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    Tasosartan

    ACTIVE PHARMA INGREDIENTS

    INTERMEDIATES

    PharmaCompass
    Xls

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    2D Structure
    Also known as: 145733-36-4, Ana-756, Way-ana-756, 2,4-dimethyl-8-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[2,3-d]pyrimidin-7-one, Chembl432162, 48g92v856h
    Molecular Formula
    C23H21N7O
    Molecular Weight
    411.5  g/mol
    InChI Key
    ADXGNEYLLLSOAR-UHFFFAOYSA-N
    FDA UNII
    48G92V856H
    Tasosartan is a long-acting angiotensin II (AngII) receptor blocker. Its long duration of action has been attributed to its active metabolite enoltasosartan. It is used to treat patients with essential hypertension.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    2,4-dimethyl-8-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[2,3-d]pyrimidin-7-one
    2.1.2 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)
    2.1.3 InChI Key
    ADXGNEYLLLSOAR-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    CC1=C2CCC(=O)N(C2=NC(=N1)C)CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5
    2.2 Other Identifiers
    2.2.1 UNII
    48G92V856H
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. 5,8-dihydro-2,4-dimethyl-8-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)pyrido(2,3-d)pyrimidin-7(6h)-one

    2. Ana 756

    3. Ana-756

    4. Ana756

    5. Taso-sartan

    2.3.2 Depositor-Supplied Synonyms

    1. 145733-36-4

    2. Ana-756

    3. Way-ana-756

    4. 2,4-dimethyl-8-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[2,3-d]pyrimidin-7-one

    5. Chembl432162

    6. 48g92v856h

    7. Verdia

    8. 2,4-dimethyl-8-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[6,5-d]pyrimidin-7-one

    9. 5,8-dihydro-2,4-dimethyl-8-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)pyrido(2,3-d)pyrimidin-7(6h)-one

    10. Taso-sartan

    11. 8-((2'-(1h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2,4-dimethyl-5,8-dihydropyrido[2,3-d]pyrimidin-7(6h)-one

    12. Ana756

    13. Tasosartan (usan/inn)

    14. Tasosartan [usan:inn:ban]

    15. Unii-48g92v856h

    16. Ana 756

    17. Way-126756

    18. Ethylglycidylether

    19. Tasosartan [mi]

    20. Tasosartan [inn]

    21. Tasosartan [usan]

    22. Tasosartan [mart.]

    23. Tasosartan [who-dd]

    24. Schembl49626

    25. Way-ana 756

    26. Gtpl6898

    27. Dtxsid40163148

    28. Ex-a082

    29. Chebi:135666

    30. Act06754

    31. Amy31168

    32. Bcp06091

    33. Hy-a0250

    34. Bdbm50040439

    35. Mfcd00865905

    36. Zinc13444037

    37. Akos000278114

    38. Db01349

    39. Ds-6574

    40. Ncgc00390218-01

    41. 5,8-dihydro-2,4-dimethyl-8-(p-(o-1h-tetrazol-5-ylphenyl)benzyl)pyrido(2,3-d)pyrimidin-7(6h)-one

    42. Ac-35374

    43. Db-042802

    44. Cs-0017594

    45. Ft-0631174

    46. D06010

    47. 733t364

    48. A846571

    49. L001443

    50. J-524315

    51. Q1317131

    52. 2,4-dimethyl-8-({4-[2-(2h-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-5h,6h,7h,8h-pyrido[2,3-d]pyrimidin-7-one

    53. 2,4-dimethyl-8-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-5,8-dihydro-6h-pyrido[2,3-d]pyrimidin-7-one

    54. 2,4-dimethyl-8-[2''-(2h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-5,8-dihydro-6h-pyrido[2,3-d]pyrimidin-7-one

    55. 2,4-dimethyl-8-[2'-(1h-tetrazol-5-yl)biphenyl-4-ylmethyl]-5,8-dihydro-6h-pyrido[2,3-d]pyrimidin-7-one

    56. 2,4-dimethyl-8-{[2'-(1h-tetrazol-5-yl)biphenyl-4-yl]methyl}-5,8-dihydropyrido[2,3-d]pyrimidin-7(6h)-one

    57. 5,8-dihydro-2,4-dimethyl-8-[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-pyrido[2,3-d]pyrimidin-7(6h)-one

    58. 5,8-dihydro-2,4-dimethyl-8-[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]pyrido[2,3-d]pyrimidin-7(6h)-one

    59. 8-((2'-(1h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2,4-dimethyl-5,6-dihydropyrido[2,3-d]pyrimidin-7(8h)-one

    60. 8-((2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl)-2,4-dimethyl-5,6-dihydropyrido[2,3-d]pyrimidin-7(8h)-one

    61. Pyrido(2,3-d)pyrimidin-7(6h)-one, 5,8-dihydro-2,4-dimethyl-8-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-

    62. Pyrido[2,3-d]pyrimidin-7(6h)-one, 5,8-dihydro-2,4-dimethyl-8-[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-

    2.4 Create Date
    2005-08-08
    3 Chemical and Physical Properties
    Molecular Weight 411.5 g/mol
    Molecular Formula C23H21N7O
    XLogP33
    Hydrogen Bond Donor Count1
    Hydrogen Bond Acceptor Count6
    Rotatable Bond Count4
    Exact Mass411.18075832 g/mol
    Monoisotopic Mass411.18075832 g/mol
    Topological Polar Surface Area101 Ų
    Heavy Atom Count31
    Formal Charge0
    Complexity625
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Indication

    Tasosartan is infrequently in the treatment of hypertension and heart failure.

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    By blocking the angiotensin II (AT1) receptor, the drug ultimately causes vasodilation, reduced secretion of vasopressin (ADH), reduced production and secretion of aldosterone, amongst other actions leading to the combined effect of a reduction of blood pressure.

    5.2 MeSH Pharmacological Classification

    Angiotensin II Type 1 Receptor Blockers

    Agents that antagonize ANGIOTENSIN II TYPE 1 RECEPTOR. Included are ANGIOTENSIN II analogs such as SARALASIN and biphenylimidazoles such as LOSARTAN. Some are used as ANTIHYPERTENSIVE AGENTS. (See all compounds classified as Angiotensin II Type 1 Receptor Blockers.)

    5.3 ATC Code

    C - Cardiovascular system

    C09 - Agents acting on the renin-angiotensin system

    C09C - Angiotensin ii receptor blockers (arbs), plain

    C09CA - Angiotensin ii receptor blockers (arbs), plain

    C09CA05 - Tasosartan

    5.4 Metabolism/Metabolites

    Tasosartan has known human metabolites that include enoltasosartan.

    S73 | METXBIODB | Metabolite Reaction Database from BioTransformer | DOI:10.5281/zenodo.4056560

    5.5 Mechanism of Action

    Tasosartan is a selective, potent, orally active and long-acting nonpeptide Angiotensin II type 1 (AT1) receptor antagonist. Tasosartan blocks the renin-angiotensin-aldosterone system (RAAS) at the level of the AT1 receptor that mediates most, if not all, of the important actions of Ang II. Tasosartan binds reversibly to the AT1 receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance. AT1 receptor antagonists avoid the nonspecificity of the Ang I converting enzyme (ACE) inhibitors.