OBJECTIVES Hybridization of bioactive natural and synthetic compounds is one of the most promising novel approaches for the design of hit and lead compounds with new molecular structures. In this investigation, a series of novel hybrid structures bearing quinazolinone, benzofuran and imidazolium moieties were designed and synthesized. MATERIALS AND METHODS Novel hybrid compounds were prepared...

We report a synthetic methodology for the construction of the fused heterocyclic compounds pyrido[2,1-b]quinazolin-9(1H)-ones and pyrrolo[2,1-b]quinazolin-9(1H)-ones through an AgOTf-catalyzed intramolecular alkyne hydroamination reaction. The methodology is applicable to a wide scope of substrates and produces a series of fused quinazolinone heterocycles in good to excellent yields.

In the centrosymmetric title compound, C(34)H(30)F(2)N(6)O(4), the dihedral angle between the quinazolinone and fluorobenzene ring planes are 71.00 (2) and 74.94 (2)° and an intra-molecular N-H⋯O interaction stabilizes the conformation. In the crystal, C-H⋯F and C-H⋯O links help to establish the packing.

for the first time, a spectrum of morphological abnormalities have been produced in developingmouse embryos (n=50), by injecting (ip) 75 and 100 mg/kg of maternal body weight of a new quinazolinonederivative, 4(3h)quinazolinone-2-propyl-2-phenylethyl(qppe), on days 9, 10 and 11 of gestation.measurements of the length of the crown-rump (cr), weight of body of the embryos and placenta on day 17sh...

Synthesis of a new fluorinated nucleoside 6,7-difluoro-2-methyl-4-quinazolinone was described. 2-Amino-4,5-difluorobenzoic acid 1 reacts with (CH3CO)2O followed by ammonia to form (1H)-6,7-difluoro-2-methyl-4-quinazolinone 3a. Ribosylation silylated 4 l-O-acety1-2,3-5-tri-O-benzoyl-α-D-ribofuranose 5 forms protected 6 then unprotected from give free 7. Greener pasture biological docking the cys...

We have developed a general and highly efficient copper-catalyzed method for synthesis of quinazoline and quinazolinone derivatives, the target products were obtained in good to excellent yields via cascade reactions of amidine hydrochlorides with substituted 2-halobenzaldehydes, 2-halophenylketones, or methyl 2-halobenzoates, and the method is of simple, economical and practical advantages.

Several new fluorinated quinazolinone derivatives were prepared and evaluated for in vitro anti-inflammatory activity. The molecular modelling study was performed for compounds 4, 8, 9, 10 and 13. The tested compounds showed strong interactions at the COX-2 binding sites. Compounds 8, 13, 9, and 10 containing triazole, thiadiazole, and oxadiazole rings showed the highest in vitro anti-inflammat...

Quinazolinone and quinazolinedione derivatives are of considerable interest due to their wide array of pharmacological properties. In this paper we report the synthesis of ten quinazolinediones. The previous isolation of two of these compounds, namely 1-methyl-3-(2'-phenylethyl)-1H,3H-quinazoline-2,4-dione and 1-methyl-3-[2'-(4'- methoxyphenyl)ethyl]-lH,3H-quinazoline-2,4-dione, from the seed h...

In the presence of (R)-DTBM-SEGPHOS-Pd(OAc)2 catalyst, treatment of various 3-(2,6-dibromophenyl)quinazolin-4-ones with NaBH4 gave optically active N-C axially chiral quinazolinone (mebroqualone) derivatives through reductive asymmetric desymmetrization (enantioselective monohydrodebromination) followed by kinetic resolution of the resulting monobromophenyl products (up to 99% ee). The enantios...