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    Chemistry

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    Also known as: 21187-98-4, Glimicron, 1-(3,3a,4,5,6,6a-hexahydro-1h-cyclopenta[c]pyrrol-2-yl)-3-(4-methylphenyl)sulfonylurea, 1-(3-azabicyclo(3.3.0)oct-3-yl)-3-(p-tolylsulfonyl)urea, Chebi:31654, 1-(hexahydrocyclopenta(c)pyrrol-2(1h)-yl)-3-(p-tolylsulfonyl)urea
    Molecular Formula
    C15H21N3O3S
    Molecular Weight
    323.4  g/mol
    InChI Key
    BOVGTQGAOIONJV-UHFFFAOYSA-N
    Gliclazide
    An oral sulfonylurea hypoglycemic agent which stimulates insulin secretion.
    1 2D Structure

    Gliclazide

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    1-(3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-2-yl)-3-(4-methylphenyl)sulfonylurea
    2.1.2 InChI
    InChI=1S/C15H21N3O3S/c1-11-5-7-14(8-6-11)22(20,21)17-15(19)16-18-9-12-3-2-4-13(12)10-18/h5-8,12-13H,2-4,9-10H2,1H3,(H2,16,17,19)
    2.1.3 InChI Key
    BOVGTQGAOIONJV-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    CC1=CC=C(C=C1)S(=O)(=O)NC(=O)NN2CC3CCCC3C2
    2.2 Synonyms
    2.2.1 MeSH Synonyms

    1. Diabrezide

    2. Diaglyk

    3. Diaikron

    4. Diamicron

    5. Gen Gliclazide

    6. Gen-gliclazide

    7. Gliklazid

    8. Glyade

    9. Glyclazide

    10. Novo Gliclazide

    11. Novo-gliclazide

    12. S 1702

    13. S 852

    14. S-1702

    15. S-852

    16. S1702

    17. S852

    2.2.2 Depositor-Supplied Synonyms

    1. 21187-98-4

    2. Glimicron

    3. 1-(3,3a,4,5,6,6a-hexahydro-1h-cyclopenta[c]pyrrol-2-yl)-3-(4-methylphenyl)sulfonylurea

