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Darunavir — разлика између измена

С Википедије, слободне енциклопедије
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(Није приказано 7 међуизмена 3 корисника)
Ред 7: Ред 7:
| width2 =
| width2 =
| alt2 =
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| imagename =
| drug_name = Darunavir
| drug_name = Darunavir
| caption =
| caption =
Ред 69: Ред 68:
| StdInChI_comment =
| StdInChI_comment =
| StdInChIKey = CJBJHOAVZSMMDJ-HEXNFIEUSA-N
| StdInChIKey = CJBJHOAVZSMMDJ-HEXNFIEUSA-N
| StdStdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| density =
| density =
| melting_point =
| melting_point =
Ред 80: Ред 79:
| sec_combustion =
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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>
== Osobine ==
== Osobine ==


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
|-
|-
| [[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
|}
|}


Ред 104: Ред 103:


== Literatura ==
== Literatura ==
{{Литература}}
{{refbegin}}
* {{GoodmanGilman10th}}
* {{GoodmanGilman10th}}
* {{FoyePrinciplesMedChem6th}}
* {{FoyePrinciplesMedChem6th}}
{{Литература крај}}
{{refend}}
== Spoljašnje veze ==
== Spoljašnje veze ==

{{Portal-lat|Medicina|Hemija}}

{{Commonscat-lat|Darunavir}}
* [http://www.drugbank.ca/drugs/DB01264 -{Darunavir}-]
* [http://www.drugbank.ca/drugs/DB01264 -{Darunavir}-]


{{Medicinsko upozorenje-lat}}
{{Medicinsko upozorenje-lat}}
{{Podnožje|lat=da|Medicina|Hemija}}


[[Категорија:Антивиротици]]
[[Категорија:Антивиротици]]

Тренутна верзија на датум 9. април 2024. у 22:21

Darunavir
Klinički podaci
Drugs.comMonografija
Način primeneOralno
Farmakokinetički podaci
Poluvreme eliminacije15 h
IzlučivanjeRekalno, renaln o
Identifikatori
CAS broj206361-99-1 ДаY
ATC kodJ05AE10 (WHO)
PubChemCID 213039
DrugBankDB01264 ДаY
ChemSpider184733 ДаY
ChEBICHEBI:367163 ДаY
ChEMBLCHEMBL1323 ДаY
Hemijski podaci
FormulaC27H37N3O7S
Molarna masa547,664
  • [H][C@@]12CCO[C@]1([H])OC[C@@H]2OC(=O)N[C@@H](CC1=CC=CC=C1)[C@H](O)CN(CC(C)C)S(=O)(=O)C1=CC=C(N)C=C1
  • InChI=1S/C27H37N3O7S/c1-18(2)15-30(38(33,34)21-10-8-20(28)9-11-21)16-24(31)23(14-19-6-4-3-5-7-19)29-27(32)37-25-17-36-26-22(25)12-13-35-26/h3-11,18,22-26,31H,12-17,28H2,1-2H3,(H,29,32)/t22-,23-,24+,25-,26+/m0/s1 ДаY
  • Key:CJBJHOAVZSMMDJ-HEXNFIEUSA-N ДаY

Darunavir je organsko jedinjenje, koje sadrži 27 atoma ugljenika i ima molekulsku masu od 547,664 Da.[1][2][3][4][5][6][7]

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
  1. ^ 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
  2. ^ Tremblay CL: Combating HIV resistance - focus on darunavir. Ther Clin Risk Manag. 2008 Aug;4(4):759-66. PMID 19209258
  3. ^ 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
  4. ^ 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
  5. ^ 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
  6. ^ 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 3013709Слободан приступ. PMID 21059682. doi:10.1093/nar/gkq1126.  уреди
  7. ^ 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 2238889Слободан приступ. PMID 18048412. doi:10.1093/nar/gkm958.  уреди
  8. ^ 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. 
  9. ^ 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.  уреди
  10. ^ 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.  уреди

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