Darunavir — разлика између измена
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| drug_name = Darunavir |
| drug_name = Darunavir |
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'''Darunavir''' je [[organsko jedinjenje]] koje sadrži 27 [[atom]]a [[ugljenik]]a i ima [[Молекулска маса|molekulsku masu]] od 547,664 [[Јединица атомске масе|-{Da}-]].<ref>-{Back D, Sekar V, Hoetelmans RM: Darunavir: pharmacokinetics and drug interactions. Antivir Ther. 2008;13(1):1-13. [[PubMed|PMID]] [http://www.ncbi.nlm.nih.gov/pubmed/18389894 Medilexicon Link:http://www.medilexicon.com/drugs/prezista.php 18389894 Medilexicon Link:http://www.medilexicon.com/drugs/prezista.php]}-</ref><ref>-{Tremblay CL: Combating HIV resistance - focus on darunavir. Ther Clin Risk Manag. 2008 Aug;4(4):759-66. [[PubMed|PMID]] [http://www.ncbi.nlm.nih.gov/pubmed/19209258 19209258]}-</ref><ref>-{Koh Y, Matsumi S, Das D, Amano M, Davis DA, Li J, Leschenko S, Baldridge A, Shioda T, Yarchoan R, Ghosh AK, Mitsuya H: Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization. J Biol Chem. 2007 Sep 28;282(39):28709-20. Epub 2007 Jul 17. [[PubMed|PMID]] [http://www.ncbi.nlm.nih.gov/pubmed/17635930 17635930]}-</ref><ref>-{Kovalevsky AY, Tie Y, Liu F, Boross PI, Wang YF, Leshchenko S, Ghosh AK, Harrison RW, Weber IT: Effectiveness of nonpeptide clinical inhibitor TMC-114 on HIV-1 protease with highly drug resistant mutations D30N, I50V, and L90M. J Med Chem. 2006 Feb 23;49(4):1379-87. [[PubMed|PMID]] [http://www.ncbi.nlm.nih.gov/pubmed/16480273 16480273]}-</ref><ref>-{De Meyer S, Azijn H, Surleraux D, Jochmans D, Tahri A, Pauwels R, Wigerinck P, de Bethune MP: TMC114, a novel human immunodeficiency virus type 1 protease inhibitor active against protease inhibitor-resistant viruses, including a broad range of clinical isolates. Antimicrob Agents Chemother. 2005 Jun;49(6):2314-21. [[PubMed|PMID]] [http://www.ncbi.nlm.nih.gov/pubmed/15917527 15917527]}-</ref><ref>{{Cite pmid|21059682}}</ref><ref>{{cite pmid|18048412}}</ref> |
'''Darunavir''' je [[organsko jedinjenje]], koje sadrži 27 [[atom]]a [[ugljenik]]a i ima [[Молекулска маса|molekulsku masu]] od 547,664 [[Јединица атомске масе|-{Da}-]].<ref>-{Back D, Sekar V, Hoetelmans RM: Darunavir: pharmacokinetics and drug interactions. Antivir Ther. 2008;13(1):1-13. [[PubMed|PMID]] [http://www.ncbi.nlm.nih.gov/pubmed/18389894 Medilexicon Link:http://www.medilexicon.com/drugs/prezista.php 18389894 Medilexicon Link:http://www.medilexicon.com/drugs/prezista.php]}-</ref><ref>-{Tremblay CL: Combating HIV resistance - focus on darunavir. Ther Clin Risk Manag. 2008 Aug;4(4):759-66. [[PubMed|PMID]] [http://www.ncbi.nlm.nih.gov/pubmed/19209258 19209258]}-</ref><ref>-{Koh Y, Matsumi S, Das D, Amano M, Davis DA, Li J, Leschenko S, Baldridge A, Shioda T, Yarchoan R, Ghosh AK, Mitsuya H: Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization. J Biol Chem. 2007 Sep 28;282(39):28709-20. Epub 2007 Jul 17. [[PubMed|PMID]] [http://www.ncbi.nlm.nih.gov/pubmed/17635930 17635930]}-</ref><ref>-{Kovalevsky AY, Tie Y, Liu F, Boross PI, Wang YF, Leshchenko S, Ghosh AK, Harrison RW, Weber IT: Effectiveness of nonpeptide clinical inhibitor TMC-114 on HIV-1 