Naslov
Lipophilicity and metabolic stability determination on naphtho[1, 2-d]/[2, 1-d]oxazoles

Autori
Kelava, Vanja ; Šagud, Ivana ; Škorić, Irena

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Skup
XXV EFMC International Symposium on Medicinal Chemistry

Mjesto i datum
Ljubljana, Slovenija, 02.09.2018. - 06.09.2018

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
lipophilicity ; metabolic stability ; naphtho[1, 2-d]/[2, 1-d]oxazoles

Sažetak
Lipophilicity and metabolic stability was determined on a series of [1, 2/2, 1-d]- naphtooxazoles. Compound were synthetized by transformation of 4/5-styryloxazoles into [1, 2/2, 1-d]-naphtooxazoles by reaction of photochemical cyclization (1). Correlation was made based on a structural properties of compounds. In order to determine the lipophilicity range of these compounds, Chromatographic Hidrophobicity Index was measured (2). It was determined that most compounds have favorable lipophilicity for targeting central nervous system diseases. Metabolic stability was also measured and it was determined that most compounds did not have favorable stability. In the future consideration should be made on how to stabilize series of these compounds by making structural adjustments. 1. I. Šagud, F. Faraguna, Ž. Marinić, M. Šindler-Kulyk, J. Org. Chem. 76 (2011) 2904- 2908. 2. Valko K. in: Borchardt, R., Kerns, E., Lipinski, C., Thakker, D., & Wang, B. (Eds.). Pharmaceutical profiling in drug discovery for lead selection (Vol. 1), AAPS press, 2004, pp. 127-182.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Interdisciplinarne prirodne znanosti, Farmacija

POVEZANOST RADA