Etahalon
 | |
| IUPAC ime | |
|---|---|
3-(2-etilfenil)-2-metil-hinazolin-4-on | |
| Klinički podaci | |
| Drugs.com | Monografija |
| Identifikatori | |
| CAS broj | 7432-25-9  |
| ATC kod | none |
| PubChem | CID 23914 |
| ChemSpider | 22357 |
| UNII | HFS3HB32J7 |
| Hemijski podaci | |
| Formula | C17H16N2O |
| Molarna masa | 264,322 |
| |
| |
Etahalon (Aolan, Atinazon, Etinazon[1]) je GABAergik klase hinazolinona i analog je metahalonu koji je razvijen tokom 1960-ih[2][3] i plasiran uglavnom u Francuskoj i nekim drugim evropskim zemljama. Ima sedativna, hipnotička, mišićna relaksantna i depresivna svojstva centralnog nervnog sistema koja su rezultat njegove agonističke aktivnosti na β-podtipu GABAA receptora, i korišćen je za lečenje nesanice.
Osobine
[уреди | уреди извор]Etahalon je organsko jedinjenje, koje sadrži 17 atoma ugljenika i ima molekulsku masu od 264,322 Da.
| Osobina | Vrednost |
|---|---|
| Broj akceptora vodonika | 2 |
| Broj donora vodonika | 0 |
| Broj rotacionih veza | 2 |
| Particioni koeficijent[4] (ALogP) | 3,6 |
| Rastvorljivost[5] (logS, log(mol/L)) | -4,4 |
| Polarna površina[6] (PSA, Å2) | 32,7 |
Reference
[уреди | уреди извор]- ^ Pflegel P, Wagner G (новембар 1967). „[On the polarography of 2-methyl-3-(2-methylphenyl)-3,4-dihydroquinazolinone-(4) methaqualone, Dormutil) and 2-methyl-3-(2-ethylphenyl-3,4-dihydroquinazolinone-(4) (ethinazone, Aolan). 5. Polarography of heterocyclic compounds]” [On the Polarography of 2-Methyl-3-(2-methylphenyl)-3,4-dihydroquinazolinone-(4) (methaqualone, Dormutil) and 2-methyl-3-(2-ethylphenyl-3,4-dihydroquinazolinone-(4) (ethinazone, Aolan). 5. Polarography of Heterocyclic Compounds]. Die Pharmazie (на језику: German). 22 (11): 643—50. PMID 5619478.
- ^ GB patent 936902, "Quinazolinone Derivatives", issued 1963-09-18, assigned to Beiersdorf
- ^ Parmar SS, Kishor K, Seth PK, Arora RC (јануар 1969). „Role of alkyl substitution in 2,3-disubstituted and 3-substituted 4-quinazolones on the inhibition of pyruvic acid oxidation”. Journal of Medicinal Chemistry. 12 (1): 138—41. PMID 4303122. doi:10.1021/jm00301a035.
- ^ Ghose, A.K.; Viswanadhan V.N. & 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. PMID 11749573. doi:10.1021/ci000392t.
- ^ 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. PMID 11020286. doi:10.1021/jm000942e.
Literatura
[уреди | уреди извор]- Hardman JG, Limbird LE, Gilman AG (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10. изд.). New York: McGraw-Hill. ISBN 0071354697. doi:10.1036/0071422803.
- Thomas L. Lemke; David A. Williams, ур. (2007). Foye's Principles of Medicinal Chemistry (6. изд.). Baltimore: Lippincott Willams & Wilkins. ISBN 0781768799.