protease with highly drug resistant mutations D30N, I50V, and L90M. J Med Chem. 2006 Feb 23;49(4):1379-87. [[PubMed|PMID]] [http://www.ncbi.nlm.nih.gov/pubmed/16480273 16480273]}-</ref><ref>-{De Meyer S, Azijn H, Surleraux D, Jochmans D, Tahri A, Pauwels R, Wigerinck P, de Bethune MP: TMC114, a novel human immunodeficiency virus type 1 protease inhibitor active against protease inhibitor-resistant viruses, including a broad range of clinical isolates. Antimicrob Agents Chemother. 2005 Jun;49(6):2314-21. [[PubMed|PMID]] [http://www.ncbi.nlm.nih.gov/pubmed/15917527 15917527]}-</ref><ref>{{Cite pmid|21059682}}</ref><ref>{{cite pmid|18048412}}</ref> |
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== Osobine == |
== Osobine == |
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Ред 97: | Ред 96: | ||
| [[Rastvorljivost]]<ref>{{cite pmid|11749573}}</ref> (-{''logS'', log(''mol/L''}-)) || -4,9 |
| [[Rastvorljivost]]<ref>{{cite pmid|11749573}}</ref> (-{''logS'', log(''mol/L''}-)) || -4,9 |
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| [[Polarna površina]]<ref>{{cite pmid|11020286}}</ref> (''PSA'', [[Ангстрем (јединица)|Å<sup>2</sup>]]) || 148,8 |
| [[Polarna površina molekula|Polarna površina]]<ref>{{cite pmid|11020286}}</ref> (-{''PSA''}-, [[Ангстрем (јединица)|Å<sup>2</sup>]]) || 148,8 |
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== Literatura == |
== Literatura == |
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{{Литература}} |
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* {{GoodmanGilman10th}} |
* {{GoodmanGilman10th}} |
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* {{FoyePrinciplesMedChem6th}} |
* {{FoyePrinciplesMedChem6th}} |
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{{Литература крај}} |
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{{refend}} |
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== Spoljašnje veze == |
== Spoljašnje veze == |
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{{Commonscat-lat|Darunavir}} |
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* [http://www.drugbank.ca/drugs/DB01264 -{Darunavir}-] |
* [http://www.drugbank.ca/drugs/DB01264 -{Darunavir}-] |
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{{Medicinsko upozorenje-lat}} |
{{Medicinsko upozorenje-lat}} |
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[[Категорија:Антивиротици]] |
[[Категорија:Антивиротици]] |
Тренутна верзија на датум 9. април 2024. у 22:21
Klinički podaci | |
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Drugs.com | Monografija |
Način primene | Oralno |
Farmakokinetički podaci | |
Poluvreme eliminacije | 15 h |
Izlučivanje | Rekalno, renaln o |
Identifikatori | |
CAS broj | 206361-99-1 |
ATC kod | J05AE10 (WHO) |
PubChem | CID 213039 |
DrugBank | DB01264 |
ChemSpider | 184733 |
ChEBI | CHEBI:367163 |
ChEMBL | CHEMBL1323 |
Hemijski podaci | |
Formula | C27H37N3O7S |
Molarna masa | 547,664 |
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Darunavir je organsko jedinjenje, koje sadrži 27 atoma ugljenika i ima molekulsku masu od 547,664 Da.[1][2][3][4][5][6][7]
Osobine
[уреди | уреди извор]Osobina | Vrednost |
---|---|
