In this study, starting from a lead compound discovered by virtual screening, a series of novel heterocyclic substituted benzenesulfonamides were designed and synthesized as new carbonic anhydrase IX (CA IX) inhibitors. Some compounds exhibited potent inhibitory effects against CA IX (in the low...
G protein-gated inward rectifier K+ (GIRK) channels are members of the super-family of proteins known as inward rectifier K+ (Kir) channels and are expressed throughout the peripheral and central nervous systems. Neuronal GIRK channels are the downstream targets of a number of neuromodulators in...
The crystal and molecular structure of p-N,N′-tetraacetylodiaminodurene (TADD) is reported based on the X-ray diffraction studies. The N-acetyl moieties are planar and all N-acetyl groups are perpendicular to the ring plane. Methyl groups both of acetyl moieties and of durene form a number of n...
Two new complexes, [Mn(ppt)2(o-phen)] (1) and [Mn(aptt)(Cl)(o-phen)2]·2Haptt·H2O (2) with 4-phenyl (phenyl-acetyl)-3-thiosemicarbazide (Hppt) and 4-amino-5-phenyl-1,2,4-triazole-3-thiolate (Haptt) have been synthesized containing o-phenanthroline (o-phen) as a coligand. These complexes have be...
The chromone scaffold has been found to be an important tool in the drug discovery process through its relevant pharmacological activities. Chromone carboxamide derivatives synthesized within our group have shown noteworthy results as inhibitors of monoamino oxidase-B and as ligands for adesonin...
3-Methyl-2-oxazolidone has been evaluated as a solvent for the titration of various weak carboxylic acids and phenols. Its high dielectric constant and wide liquid range contribute to its outstanding solvent properties. Tetrabutylammonium hydroxide was the titrant. End-points were determined pot...
3-Methyl-2-oxazolidone was evaluated as a solvent for the titration of selected barbiturates and sulfa drugs. Its high dielectric constant and wide liquid range contribute to its outstanding solvent properties. Tetrabutylammonium hydroxide was used as the titrant. End-points were determined pote...
Two novel series of 4-thiazolidinone derivatives namely 2-substituted-3-{[4-(4-methoxybenzoylamino)benzoyl]amino}-4-thiazolidinones (7a–e) and 2-[4-(4-methoxybenzoylamino)benzoylhydrazono]-3-alkyl-4-thiazolidinones (5a–c) together with 2-[4-(4-methoxybenzoylamino)phenyl]-5-(substituted phenyl)...
The prostaglandins (PG) a group of physiologically active lipid compounds having diverse hormone like effects are important mediators of the body’s response to pain and inflammation, and are formed from essential fatty acids found in cell membranes. This reaction is catalyzed by cyclooxygenase,...
A novel series of 2-(5-methyl-1,3-diphenyl-1H-pyrazol-4-yl)-5-phenyl-1,3,4-oxadiazoles 7(a–m) were synthesized either by cyclization of N′-benzoyl-5-methyl-1,3-diphenyl-1H-pyrazole-4-carbohydrazide 4a using POCl3 at 120 °C or by oxidative cyclization of hydrazones derived from various arylald...
Ten new 2(4-hydroxy-3-benzoyl) benzamide-5-phenyl-1,3,4-oxadiazole derivatives (10a–j) were synthesized by coupling 3-benzoyl-4-hydroxybenzoic acid (5) with 2-amino-5-phenyl-1,3,4-oxadiazoles (9a–j). The structures of these compounds were confirmed by IR, 1H, 13C NMR, and mass spectra, and als...
Potassium N′-(benzoyl)-hydrazine carbodithioate forms novel complexes [Zn3(μ-bhcp)2(py)4] (1) and [Zn(phot)2(en)2] (2) containing newly generated ligands N′-benzoyl hydrazinecarboperthioate (bhcp)3− and 5-phenyl-1,3,4-oxadiazole-2-thione (phot)− which have been characterized by elemental anal...
Histone lysine specific demethylase 1 (LSD1) has been recognized as an important modulator in post-translational process in epigenetics. Dysregulation of LSD1 has been implicated in the development of various cancers. Herein, we report the discovery of the hit compound 8a (IC50 = 3.93 μmol/L) a...
Thiazolo[5,4-d]pyrimidines are important class of heterocyclic compounds possessing diverse range of biological activities. Herein, we report an efficient synthesis of thiazolo[5,4-d]pyrimidines using recyclable KF/alumina catalyst. The reaction of 4,6-dichloro-5-aminopyrimidine with isothiocyan...
The present study involves the development of certain thiazolo[3,2-a]pyrimidin-5-ones linked through an ethylene bridge to various amines. The newly synthesized compounds 4–6(a–c) were subjected to in vitro anticancer evaluation using NCI antitumor screening. The target compounds showed observ...
In this study a new set of thiazolo[5,4-d]pyrimidine derivatives was synthesized. These derivatives bear different substituents at positions 2 and 5 of the thiazolopyrimidine core while maintaining a free amino group at position-7. The new compounds were tested for their affinity and potency at ...
Publisher SummaryThis chapter reviews the chemistry, biological significance, and uses of 1,2,4-triazolo- and tetrazolo-[x,y-zl pyrimidines. The arrangement of each ring follows the order of the site of fusion on the pyrimidine ring, denoted by the letter t, and the site of fusion on the triazol...
The reaction between 5-amino-4-imino-1(2)-substituted-1(2)H-4,5-dihydropyrazolo[3,4-d]pyrimidines and several commercially available reactants afforded new heterocycles with a conserved pyrazolo[3,4-d]pyrimidine nucleus. The key intermediates employed proved to be suitable compounds by virtue of...
Direct fluorination at the 2′-arabino-position of a pyrimidine nucleoside has been a long-standing challenge, yet we recently reported such a stereospecific fluorination for the first time in the synthesis of [18F]FMAU, albeit in low yields. Herein we report the results of an investigation on s...
5-Pivaloyloxymethyluridine and its 2-thio analogue have been utilized as convenient substrates for the synthesis of various 5-methyluridines (xm5U) and 5-methyl-2-thiouridines (xm5s2U). The pivaloyloxy group (OPiv) located at the pseudobenzylic position was effectively substituted with a series ...
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