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Estimation of passive gastrointestinal absorption and membrane retention using PAMPA test, quantitative structure-permeability and quantitative structure-retention relationship analyses of ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid and 1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid derivatives
dc.creator | Tubić, Biljana | |
dc.creator | Dobričić, Vladimir | |
dc.creator | Poljarević, Jelena | |
dc.creator | Savić, Aleksandar | |
dc.creator | Sabo, Tibor | |
dc.creator | Marković, Bojan | |
dc.date.accessioned | 2020-03-13T09:27:09Z | |
dc.date.available | 2022-02-24 | |
dc.date.issued | 2020 | |
dc.identifier.issn | 0731-7085 | |
dc.identifier.uri | https://farfar.pharmacy.bg.ac.rs/handle/123456789/3553 | |
dc.description.abstract | Passive gastrointestinal absorption and membrane retention of twelve esters of (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (EDCP) and (S,S)-1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid (PDCP), as well as of these two non-esterified acids were estimated using PAMPA test. Artificial PAMPA membrane used in this study for the simulation of gastrointestinal barrier was solution of egg lecithin in dodecane (1 % w/v). All tested compounds belong to class III (high membrane retention and low permeation), whereas EDCP, dipentyl ester of PDCP (DPE-PDCP) and diisopentyl ester of PDCP (DIPE-PDCP) belong to class I (negligible membrane retention and low permeation). Finally, quantitative structure – permeability and structure – retention relationships models were created in order to find quantitative relationships between physico-chemical properties of tested compounds and PAMPA membrane permeability/membrane retention parameters. Statistically the most reliable models were analysed and used for the design of new compounds for which favourable membrane permeability and retention can be expected. | en |
dc.publisher | Elsevier B.V. | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172041/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172035/RS// | |
dc.rights | embargoedAccess | |
dc.rights.uri | https://creativecommons.org/licenses/by-nc-nd/4.0/ | |
dc.source | Journal of Pharmaceutical and Biomedical Analysis | |
dc.subject | (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid and (S,S)-1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid derivatives | |
dc.subject | Membrane permeability | |
dc.subject | Membrane retention | |
dc.subject | PAMPA | |
dc.title | Estimation of passive gastrointestinal absorption and membrane retention using PAMPA test, quantitative structure-permeability and quantitative structure-retention relationship analyses of ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid and 1,3-propanediamine-N,N'-di-2-(3-cyclohexyl)propanoic acid derivatives | en |
dc.type | article | |
dc.rights.license | BY-NC-ND | |
dcterms.abstract | Тубић, Биљана; Сабо, Тибор; Пољаревић, Јелена; Савић, Aлександар; Марковић, Бојан; Добричић, Владимир; | |
dc.citation.volume | 184 | |
dc.citation.rank | M21 | |
dc.description.other | This is the peer-reviewed version of the following article: Tubić, B.; Dobričić, V.; Poljarević, J.; Savić, A.; Sabo, T.; Marković, B. Estimation of Passive Gastrointestinal Absorption and Membrane Retention Using PAMPA Test, Quantitative Structure-Permeability and Quantitative Structure-Retention Relationship Analyses of Ethylenediamine-N,N’-Di-2-(3-Cyclohexyl)Propanoic Acid and 1,3-Propanediamine-N,N’-Di-2-(3-Cyclohexyl)Propanoic Acid Derivatives. Journal of Pharmaceutical and Biomedical Analysis 2020, 184. [https://doi.org/10.1016/j.jpba.2020.113213] | |
dc.identifier.wos | 000527297500035 | |
dc.identifier.doi | 10.1016/j.jpba.2020.113213 | |
dc.identifier.scopus | 2-s2.0-85080081642 | |
dc.type.version | acceptedVersion | |
dc.type.version | publishedVersion |