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. 2020 Aug 25;25(17):3864. doi: 10.3390/molecules25173864

Table 4.

Opioid and benzodiazepine receptor binding of imidazodiazepine oxazoles.

graphic file with name molecules-25-03864-i004.jpg

Entry Name R1 R2 R3 X KOR 1 % MOR 1 % DOR 1 % BZR 1 % KOR
(Ki, nM) 		BZR
(Ki, nM)
1 SH-I-85 Br H H C-F 91 16 33 99 162 11
2 GL-III-76 Br H (S) C-F 83 3 0 100 221 120
3 GL-III-36 Br H (R) C-F 88 0 12 86 246 319
4 KRM-II-18B HC≡C H H C-F 89 11 20 97 361 38
5 KRM-III-59 Br Me H C-F 73 0 11 96 408 20
6 GL-III-73 HC≡C H (R) C-F 74 12 4 65 449 602
7 GL-III-78 HC≡C H (S) C-F 74 10 9 101 451 261
8 KRM-II-73 Br H H C-H 83 11 32 97 736 45
9 KRM-III-66 Br Me H C-H 67 12 11 86 756 49
10 KRM-III-65 HC≡C Me H C-F 64 0 16 96 879 45
11 KRM-II-82 HC≡C H H C-H 78 5 20 95 1203 96
12 KRM-II-97 Br H H N 62 18 8 93 1959 140
13 KRM-III-67 HC≡C H H N 48 30 3 71 - 2 144
14 KRM-II-81 Br Me H N 46 7 15 86 - 2 294
15 KRM-III-79 HC≡C Me H N 9 32 1 81 - 2 308

1 Percent inhibition at 10,000 nM, 2 dose response was carried out only for compounds with an inhibition of >50%.