acids, possessing a polar (Ser, Thr, Asn, Gln) and non-polar (Ala, Tyr, Trp) side chain, have been synthesized. The optimized synthetic, purification, and isolation procedures provided several pronounced benefits such as a short reaction time (in sodium bicarbonate aqueous medium), satisfactory yields for the majority of new products (20.6–91.8%, average 60.4%), an effective, well defined semi-preparative RP-C18 liquid chromatography (LC) isolation of desired products with a high purity (>97%), as well as preservation of green chemistry principles. These newly synthesized conjugates, plus their 4-aminobenzenesulfonamide analogues prepared previously, have been investigated in in vitro inhibition studies towards hCA I, II, IV and tumor-associated isozymes IX and XII. The experimental results revealed the strongest inhibition of hCA XII with low nanomolar inhibitory constants (Kis) for the derivatives with amino acids possessing non-polar side chains (7.5–9.6 nM). Various derivatives were also promising for some other isozymes.

Sign in / Sign up

Export Citation Format

Share Document