Synthesis of novel 5-methylidene-1,2,3,5-tetrahydro[2,1-b]-quinazoline derivatives 2-4 with potential biological activities mediated by alpha-adrenergic and/or imidazoline receptors was performed by reacting 2-chloro-4,5-dihydroimidazole (1) with the corresponding 2-aminoacetophenones. Compound 2, which incorporates an enamine moiety, underwent a 1,3-dipolar cycloaddition reaction with the appr...

Quinazoline and quinazolinone derivatives display an extensive application in organic pharmaceutical chemistry, they have been used as natural synthetic materials for medicinal chemistry purposes. Here I reported investigation of a new series quinazolin-4(3H)-one ring derivatives. In this context, starting from the methyl anthranilate, six (4a-f) with various aminomethyl moieties at position 2 ...

To develop a lead anti-diabetic compound, a series of 21 novel quinazoline derivatives have been synthesized and screened against alpha Glucosidase. The binding mode of the compounds at the active site of alpha Glucosidase was explored using Glide docking method. The binding model suggests one to four hydrogen bonding interactions between quinazoline derivatives and alpha-glucosidase. 6-Bromo-2...

A hexachlorocyclotriphosphazene (HCCP)-mediated direct formation of quinazoline (thio)ethers from quinazolin-4(3H)-ones has been developed. Treatment of quinazolin-4(3H)-ones with HCCP, diisopropylethylamine (DIPEA), and thiophenols resulted in formation of the corresponding 4-arylthioquinazoline derivatives in moderate to excellent yields. This method has also been utilized to prepare 4-arylox...

BACKGROUND The quinazoline are an important class of medicinal compounds that possess a number of biological activities like anticancer, anticonvulsant and antioxidant etc. RESULTS We evaluated the previously synthesized quinazoline derivatives 1-3 for their anticancer activities against three cancer cell lines (HepG2, MCF-7, and HCT-116). Among the tested compounds, quinazolines 1 and 3 were...

Previous reports have designated the labeled derivatives of [4-(phenylamino)-quinazoline-6-yl]-amide group as the most promising EGFR-PET imaging agent candidates. To further improve tracer qualifications and increase stability and solubility, additional derivatives of this group substituted at the 7-position with various lengths of fluoro-polyethyleneglycol (F-PEG) chains were synthesized. The...