Broj akceptora vodonika | 8 |
Broj donora vodonika | 3 |
Broj rotacionih veza | 12 |
Particioni koeficijent[8] (ALogP) | 2,6 |
Rastvorljivost[9] (logS, log(mol/L)) | -4,9 |
Polarna površina[10] (PSA, Å2) | 148,8 |
Reference
[уреди | уреди извор]- ^ Back D, Sekar V, Hoetelmans RM: Darunavir: pharmacokinetics and drug interactions. Antivir Ther. 2008;13(1):1-13. PMID Medilexicon Link:http://www.medilexicon.com/drugs/prezista.php 18389894 Medilexicon Link:http://www.medilexicon.com/drugs/prezista.php
- ^ Tremblay CL: Combating HIV resistance - focus on darunavir. Ther Clin Risk Manag. 2008 Aug;4(4):759-66. PMID 19209258
- ^ Koh Y, Matsumi S, Das D, Amano M, Davis DA, Li J, Leschenko S, Baldridge A, Shioda T, Yarchoan R, Ghosh AK, Mitsuya H: Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization. J Biol Chem. 2007 Sep 28;282(39):28709-20. Epub 2007 Jul 17. PMID 17635930
- ^ Kovalevsky AY, Tie Y, Liu F, Boross PI, Wang YF, Leshchenko S, Ghosh AK, Harrison RW, Weber IT: Effectiveness of nonpeptide clinical inhibitor TMC-114 on HIV-1 protease with highly drug resistant mutations D30N, I50V, and L90M. J Med Chem. 2006 Feb 23;49(4):1379-87. PMID 16480273
- ^ De Meyer S, Azijn H, Surleraux D, Jochmans D, Tahri A, Pauwels R, Wigerinck P, de Bethune MP: TMC114, a novel human immunodeficiency virus type 1 protease inhibitor active against protease inhibitor-resistant viruses, including a broad range of clinical isolates. Antimicrob Agents Chemother. 2005 Jun;49(6):2314-21. PMID 15917527
- ^ Knox C, Law V, Jewison T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS (2011). „DrugBank 3.0: a comprehensive resource for omics research on drugs”. Nucleic Acids Res. 39 (Database issue): D1035—41. PMC 3013709 . PMID 21059682. doi:10.1093/nar/gkq1126.
- ^ David S. Wishart; Craig Knox; An Chi Guo; Dean Cheng; Savita Shrivastava; Dan Tzur; Bijaya Gautam; Murtaza Hassanali (2008). „DrugBank: a knowledgebase for drugs, drug actions and drug targets”. Nucleic acids research. 36 (Database issue): D901—6. PMC 2238889 . PMID 18048412. doi:10.1093/nar/gkm958.
- ^ Ghose, A.K.; Viswanadhan V.N. & Wendoloski, J.J. (1998). „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragment Methods: An Analysis of AlogP and CLogP Methods”. J. Phys. Chem. A. 102: 3762—3772. doi:10.1021/jp980230o.
- ^ Tetko IV, Tanchuk VY, Kasheva TN, Villa AE (2001). „Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices”. Chem Inf. Comput. Sci. 41: 1488—1493. PMID 11749573. doi:10.1021/ci000392t.
- ^ Ertl P.; Rohde B.; Selzer P. (2000). „Fast calculation of molecular polar surface area as a sum of fragment based contributions and its application to the prediction of drug transport properties”. J. Med. Chem. 43: 3714—3717. PMID 11020286. doi:10.1021/jm000942e.
Literatura
[уреди | уреди извор]- Hardman JG, Limbird LE, Gilman AG (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10. изд.). New York: McGraw-Hill. ISBN 0071354697. doi:10.1036/0071422803.
- Thomas L. Lemke; David A. Williams, ур. (2007). Foye's Principles of Medicinal Chemistry (6. изд.). Baltimore: Lippincott Willams & Wilkins. ISBN 0781768799.
Spoljašnje veze
[уреди | уреди извор]
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