Studies on 4(1H)-Quinazolinones. 5. Synthesis and Antiinflammatory Activity of 4(1H)-Quinazolinone Derivatives

Abstract

A number of new 4(1H)-quinazolinones were synthesized and evaluated in the carrageenin-induced paw edema test. Most of the compounds were obtained by the cyclization of the appropriately substituted anthranilamides with acid chlorides, followed by further chemical transformation. Structure-activity data suggest that 2-isopropyl-1-phenyl-, 2-cyclopropyl-1-phenyl-, and 1-isopropyl-2-phenyl-4(1H)-quinazolinones afford optimal potency and the presence of a halogen atom is preferred for activity. Adrenalectomy does not affect the antiinflammatory test results. The best result taking into account both efficacy and side effects was displayed by 1-isopropyl-(2-fluorophenyl)-4-(1H)-quinazolinone (50).

Synthesis and Antimicrobial Evaluation of Quinazolinone Peptide Derivatives

“…Thus keeping in mind the therapeutic potential of quinazolinone as well as biodegradability and bioavailability profile of amino acids/peptide, an attempt has been made to synthesize amino acid/peptide derivatives of quinazolinone so as to increase its therapeutic potential and minimize adverse effects [30][31][32][33].…”

Silica Supported Zinc (II) Chloride (SiO2-ZnCl2) as an Efficient Catalyst for the Eco-Friendly Synthesis of 2,3-Dihydroquinazolin-4(1H)-Ones

“…In particular dihydroquinazolin-4(1H)-one scaffold were found as a core unit in a number of biologically active compounds that they include anticancer, antidituric, anticonvulsant activities. [1][2][3][4][5][6][7][8] Thus, extensive efforts have been exerted on developing methodology for the synthesis of dihydroquinazolin-4(1H)-one derivative. Several numbers of synthetic strategies are known for the preparation of substituted dihydroquinazolin-4(1H)-ones.…”

Synthesis and structural properties of 2-([2.2]paracyclophanyl)-2,3-dihydroquinazolines by cyclocondensation of 2-aminoaryl-benzimidamides with 4-formyl[2.2]paracyclophane catalyzed efficiently by iodine

“…1,2 Quinazoline moieties are considered to be pharmacophores because they show many types of pharmacological properties 3,4 especially as antiinflamatory, 5 antiallergic 6 and antimalarial agents 7 and in cancer treatment. 8 Some quinazolines possess inhibiting properties for tyrosine kinase, 9 which is useful in inhibiting tumour growth.…”