Application of ELISA Technique and Human Microsomes in the Search for 11β-Hydroxysteroid Dehydrogenase Inhibitors

Table 1

N-allyl-2-thiouracil derivatives.

No.		M.p. of 1 – 6; / lit. M.p.; (°C)	% of inhibition; 11β-HSD1; 10μM^1	% of inhibition; 11β-HSD2; 10μM^1
1.		192.5-194 /193.5-194.5 [34]	8.82±0.86	28.08±1.02
2.		153-154 / 154.5-155 [35]	30.88±1.29	19.18±1.45
3.		204-205.5 /201-203.5 [35]	35.29±2.01	37.33±2.03
4.		176-177.5 /177.5-179.5 [34]	39.71±1.94	24.66±2.09
5.		121-122 / 119.5-121 [36]	30.88±1.53	16.78±1.24
6.		188-189.5 / 189-191 [36]	38.24±1.85	23.29±1.35
7.	carbenoxolone	-	89.70±3.45	15.06±2.06
8.	18β-glycyrrhitinic acid	-	88.24±2.05	10.96±3.01

inhibition of 11β -HSD1 and 11β –HSD2 was determined with inhibitors concentration 10 μM from three independent determinations.