2-Aminothiophene scaffolds: Diverse biological and pharmacological attributes in medicinal chemistry

2-Aminothiophene scaffolds: Diverse biological and pharmacological attributes in medicinal chemistry
Khurshed Bozorov ^a,b, Li Fei Nie ^a,c, Jiangyu Zhao ^a, and Haji A. Aisa ^a,1
a Key Laboratory of Plant Resources and Chemistry in Arid Regions, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, 40-1 South Beijing Rd, Urumqi, 830011, PR China
^b Institute of the Chemistry of Plant Substances, Academy of Sciences of Uzbekistan, Mirzo Ulugbek str. 77, Tashkent, 100170, Uzbekistan
^c University of Chinese Academy of Sciences, 19 A Yuquan Rd, Beijing, 100049, PR China

ABSTRACT
2-Aminothiophenes are important five-membered heterocyclic building blocks in organic synthesis, and the chemistry of these small molecules is still developing based on the discovery of cyclization by Gewald. Another attractive feature of 2-aminothiophene scaffolds is their ability to act as synthons for the synthesis of biological active thiophene-containing heterocycles, conjugates and hybrids. Currently, the biological actions of 2-aminothiophenes or their 2-N-substituted analogues are still being investigated because of their various mechanisms of action (e.g., pharmacophore and pharmacokinetic properties). Likewise, the 2-aminothiophene family is used as diverse promising selective inhibitors, receptors, and modulators in medicinal chemistry, and these compounds even exhibit effective pharmacological properties in the various clinical phases of appropriate diseases. In this review, major biological and pharmacological reports on 2-aminothiophenes and related compounds have been highlighted; most perspective drug-candidate hits were selected for discussion and described, along with additional synthetic pathways. In addition, we focused on the literature dedicated to 2-aminothiophenes and 2-N-substituted derivatives, which have been published from 2010-2017.