ChemInform Abstract: Substituted 2‐Aminothiophenes: Synthesis, Properties and Applications

Abstract

Review: 188 refs.

Improvement of Solubility and Antifungal Activity of a New Aminothiophene Derivative by Complexation with 2-Hydroxypropyl-β-cyclodextrin

“…Solubility data were fitted using linear regression. Assuming the formation of a complex with 1:1 stoichiometric ratio, the apparent stability constant (K 1:1 ) of 6CN10 was calculated from the linear relationship between the molar concentration of 6CN10 in the solution medium as a function of the HP-β-CD molar concentration according to equation 1,14 where the S 0 is the solubility of the 6CN10 in the absence of HP-β-CD. The stability constant (K 1:2 ) of 6CN10 was calculated …”

“…The proton spin-lattice relaxation time T 1 was measured using the saturation method in a spectrometer working at 400 MHz. 1 H chemical shifts were referenced to DMSO (2.50 ppm).…”

“…1 This class of heterocycles has attracted great interest from researchers due to their great versatility as precursors of molecules with pharmacological properties. 2 6CN10 is a 2-aminothiophene derivative synthesized via two-step reaction, starting with the obtainment of 2-amino-4,5,6,7-tetrahydro-4H-benzo [b]thiophene-3-carbonitrile through the Gewald reaction, followed by condensation with 4-nitro-benzaldehyde to produce the 2-[(4-nitrobenzylidene)amino]-4,5,6,7-tetrahydro-4H-benzo [b]thiophene-3-carbonitrile, called 6CN10 (Table 1).…”

Synthesis and Structure Activity Relationship of Some Indole Derivatives as Potential Anti-inflammatory Agents

“…[46][47][48] Research in-dicated that α-amino ketones used for the preparation of o-amino-cyanopyrroles were usually obtained in situ [49][50][51] via the reaction of α-hydroxy ketones with amines in acid medium, [52][53][54][55] or via the reaction of α-halo ketones with either amines and/or α-amino acids. 56 As previously mentioned, α-hydroxy ketones and α-halo ketones, malononitriles or suitable substituted alkylidenemalonitrile and primary amines constituted essential components for the synthesis of o-amino-cyanopyrrole derivatives.…”

Uses of Cyclohexan-1,4-dione for the Synthesis of 2-Amino-4,5-dihydrobenzo[<i>b</i>]thiophen-6(7<i>H</i>)-one Derivatives with Anti-proliferative and Pim-1 Kinase Activities

“…[11][12][13] Various thiophene derivatives are produced by molecular modifications through varied synthesis routes that result in increases in specificity and thus safety profiles. 14,15) Within the thiophenic family, the 2-amino-thiophenes have been well reported. In recent drugs investigations, they acquired a particular importance due to the innovations in their synthesis (Gewald reaction), availability, stability, and structural simplicity that allow them to be important scaffolds in chemical and therapeutic products; like the top selling drugs olanzepine and tinoridine.…”