Zofenopril (Zofenoprilum) je inhbitor angiotenzin konvertujućeg enzima (ACE) sa kardioprotektivnim svojstvima, koji se koristi za tretman hipertenzije.[6]

Zofenopril
(IUPAC) ime
(2S,4S)-1-((S)-3-(benzoiltio)-2-metilpropanoil)-4-(feniltio)pirolidin-2-karboksilna kiselina
Klinički podaci
AHFS/Drugs.com Internacionalno ime leka
Identifikatori
CAS broj 81872-10-8
ATC kod C09AA15
PubChem[1][2] 92400
ChemSpider[3] 83422
UNII 290ZY759PI DaY
KEGG[4] D08688 DaY
ChEMBL[5] CHEMBL331378 DaY
Hemijski podaci
Formula C22H23NO4S2 
Mol. masa 429,552 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status
Način primene Oralno

U manjim kliničkim studijama je utvrđeno da je zofenopril znatno efektivniji od starijih antihipertenziva atenolola i enalaprila, i da uzrokuje manji broj nuspojava.[7][8]

Osobine

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Osobina Vrednost
Broj akceptora vodonika 6
Broj donora vodonika 1
Broj rotacionih veza 8
Particioni koeficijent[9] (ALogP) 3,9
Rastvorljivost[10] (logS, log(mol/L)) -5,8
Polarna površina[11] (PSA, Å2) 125,3

Reference

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  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H. 
  5. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  6. Ambrosioni E (2007). „Defining the role of zofenopril in the management of hypertension and ischemic heart disorders”. Am J Cardiovasc Drugs 7 (1): 17-24. DOI:10.2165/00129784-200707010-00002. PMID 17355163. 
  7. Nilsson P (October 2007). „Antihypertensive efficacy of zofenopril compared with atenolol in patients with mild to moderate hypertension”. Blood Press Suppl 2: 25-30. PMID 18046976. 
  8. Mallion JM (October 2007). „An evaluation of the initial and long-term antihypertensive efficacy of zofenopril compared with enalapril in mild to moderate hypertension”. Blood Press Suppl 2: 13-8. PMID 18046974. 
  9. Ghose, A.K., Viswanadhan V.N., and 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. 
  10. 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. DOI:10.1021/ci000392t. PMID 11749573. 
  11. 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. DOI:10.1021/jm000942e. PMID 11020286. 

Literatura

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Spoljašnje veze

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