Modification of 5-position phenyl of 1,2,4-triazole ring.

Compound #	X	R	Binding affinity					Activity
			Ki (nM)					EC50 (nM)
			SST1	SST2A	SST3	SST4	SST5	SST4
179	—	—	—	>10 000	—	827.6	—	—
158	H	H	>10 000	>10 000	>10 000	12.0	>10 000	16.5
4 a	3,4-Cl2	H	4750	>10 000	6628	19.8	>10 000	6.8
165	3,5-Cl2	H	—	6975	—	51.7	—	17.0
160	3,5-F2	H	>10 000	>10 000	>10 000	16.2	>10 000	8.8
161	2-Cl	H	>10 000	>10 000	>10 000	21.5	>10 000	17.3
162	3-Cl	H	6929	>10 000	>10 000	5.1	>10 000	7.3
163	4-Cl	H	—	>10 000	—	37.5	—	19.3
159	3-F	H	>10 000	>10 000	>10 000	12.4	>10 000	21.0
166	3-Br	H	4744	>10 000	>10 000	5.5	>10 000	4.4
167	3-CF3	H	5309	>10 000	>10 000	3.2	>10 000	6.1
169	3-CN	H	—	>10 000	—	30.3	—	75.8
170	3-NO2	H	—	>10 000	—	36.6	—	98.4
171	2-OCH3	H	>10 000	>10 000	>10 000	39.5	>10 000	28.9
172	3-OCH3	H	>10 000	>10 000	>10 000	7.7	>10 000	15.6
173	4-OCH3	H	—	>10 000	—	267.2	—	—
174	3-OCF3	H	4076	>10 000	—	14.9	—	55.0
175	3-OBn	H	—	>10 000	—	386.6	—	254.5
176	3-SO2CH3	H	3653	>10 000	>10 000	7.0	>10 000	22.7
177	4-C6H5	H	—	>10 000	—	945.3	—	—
164	3,4-Cl2	CH3	3172	>10 000	6989	40.4	>10 000	21.3
168	3-CF3	CH3	2236	>10 000	>10 000	11.0	>10 000	10.7

^aRef. 58