Elucidation of structure-activity relationships of 2-amino-3-benzoylthiophenes: Study of their allosteric enhancing vs. antagonistic activity on adenosine A1 receptors

International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and Classification of Adenosine Receptors—An Update

“…The prototypical benzoylthiophene to act as an A 1 receptor allosteric modulator is (2-amino-4,5-dimethyl-3-thienyl)(3-(trifluoromethyl)phenyl)-methanone (PD81,723; Fig. 10), and many analogs have been prepared (Kourounakis et al, 2000;Baraldi et al, 2007a,b). The 2-amino-3-carbonylthiophene moiety is required as a minimal pharmacophore.…”

International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and Classification of Adenosine Receptors—An Update

“…The prototypical benzoylthiophene to act as an A 1 receptor allosteric modulator is (2-amino-4,5-dimethyl-3-thienyl)(3-(trifluoromethyl)phenyl)-methanone (PD81,723; Fig. 10), and many analogs have been prepared (Kourounakis et al, 2000;Baraldi et al, 2007a,b). The 2-amino-3-carbonylthiophene moiety is required as a minimal pharmacophore.…”

Gewald reaction: synthesis, properties and applications of substituted 2-aminothiophenes

“…Because the structure-based drug design program through substituted 2-aminothiophenes has been investigated broadly, up to this date there are many other research works dealing with the synthesis, pharmacology and application of thiophene-based structures in medicinal chemistry. 7,[12][13][14]36,37,51,69,100,101,[119][120][121][122][123][124][125][126][127] It is no doubt, that this area of Gewald-like thiophene derivatives exhibits the highest progress in a scope and utilization.…”

Allosteric Modulation of Purine and Pyrimidine Receptors

“…Many analogues have been prepared and found to have comparable or more favorable activity as allosteric modulators (Kourounakis et al, 2000; Gao et al, 2005; Baraldi et al, 2007; Baraldi et al, 2003; Baraldi et al, 2004; Romagnoli et al, 2006). The 2-amino-3-carbonyl thiophene moiety is required as a minimal pharmacophore (shown in box).…”

International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and Classification of Adenosine Receptors—An Update

“…The prototypical benzoylthiophene to act as an A 1 receptor allosteric modulator is (2-amino-4,5-dimethyl-3-thienyl)(3-(trifluoromethyl)phenyl)-methanone (PD81,723; Fig. 10), and many analogs have been prepared (Kourounakis et al, 2000;Baraldi et al, 2007a,b). The 2-amino-3-carbonylthiophene moiety is required as a minimal pharmacophore.…”

Gewald reaction: synthesis, properties and applications of substituted 2-aminothiophenes

“…Because the structure-based drug design program through substituted 2-aminothiophenes has been investigated broadly, up to this date there are many other research works dealing with the synthesis, pharmacology and application of thiophene-based structures in medicinal chemistry. 7,[12][13][14]36,37,51,69,100,101,[119][120][121][122][123][124][125][126][127] It is no doubt, that this area of Gewald-like thiophene derivatives exhibits the highest progress in a scope and utilization.…”

Allosteric Modulation of Purine and Pyrimidine Receptors

“…Many analogues have been prepared and found to have comparable or more favorable activity as allosteric modulators (Kourounakis et al, 2000; Gao et al, 2005; Baraldi et al, 2007; Baraldi et al, 2003; Baraldi et al, 2004; Romagnoli et al, 2006). The 2-amino-3-carbonyl thiophene moiety is required as a minimal pharmacophore (shown in box).…”

International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and Classification of Adenosine Receptors—An Update

“…The prototypical benzoylthiophene to act as an A 1 receptor allosteric modulator is (2-amino-4,5-dimethyl-3-thienyl)(3-(trifluoromethyl)phenyl)-methanone (PD81,723; Fig. 10), and many analogs have been prepared (Kourounakis et al, 2000;Baraldi et al, 2007a,b). The 2-amino-3-carbonylthiophene moiety is required as a minimal pharmacophore.…”

Gewald reaction: synthesis, properties and applications of substituted 2-aminothiophenes

“…Because the structure-based drug design program through substituted 2-aminothiophenes has been investigated broadly, up to this date there are many other research works dealing with the synthesis, pharmacology and application of thiophene-based structures in medicinal chemistry. 7,[12][13][14]36,37,51,69,100,101,[119][120][121][122][123][124][125][126][127] It is no doubt, that this area of Gewald-like thiophene derivatives exhibits the highest progress in a scope and utilization.…”

Allosteric Modulation of Purine and Pyrimidine Receptors

“…Many analogues have been prepared and found to have comparable or more favorable activity as allosteric modulators (Kourounakis et al, 2000; Gao et al, 2005; Baraldi et al, 2007; Baraldi et al, 2003; Baraldi et al, 2004; Romagnoli et al, 2006). The 2-amino-3-carbonyl thiophene moiety is required as a minimal pharmacophore (shown in box).…”