    4. 1-(3-azabicyclo(3.3.0)oct-3-yl)-3-(p-tolylsulfonyl)urea

    5. Chebi:31654

    6. 1-(hexahydrocyclopenta(c)pyrrol-2(1h)-yl)-3-(p-tolylsulfonyl)urea

    7. Gliclazidum [inn-latin]

    8. Gliclazida [inn-spanish]

    9. Gliclazida

    10. N-(hexahydrocyclopenta[c]pyrrol-2(1h)-ylcarbamoyl)-4-methylbenzenesulfonamide

    11. 1-[(4-methylbenzene)sulfonyl]-3-{octahydrocyclopenta[c]pyrrol-2-yl}urea

    12. Nsc-758673

    13. Se-1702

    14. S1702;se1702

    15. Dsstox_cid_3095

    16. N-((hexahydrocyclopenta[c]pyrrol-2(1h)-yl)carbamoyl)-4-methylbenzenesulfonamide

    17. Dsstox_rid_76872

    18. Dsstox_gsid_23095

    19. S-852

    20. S-1702

    21. N-(4-methylbenzenesulfonyl)-n'-(3-azabicyclo(3.3.0)oct-3-yl)urea

    22. Glimicron (tn)

    23. Smr000542971

    24. Sr-01000816184

    25. 1-(3-azabicyclo[3.3.0]oct-3-yl)-3-p-tolylsulphonylurea

    26. Mfcd00409893

    27. J3.151h

    28. Gliclazide,(s)

    29. Benzenesulfonamide, N-[[(hexahydrocyclopenta[c]pyrrol-2(1h)-yl)amino]carbonyl]-4-methyl-

    30. Ncgc00016751-01

    31. Prestwick_869

    32. Cas-21187-98-4

    33. Gliclazide (diamicron)

    34. Spectrum_001478

    35. Specplus_000870

    36. Prestwick0_000558

    37. Prestwick1_000558

    38. Prestwick2_000558

    39. Prestwick3_000558

    40. Spectrum3_001862

    41. Spectrum4_000598

    42. Spectrum5_000753

    43. Gliclazide (jp17/inn)

    44. Schembl16387

    45. Bspbio_000635

    46. Bspbio_003304

    47. Kbiogr_001096

    48. Kbioss_001958

    49. Mls001215197

    50. Mls001304077

    51. Mls001304118

    52. Divk1c_006966

    53. Gliclazide, Powder, >=98%

    54. Spectrum1504145

    55. Spectrum1505013

    56. Spbio_002556

    57. Bpbio1_000699

    58. Chembl427216

    59. Dtxsid9023095

    60. Urea, 1-(hexahydrocyclopenta[c]pyrrol-2(1h)-yl)-3-(p-tolylsulfonyl)-

    61. Kbio1_001910

    62. Kbio2_001958

    63. Kbio2_004526

    64. Kbio2_007094

    65. Kbio3_002806

    66. 1-[3-azabicyclo[3.3.0]oct-3-yl]-3-p-toluenesulfonylurea

    67. Hms1569p17

    68. Hms1922d15

    69. Hms2090k16

    70. Hms2096p17

    71. Hms2855p09

    72. Hms3656c22

    73. Hms3713p17

    74. Hms3744o13

    75. Pharmakon1600-01504145

    76. Bcp21240

    77. Hy-b0753

    78. Tox21_110590

    79. Bbl012275

    80. Bdbm50103512

    81. Nsc758673

    82. Nsc813216

    83. S2601

    84. Se1702

    85. Stk803142

    86. Akos003237903

    87. Akos016340698

    88. Tox21_110590_1

    89. Ab05958

    90. Ccg-213918

    91. Db01120

    92. Ks-1067

    93. Nsc-813216

    94. N-[(hexahydrocyclopenta[c]pyrrol-2(1h)-ylamino)carbonyl]-4-methylbenzenesulfonamide

    95. Ncgc00095107-01

    96. Ncgc00095107-02

    97. Ncgc00095107-03

    98. Ncgc00095107-04

    99. Ncgc00095107-05

    100. Ncgc00095107-06

    101. Ncgc00095107-09

    102. Ncgc00095107-10

    103. Ac-12045

    104. Sbi-0052662.p002

    105. Ab00053165

    106. Ft-0626712

    107. G0381

    108. Sw196994-3

    109. D01599

    110. D83168

    111. Ab00053165-09

    112. Ab00053165_10

    113. Ab00053165_11

    114. 187g984

    115. A815188

    116. Q290001

    117. J-013905

    118. J-522753

    119. Sr-01000816184-2

    120. Sr-01000816184-3

    121. Sr-01000816184-4

    122. Brd-a61154809-001-04-3

    123. Gliclazide, British Pharmacopoeia (bp) Reference Standard

    124. Gliclazide, European Pharmacopoeia (ep) Reference Standard

    125. 1-(4-methylbenzenesulfonyl)-3-{octahydrocyclopenta[c]pyrrol-2-yl}urea

    126. 1-(3,3a,4,5,6,6a-hexahydro-1h-cyclopenta[c]pyrrol-2-yl)-3-(4-methylphenyl)sulfonyl-urea

    127. Benzenesulfonamide,n-[[(hexahydrocyclopenta[c]pyrrol-2(1h)-yl)amino]carbonyl]-4-methyl-

    128. Benzenesulfonamide, N-[[(hexahydrocyclopenta[c]pyrrol-2(1h)-yl)amino]carbonyl]-4-methyl

    2.3 Create Date
    2005-03-25
    3 Chemical and Physical Properties
    Molecular Weight 323.4 g/mol
    Molecular Formula C15H21N3O3S
    XLogP31.5
    Hydrogen Bond Donor Count2
    Hydrogen Bond Acceptor Count4
    Rotatable Bond Count3
    Exact Mass323.13036271 g/mol
    Monoisotopic Mass323.13036271 g/mol
    Topological Polar Surface Area86.9 Ų
    Heavy Atom Count22
    Formal Charge0
    Complexity497
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count2
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Indication

    For the treatment of NIDDM in conjunction with diet and exercise.

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    Based on the pharmacological properties, gliclazide is a second generation sulphonylurea which acts as a hypoglycemic agent. It stimulates β cells of the islet of Langerhans in the pancreas to release insulin. It also enhances peripheral insulin sensitivity. Overall, it potentiates insulin release and improves insulin dynamics.

    5.2 MeSH Pharmacological Classification

    Hypoglycemic Agents

    Substances which lower blood glucose levels. (See all compounds classified as Hypoglycemic Agents.)

    5.3 ATC Code

    A10BB09

    S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355

    A - Alimentary tract and metabolism

    A10 - Drugs used in diabetes

    A10B - Blood glucose lowering drugs, excl. insulins

    A10BB - Sulfonylureas

    A10BB09 - Gliclazide

    5.4 Absorption, Distribution and Excretion

    Absorption

    Rapidly and well absorbed but may have wide inter- and intra-individual variability. Peak plasma concentrations occur within 4-6 hours of oral administration.

    Route of Elimination

    Metabolites and conjugates are eliminated primarily by the kidneys (60-70%) and also in the feces (10-20%).

    5.5 Metabolism/Metabolites

    Extensively metabolized in the liver. Less than 1% of the orally administered dose appears unchanged in the urine. Metabolites include oxidized and hydroxylated derivates, as well as glucuronic acid conjugates.

    Gliclazide has known human metabolites that include 6-hydroxy-gliclazide, 7-hydroxy-gliclazide, and Methylhydroxygliclazide.

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

    5.6 Biological Half-Life

    10.4 hours. Duration of action is 10-24 hours.

    5.7 Mechanism of Action

    Gliclazide binds to the β cell sulfonyl urea receptor (SUR1). This binding subsequently blocks the ATP sensitive potassium channels. The binding results in closure of the channels and leads to a resulting decrease in potassium efflux leads to depolarization of the β cells. This opens voltage-dependent calcium channels in the β cell resulting in calmodulin activation, which in turn leads to exocytosis of insulin containing secretorty granules.

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    01-Jan-2021
    31-Aug-2024
    KGS
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