engleski

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

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.

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

nije evidentirano