Towards the rational design of novel drugs based on solubility, partitioning/distribution, biomimetic permeability and biological activity exemplified by 1,2,4-thiadiazole derivatives
Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors were synthesized and identified. Their ability to inhibit the glutamate stimulated Ca uptake was investigated. The solubility of thiadiazoles was measured in a buffer solution (pH 7.4) at 298 K. The distribution coefficients in 1-octanol/...
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| Published in: | MedChemComm Vol. 8; no. 1; pp. 162 - 175 |
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| Main Authors: | , , , , , |
| Format: | Journal Article |
| Language: | English |
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01-01-2017
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| Abstract | Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors were synthesized and identified. Their ability to inhibit the glutamate stimulated Ca
uptake was investigated. The solubility of thiadiazoles was measured in a buffer solution (pH 7.4) at 298 K. The distribution coefficients in 1-octanol/buffer (pH 7.4) and 1-hexane/buffer (pH 7.4) immiscible phases as model systems imitating the gastrointestinal tract epithelium and the blood-brain barrier were determined. Permeation experiments the new Permeapad™ barrier using Franz diffusion cells were conducted and the apparent permeability coefficients were obtained. The influence of the compound structure on the physicochemical properties determining the bioavailability of drug-like substances was revealed. Solubility-permeability interplay has been assessed to evaluate potential bioavailability of the compounds studied. |
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| AbstractList | Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors were synthesized and identified. Their ability to inhibit the glutamate stimulated Ca
uptake was investigated. The solubility of thiadiazoles was measured in a buffer solution (pH 7.4) at 298 K. The distribution coefficients in 1-octanol/buffer (pH 7.4) and 1-hexane/buffer (pH 7.4) immiscible phases as model systems imitating the gastrointestinal tract epithelium and the blood-brain barrier were determined. Permeation experiments the new Permeapad™ barrier using Franz diffusion cells were conducted and the apparent permeability coefficients were obtained. The influence of the compound structure on the physicochemical properties determining the bioavailability of drug-like substances was revealed. Solubility-permeability interplay has been assessed to evaluate potential bioavailability of the compounds studied. Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors were synthesized and identified. Their ability to inhibit the glutamate stimulated Ca2+ uptake was investigated. The solubility of thiadiazoles was measured in a buffer solution (pH 7.4) at 298 K. The distribution coefficients in 1-octanol/buffer (pH 7.4) and 1-hexane/buffer (pH 7.4) immiscible phases as model systems imitating the gastrointestinal tract epithelium and the blood-brain barrier were determined. Permeation experiments the new Permeapad™ barrier using Franz diffusion cells were conducted and the apparent permeability coefficients were obtained. The influence of the compound structure on the physicochemical properties determining the bioavailability of drug-like substances was revealed. Solubility-permeability interplay has been assessed to evaluate potential bioavailability of the compounds studied.Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors were synthesized and identified. Their ability to inhibit the glutamate stimulated Ca2+ uptake was investigated. The solubility of thiadiazoles was measured in a buffer solution (pH 7.4) at 298 K. The distribution coefficients in 1-octanol/buffer (pH 7.4) and 1-hexane/buffer (pH 7.4) immiscible phases as model systems imitating the gastrointestinal tract epithelium and the blood-brain barrier were determined. Permeation experiments the new Permeapad™ barrier using Franz diffusion cells were conducted and the apparent permeability coefficients were obtained. The influence of the compound structure on the physicochemical properties determining the bioavailability of drug-like substances was revealed. Solubility-permeability interplay has been assessed to evaluate potential bioavailability of the compounds studied. Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors were synthesized and identified. Their ability to inhibit the glutamate stimulated Ca2+ uptake was investigated. The solubility of thiadiazoles was measured in a buffer solution (pH 7.4) at 298 K. The distribution coefficients in 1-octanol/buffer (pH 7.4) and 1-hexane/buffer (pH 7.4) immiscible phases as model systems imitating the gastrointestinal tract epithelium and the blood-brain barrier were determined. Permeation experiments the new Permeapad(TM) barrier using Franz diffusion cells were conducted and the apparent permeability coefficients were obtained. The influence of the compound structure on the physicochemical properties determining the bioavailability of drug-like substances was revealed. Solubility-permeability interplay has been assessed to evaluate potential bioavailability of the compounds studied. Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors were synthesized and identified. Their ability to inhibit the glutamate stimulated Ca 2+ uptake was investigated. The solubility of thiadiazoles was measured in a buffer solution (pH 7.4) at 298 K. The distribution coefficients in 1-octanol/buffer (pH 7.4) and 1-hexane/buffer (pH 7.4) immiscible phases as model systems imitating the gastrointestinal tract epithelium and the blood–brain barrier were determined. Permeation experiments the new Permeapad™ barrier using Franz diffusion cells were conducted and the apparent permeability coefficients were obtained. The influence of the compound structure on the physicochemical properties determining the bioavailability of drug-like substances was revealed. Solubility–permeability interplay has been assessed to evaluate potential bioavailability of the compounds studied. |
| Author | Terekhova, I V Volkova, T V Bauer-Brandl, A Perlovich, G L Silyukov, O I Proshin, A N |
| Author_xml | – sequence: 1 givenname: T V surname: Volkova fullname: Volkova, T V email: glp@isc-ras.ru organization: Department of Physical Chemistry of Drugs , Krestov's Institute of Solution Chemistry, Russian Academy of Sciences , 153045 Akademicheskaya str. 1 , Ivanovo , Russia . Email: glp@isc-ras.ru – sequence: 2 givenname: I V surname: Terekhova fullname: Terekhova, I V email: glp@isc-ras.ru organization: Department of Physical Chemistry of Drugs , Krestov's Institute of Solution Chemistry, Russian Academy of Sciences , 153045 Akademicheskaya str. 1 , Ivanovo , Russia . Email: glp@isc-ras.ru – sequence: 3 givenname: O I orcidid: 0000-0003-1235-727X surname: Silyukov fullname: Silyukov, O I email: glp@isc-ras.ru organization: Department of Physical Chemistry of Drugs , Krestov's Institute of Solution Chemistry, Russian Academy of Sciences , 153045 Akademicheskaya str. 1 , Ivanovo , Russia . Email: glp@isc-ras.ru – sequence: 4 givenname: A N surname: Proshin fullname: Proshin, A N organization: Institute of Physiologically Active Compounds , Russian Academy of Sciences , 142432 , Chernogolovka , Russia – sequence: 5 givenname: A surname: Bauer-Brandl fullname: Bauer-Brandl, A organization: Department of Physics , Chemistry and Pharmacy , University of Southern Denmark , 5230 Odense M , Denmark – sequence: 6 givenname: G L surname: Perlovich fullname: Perlovich, G L email: glp@isc-ras.ru organization: Department of Physical Chemistry of Drugs , Krestov's Institute of Solution Chemistry, Russian Academy of Sciences , 153045 Akademicheskaya str. 1 , Ivanovo , Russia . Email: glp@isc-ras.ru |
| BackLink | https://www.ncbi.nlm.nih.gov/pubmed/30108702$$D View this record in MEDLINE/PubMed |
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| Cites_doi | 10.1016/j.jct.2015.12.016 10.1021/cg400666v 10.1021/jm00169a041 10.1007/978-3-7091-9376-1 10.1007/s10517-006-0289-7 10.1021/je300143a 10.1002/047145026X 10.1039/j39670002005 10.1021/cr60274a001 10.1021/jp405624e 10.1016/j.ejps.2015.05.008 10.2174/0929867321666141106122628 10.1016/j.tics.2010.11.002 10.1039/C5CP03263F 10.1021/acs.molpharmaceut.5b00020 10.2165/00003495-199753050-00003 10.1021/jm011020u 10.1248/cpb.53.958 10.1007/s00213-005-2200-z 10.1021/mp300011r 10.1016/j.ejps.2015.03.019 10.1021/ja01062a035 10.1002/jps.2600690814 10.1016/j.jconrel.2004.11.021 10.1016/j.bmc.2005.10.012 10.1128/AAC.37.1.100 10.1021/jm8012882 10.1002/jps.2600760217 10.1002/jps.22143 10.1021/mp2003237 |
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| Snippet | Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors were synthesized and identified. Their ability to inhibit the glutamate stimulated Ca
uptake was... Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors were synthesized and identified. Their ability to inhibit the glutamate stimulated Ca 2+ uptake... Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors were synthesized and identified. Their ability to inhibit the glutamate stimulated Ca2+ uptake... |
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