diamide and squaric-acid

diamide has been researched along with squaric-acid* in 3 studies

Other Studies

3 other study(ies) available for diamide and squaric-acid

ArticleYear
Piperazine squaric acid diamides, a novel class of allosteric P2X7 receptor antagonists.
    European journal of medicinal chemistry, 2021, Dec-15, Volume: 226

    The P2X7 receptor (P2X7R) stands out among the purinergic receptors due to its strong involvement in the regulation of tumor growth and metastasis formation as well as in innate immune responses and afferent signal transmission. Numerous studies have pointed out the beneficial effects of P2X7R antagonism for the treatment of a variety of cancer types, inflammatory diseases, and chronic pain. Herein we describe the development of novel P2X7R antagonists, incorporating piperazine squaric diamides as a central element. Besides improving the antagonists' potency from pIC

    Topics: Cyclobutanes; Diamide; Dose-Response Relationship, Drug; HEK293 Cells; Humans; Molecular Structure; Piperazine; Purinergic P2X Receptor Antagonists; Receptors, Purinergic P2X; Structure-Activity Relationship; Tumor Cells, Cultured

2021
Crystal structures and spectroscopic properties of ester amide and diamide of squaric acid with prolinamide.
    Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 2009, Volume: 72, Issue:3

    We report the synthesis, spectroscopic and structural elucidation of two prolinamide derivatives of squaric acid, i.e. prolinamide ester amide of squaric acid ethyl ester (1) and prolinamide diamide of squaric acid dihydrate (2). Both compounds crystallize in non-centrosymmetric space groups, monoclinic P2(1) (1) and orthorhombic P2(1)2(1)2(1) (2), respectively. For first time in the literature the crystal structure of homodiamide of amino acid amide of squaric acid is reported. The data for heterodiamides is also absent. Supramolecular zig-zag chains by hydrogen bonds of H(2)N-C=O ..., HNH (3.020 A) and HNH ..., OC((S(q))) (2.972 A) types with the participation of amide and squaric acid (S(q)) fragments, -CO=NH(2) and O=C((S(q))) are refined in (1). A helix supramolecular structure is formed in (2) by moderate intermolecular HNH ... O=C(NH(2)) hydrogen bond with length of 2.947A. The two crystallographical non-equivalent water molecules stabilized the helix by interactions of types HOH...OC((Sq)) (2.917A), HOH...O=C(NH(2)) (2.899A), H(2)O...NH(2)(C=O) (2.972A), respectively. Optical and magnetic properties are investigated with a view to explain the correlation structure-properties of the newly synthesized molecules.

    Topics: Calorimetry, Differential Scanning; Chromatography, High Pressure Liquid; Crystallography; Cyclobutanes; Diamide; Esters; Hydrogen Bonding; Magnetic Resonance Spectroscopy; Models, Molecular; Molecular Conformation; Molecular Structure; Molecular Weight; Proline; Protein Conformation; Protein Structure, Secondary; Spectrophotometry, Infrared; Tandem Mass Spectrometry; Thermogravimetry; Water; X-Ray Diffraction

2009
Design and synthesis of a novel peptidomimetic inhibitor of HIV-1 Tat-TAR interactions: squaryldiamide as a new potential bioisostere of unsubstituted guanidine.
    Bioorganic & medicinal chemistry letters, 2005, Oct-01, Volume: 15, Issue:19

    By performing RNA-targeted structure-activity relationship studies, we discovered a novel peptidomimetic containing squaryldiamide as a potential bioisostere replacement for guanidine that binds transactivation responsive RNA with high affinity.

    Topics: Anti-HIV Agents; Cyclobutanes; Diamide; Drug Design; Gene Products, tat; Guanidine; HIV Long Terminal Repeat; HIV-1; Molecular Mimicry; Oligopeptides; RNA-Binding Proteins; Structure-Activity Relationship; tat Gene Products, Human Immunodeficiency Virus

2005