Arsthinol Explained

Arsthinol (INN) is an antiprotozoal agent. It was synthesized for the first time in 1949 by Ernst A.H. Friedheim by complexation of acetarsol with 2,3-dimercaptopropanol (British anti-Lewisite)[1] and has been demonstrated to be effective against amoebiasis and yaws. It was marketed a few years later by Endo Products (Balarsen, Tablets, 0.1 g).[2]

Among trivalent organoarsenicals, arsthinol was considered very well tolerated.[3] Recently, it was studied for its anticancer activity.[4] [5]

Identification

Arsthinol has IUPAC name of N-[2-hydroxy-5-[4-(hydroxymethyl)-1,3,2-dithiarsolan-2-yl]phenyl] acetamide with a molecular formula of C11H14AsNO3S2 and is represented by the SMILES notation, CC(=O)NC1=C(C=CC(=C1)[As]2SCC(S2)CO)O.[6]

Properties

The molecular weight of Arsthinol is 347.3 g/mol, with a hydrogen bond donor count of 3 and a hydrogen bond acceptor count of 5. It has 3 rotatable bonds, an exact mass of 347.279 g/mol, and a monoisotopic mass of 346.963105 g/mol. The topological polar surface area is 120Ų, and the compound contains 18 heavy atoms. It has no formal charge, a complexity of 308, and contains no isotope atoms. There are no defined atom stereocenters, but there is 1 undefined atom stereocenter. The compound has no defined or undefined bond stereocenters, includes 1 covalently bonded unit, and is canonicalized.[7] [8]

Notes and References

  1. Friedheim . Ernst AH . 1949 . A Five Day Peroral Treatment of Yaws with STB, a New Trivalent Arsenical . . s1-29 . 2 . 185–188 . 10.4269/ajtmh.1949.s1-29.185 . 18116845 .
  2. Anonyme . 1953 . New and nonofficial remedies; arsthinol . . 152 . 531 .
  3. Brown . CH . Gebhart . WF . Reich . A . 1956 . Intestinal amebiasis: incidence, symptoms, and treatment with arsthinol (Balarsen) . . 160 . 5. 360–363 . 10.1001/jama.1956.02960400018005. 13278204 .
  4. Gibaud . S . Alfonsi . R . Mutzenhardt . P . et al . 2006 . (2-Phenyl-[1, 3, 2] dithiarsolan-4-yl)-methanol derivatives show in vitro antileukemic activity . . 691 . 5. 1081–1084 . 10.1016/j.jorganchem.2005.11.007.
  5. Becherirat . S. . Lanhers . M.-C. . Socha . M. . Yemloul . M. . Astier . A. . Loboda . C. . Aniceto . N. . Gibaud . S. . 2013 . The antitumor effects of an arsthinol-cyclodextrin complex in an heterotopic mouse model of glioma . . 85. 3. 560–568. 10.1016/j.ejpb.2013.06.021 . 23831266 .
  6. Web site: PubChem . PubChem . 2024-10-17 . pubchem.ncbi.nlm.nih.gov . en.
  7. Web site: PubChem . Arsthinol . 2024-10-17 . pubchem.ncbi.nlm.nih.gov . en.
  8. Web site: arsthinol C11H14AsNO3S2 . 2024-10-17 . www.chemspider.com.