نتایج جستجو برای: 4 hydroxyquinazoline
تعداد نتایج: 1303594 فیلتر نتایج به سال:
From the ethyl acetate extract of the strain Streptomyces sp. isolate GW23/1540, besides 16 known products, several 1H-quinazolin-4-one derivatives were isolated. (SR)-2-(1-Hydroxyethyl)-2-methyl-2,3-dihydro-1H-quinazolin-4-one (4) and (RR)-2-(1-hydroxyethyl)-2-methyl-2,3-dihydro-1H-quinazolin-4-one (5) are new natural products. 2-Methyl-3H-quinazolin-4-one (2) and 1H-quinazoline-2,4-dione (3) ...
4(3H)-Quinazolinones 1 are known for more than a century [1]. Molecules based on quinazoline and quinazolinone exhibit a multitude of interesting pharmacological activities [2], including anticonvulsant, antibacterial and antidiabetic activity [3,4]. The important natural and synthetic 4(3H)-quinazolinones include l-vasicinone 2 [5], chrysogine 3 [6], methaquinalon 4 [7] – a sedative, piriqualo...
Heterocyclic scaffold has been under discovery due to their considerable therapeutic and medicinal importance. One of such heterocycles 2-pyrimidinone, while not naturally occurring, are receiving increased attention because of their wide-ranging biological activity like, an efficient inhibitor of DNA synthesis in E. coli, inhibitors of the enzyme cytidinedeaminase, and as metaphase inhibitors....
A novel class of 3-phenyl-2-styryl-3H-quinazolin-4-one Hsp90 inhibitors with in vitro anti-tumor activity are identified by structure-based virtual screening of a chemical database with docking simulations in the N-terminal ATP-binding site, in vitro ATPase assay using yeast Hsp90, and cell-based Her2 degradation assay in a consecutive fashion. These results exemplify the usefulness of the stru...
In the title complex, [NiCl(2)(C(8)H(6)N(2)O)(2)(H(2)O)(2)], the Ni(II) ion is located on an inversion center and is six-coordinated by two N atoms of 1H-quinazolin-4-one ligands, two chloride ions and two water mol-ecules. The water mol-ecules are involved in intra- and inter-molecular O-H⋯O and O-H⋯Cl hydrogen bonding. Inter-molecular N-H⋯O and N-H⋯Cl hydrogen bonds are formed between ligands...
In order to develop transferable and practical avenues for the assembly of coordination complexes into architectures with specific dimensionality, a strategy utilizing ligands capable of simultaneous metal coordination and self-complementary hydrogen bonding is presented. The three ligands used, 2(1H)-pyrazinone, 4(3H)-pyrimidinone and 4(3H)-quinazolinone, consistently deliver the required synt...
We describe the structure-based design of a novel lead chemotype that binds to thumb pocket 2 of HCV NS5B polymerase and inhibits cell-based gt1 subgenomic reporter replicons at sub-micromolar concentrations (EC50<200nM). This new class of potent thumb pocket 2 inhibitors features a 1H-quinazolin-4-one scaffold derived from hybridization of a previously reported, low affinity thiazolone chemoty...
A one-pot Yb(III)-mediated cascade reaction has been developed leading to small molecules based on a novel structural motif, i.e. quinazolin-4-one moiety fused with an isoquinoline ring, for potential inhibition of TNF-α.
We recently reported on the discovery of a novel antibacterial (2) with a 4(3H)-quinazolinone core. This discovery was made by in silico screening of 1.2 million compounds for binding to a penicillin-binding protein and the subsequent demonstration of antibacterial activity against Staphylococcus aureus. The first structure-activity relationship for this antibacterial scaffold is explored in th...
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