Table 1. Structure and Antimycobacterial Activity of the 25 N,N′-Diphenylterephthalamide Derivatives Belonging to the Focused Small Library Built around the Hit Compound NSC55150 (22).
compound | R | MIC (μg/mL) |
---|---|---|
1, NSC73489 | H | 20–40 |
2, NSC164131 | o-F | >40 |
3, NSC111339 | p-F | >40 |
4, NSC73488 | p-Cl | >40 |
5, NSC204225 | m,p-di-Cl | >40 |
6, NSC71193 | p-Me | >40 |
7, NSC110298 | p-Et | >40 |
8, NSC110302 | m-Cl,p-Me | >40 |
9, NSC110317 | p-FSO2 | >40 |
10, NSC55146 | p-C(=NH)NH2 | >40 |
11, NSC53313 | p-C(=NH)NHCH3 | 0.31 |
12, NSC70138 | p-C(=NH)NHCH2CH3 | 0.62 |
13, NSC71201 | p-C(=NH)NH(CH2)2CH3 | 0.62 |
14, NSC80122 | p-C(=NH)NHCH(CH3)2 | 0.62 |
15, NSC80976 | p-C(=NH)NH(CH2)3CH3 | 1.25 |
16, NSC80975 | p-C(=NH)NH(CH2)5CH3 | 5 |
17, NSC53312 | p-C(=NCH3)NHCH3 | 0.62 |
18, NSC64897 | p-C(=NH)NHNH2 | >40 |
19, NSC77889 | 10 | |
20, NSC55148 | >10 | |
21, NSC55147 | >40 | |
22, NSC55150 | p-CH2C(=NH)NH2 | 1 |
23, NSC55151 | p-NHC(=NH)NH2 | 0.16 |
24, NSC72583 | 2.5 | |
25, NSC65376 | 0.62 |