Shiga-like toxins and ricin are ribosome-inactivating proteins (RIPs) that are lethal to mammals and pose a global health threat. No clinical vaccines or therapeutics currently exist to protect against these RIPs. Two small molecules (Retro-1 and Retro-2) were discovered with high-throughput screening and reported for their protection of cells against RIPs. Of great significance, Retro-2, repor...

OBJECTIVE A series of ten novel derivatives of 3-substituted-2-thioxoquinazolin-4(3H)-ones have been synthesized from anthranilic acid via Mannich reaction with various secondary amines in presence of formaldehyde in ice cold condition. MATERIALS AND METHODS The structure of these compounds have been elucidated by spectral (FTIR, 1H-NMR and mass) analysis. The titled compounds were evaluated ...

Quinazolinone derivatives are nowadays well recognized as valuable scaffold in drug discovery. In this manuscript an improved multicomponent process for the chemical synthesis of 2,3-dihydroquinazolin-4(1H)-one derivatives is described. Isatoic anhydride and aromatic aldehydes with ammonium acetate have been subjected to a three-component reaction under solvent-free conditions and catalysis of ...

2-Dihydroquinazolin-4(1H)-thiones were prepared in up to excellent yields from 2-aminobenzothioamides and aldehydes. The reaction is carried out in water without the use of any catalyst or promoter. The sulfur-containing substrate can be obtained easily by thiation of the corresponding nitrile by solid sodium hydrosulfide.

The base catalyzed intramolecular nucleophilic cyclization of 1-(2-bromobenzoyl)-3-(2-fluorophenyl)thiourea (1) in the presence of N,N-dimethyl formamide (DMF) afforded the 1-(3-fluorophenyl)-2-thioxo-2,3-dihydroquinazolin-4(1H)-one (2) by an intramolecular nucleophilic substitution SNAr mechanism. The structure was supported by the spectroscopic data and unambiguously confirmed by the single c...

Cobalamin-dependant cytosolic enzyme methionine synthase (MetS) catalyses the transfer of a methyl group from the methyltetrahydrofolate (MTHF) to homocysteine (Hcy) to produce methionine and tetrahydrofolate (THF). MetS is over-expressed in the cytosol of certain breast and prostate tumour cells. Methionine used as a source of one carbon atom for the building of the DNA of the tumour cells, st...

In this study some new compounds have been prepared including thereaction of diazoium salt 1,4-phenylenediamine with 2-mercaptobenzaldehyde at (0-5)0C[F1]. Then Schiff bases [F2-F6] werethen synthesized through the reaction compound [F1] withsubstituteds aniline in absolute ethanol, and were convertedinto 2,3 - dihyroquinazolin 4(1H) one derivatives [F7-F11] by 2-amino benzoic acid ethanol. The...

A simple and efficient procedure has been developed for the synthesis of 2,3-dihydroquinazolin-4(1H)-ones derivatives under solvent-free conditions. This method uses the condensation of isatoic anhydride, aldehydes, and amines in the presence of a catalytic amount Sulfonated Porous Carbon (SPC). One of the important advantages of the new method is that the SPC could be recycled and reused.