Benzolamide
Benzolamide Basic information
- Product Name:
- Benzolamide
- Synonyms:
-
- 5-(phenylsulfonylamino)-1,3,4-thiadiazole-2-sulfonamide
- 2-benzenesulfonamido-1,3,4-thiadiazole-5-sulfonamide
- Benzolamide
- 1,3,4-Thiadiazole-2-sulfonamide, 5-[(phenylsulfonyl)amino]-
- 5-(Phenylsulfonamido)-1,3,4-thiadiazole-2-sulfonamide
- W 1803
- W-1803
- Benzolamide,Inhibitor,Carbonate dehydratase,seizures,CAS3,glaucoma,inhibit,Carbonic Anhydrase
- CAS:
- 3368-13-6
- MF:
- C8H8N4O4S3
- MW:
- 320.37
- Mol File:
- 3368-13-6.mol
Benzolamide Chemical Properties
- Melting point:
- 239.5°C (rough estimate)
- Boiling point:
- 585.9±33.0 °C(Predicted)
- Density
- 1.6772 (rough estimate)
- refractive index
- 1.5690 (estimate)
- storage temp.
- 4°C, protect from light
- solubility
- DMSO : 250 mg/mL (780.35 mM; Need ultrasonic)
- form
- Solid
- pka
- 4.42±0.40(Predicted)
- color
- White to light yellow
- Water Solubility
- 384.4mg/L(25 ºC)
Benzolamide Usage And Synthesis
Uses
Benzolamide (CL11366) is a potent carbonic anhydrase (CA) inhibitor, with Kis of 15 nM, 9 nM, 94 nM and 78 nM for hCA I, hCA II, EcoCAγ and VchCAγ, respectively. Benzolamide also inhibits CAS3, with a Ki of 54 nM. Benzolamide can be used for the research of glaucoma and seizures[1][2][3].
in vivo
Benzolamide (90 μmol/kg; i.p.) decreases brain pH and suppresses electrographic post-asphyxia seizures in rats[3].
| Animal Model: | Male and female Wistar Han rats (11-day-old)[3] |
| Dosage: | 90 μmol/kg |
| Administration: | A single i.p. |
| Result: | Induced a fast brain acidosis of a comparable magnitude. Suppressed electrographic seizures after asphyxia by slowing down the recovery of brain pH. |
IC 50
CA Ⅱ
References
[1] Prete SD, et, al. Escherichia coli γ-carbonic anhydrase: characterisation and effects of simple aromatic/heterocyclic sulphonamide inhibitors. J Enzyme Inhib Med Chem. 2020 Dec;35(1):1545-1554. DOI:10.1080/14756366.2020.1800670
[2] Vullo D, et, al. Sulfonamide Inhibition Studies of the β-Class Carbonic Anhydrase CAS3 from the Filamentous Ascomycete Sordaria macrospora. Molecules. 2020 Feb 25;25(5):1036. DOI:10.3390/molecules25051036
[3] Pospelov AS, et, al. Carbonic anhydrase inhibitors suppress seizures in a rat model of birth asphyxia. Epilepsia. 2021 Jun 27. DOI:10.1111/epi.16963
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