Tasosartan

Tasosartan
(IUPAC) ime
	2,4-dimetil-8[2'-(1H-tetrazol-5-il)bifenil-4-il]metil5,8-dihidropirido[2,3-d]pirimidin-7(6H)-on
Klinički podaci
Identifikatori
CAS broj	145733-36-4
ATC kod	C09CA05
PubChem	60919
DrugBank	DB01349
ChemSpider	54890
UNII	48G92V856H
Hemijski podaci
Formula	C23H21N7O
Mol. masa	411,459 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C23H21N7O/c1-14-18-11-12-21(31)30(23(18)25-15(2)24-14)13-16-7-9-17(10-8-16)19-5-3-4-6-20(19)22-26-28-29-27-22/h3-10H,11-13H2,1-2H3,(H,26,27,28,29); Key: ADXGNEYLLLSOAR-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	Withdrawn

Tasosartan je antagonist angiotenzin II receptora.

Proizvođač je ovaj lek povukao sa FDA pregleda nakon što su klinička ispitivanja faze III pokazala povišene transaminaze (znak moguće hepatotoksičnosti) kod znatnog broja učestnika.^[4]^[5]

Osobine

Osobina	Vrednost
Broj akceptora vodonika	6
Broj donora vodonika	1
Broj rotacionih veza	4
Particioni koeficijent^[6] (ALogP)	3,1
Rastvorljivost^[7] (logS, log(mol/L))	-5,9
Polarna površina^[8] (PSA, Å²)	100,6

Reference

↑ 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
↑ 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.
↑ 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
↑ Atkinson AJ et al. (2007). Principles of clinical pharmacology. Amsterdam: Elsevier. str. 515. ISBN 0-12-369417-5.
↑ Dina R, Jafari M (July 2000). „Angiotensin II-receptor antagonists: an overview”. Am J Health Syst Pharm 57 (13): 1231–41. PMID 10902066.
↑ 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.
↑ 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. edit
↑ 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. edit

Literatura

Hardman JG, Limbird LE, Gilman AG. (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10 izd.). New York: McGraw-Hill. DOI:10.1036/0071422803. ISBN 0-07-135469-7.
Thomas L. Lemke, David A. Williams, ur. (2007). Foye's Principles of Medicinal Chemistry (6 izd.). Baltimore: Lippincott Willams & Wilkins. ISBN 0-7817-6879-9.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Tasosartan

[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] Atkinson AJ et al. (2007). Principles of clinical pharmacology. Amsterdam: Elsevier. str. 515. ISBN 0-12-369417-5.

[5] Dina R, Jafari M (July 2000). „Angiotensin II-receptor antagonists: an overview”. Am J Health Syst Pharm 57 (13): 1231–41. PMID 10902066.

[6] 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.

[7] 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. edit

[8] 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. edit

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]