14397-16-1Relevant articles and documents
Synthesis of carboxamide and sulfonyl carboxamide linked heterocycles under green conditions
Gaddam, Lakshmi Teja,Thata, Sreenivasulu,Adivireddy, Padmaja,Venkatapuram, Padmavathi
, p. 43 - 54 (2019/11/11)
Direct coupling of heteroaldehydes with heteroaryl amines / sulfonylamines is performed under green conditions using PEG-400 in the presence of oxidant CCl3CN/H2O2. The presence of electron withdrawing substituents on heteroaldehydes increased the yield. Further heteroaryl amines favor the reaction when compared with heteroaryl sulfonylamines.
2-AMINOTHIAZOLE DERIVATIVES AND METHODS OF PREPARING AND USING THE SAME
-
, (2014/02/15)
2-aminothiazole derivatives represented by formula (I), where R1 and R2 represent cycloalkyls, respectively; or R1 represents a substituted aromatic group, and R2 represents H, a C1-C11 alkyl, —CH2Ph (benzyl), or a methyl ether including a C1-C11 alkyl. R3 is a substituent including an amino group. X represents a carbonyl or a methylene and n is an integer from 0 to 5.
Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-Ribose) polymerase-1 inhibitors
Zhang, Wen-Ting,Ruan, Jin-Lan,Wu, Peng-Fei,Jiang, Feng-Chao,Zhang, Li-Na,Fang, Wei,Chen, Xiang-Long,Wang, Yue,Cao, Bao-Shuai,Chen, Gang-Ying,Zhu, Yi-Jing,Gu, Jun,Chen, Jian-Guo
experimental part, p. 718 - 725 (2009/12/27)
A series of novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors were designed within 2-aminothiazole analogues (4-10) based on a constructed three-dimensional pharmacophore model. After synthesis, the inhibitory effect on PARP-1 activity and the cytoprotective action of these compounds were tested and evaluated. Among them, compounds 4-6 and 10 appeared to be potent PARP-1 inhibitors with IC50 values less than 1 μM, which had been perfectly predicted by pharmacophore model. These compounds proved to be highly potent against cell injury induced by H2O2 and oxygen-glucose deprivation (OGD) in PC12 cells. These novel 2-aminothiazole analogues are potentially applicable as neuroprotective agents for the treatment of neurological diseases.