Archives of Biological Sciences 2015 Volume 67, Issue 1, Pages: 103-109
https://doi.org/10.2298/ABS141104011T
Full text ( 527 KB)
Cited by
The influence of certain molecular descriptors of fecal elimination of angiotensin II receptor antagonists
Trbojević-Stanković Jasna B. (School of Medicine, Belgrade + Clinical Hospital Center "Dr Dragiša Mišović", Department of Dialysis, Belgrade)
Odović Jadranka V. (Faculty of Pharmacy, Department of Analytical Chemistry, Belgrade)
Jelić Ratomir M. (Faculty of Medicinal Science, Kragujevac)
Nesić Dejan M. (School of Medicine, Institute of Medical physiology, Belgrade)
Stojimirović Biljana B. (School of Medicine, Belgrade + Clinical Center of Serbia, Clinic of Nephrology, Belgrade)
Angiotensin II receptor antagonists (ARBs) modulate the function of the
renin-angiotensin-aldosterone system and are commonly prescribed
antihypertensive drugs, especially in patients with renal failure. In this
study, the relationship between several molecular properties of seven ARBs
(candesartan, eprosartan, irbesartan, losartan, olmesartan, telmisartan,
valsartan) and their fecal elimination data obtained from the literature were
investigated. The ARB molecular descriptors were calculated using three
software packages. Simple linear regression analysis showed the best 2
correlation between fecal elimination data and lipophilicity descriptor,
ClogP values (R2 = 0.725). Multiple linear regression was applied to examine
the correlation of ARBs’ fecal elimination data with their lipophilicity and
one additional, calculated descriptor. The best correlation (R2 = 0.909 with
an acceptable probability value, P <0.05) was established between the ARB
fecal elimination data and their lipophilicity and aqueous solubility data.
Applying computed molecular descriptors for evaluating drug elimination is of
great importance in drug research.
Keywords: angiotensin II receptor antagonists, lipophilicity, aqueous solubility, fecal elimination