Synthesis and reactions of 2-chloromethyl-6-iodo-3, 1-benzoxazin-4-one with amines

Certain quinazolinones were reported to exert antimicrobial activity[1]. Consequently, in continuation of our previous work on the reaction of 3,1-benzoxazin-4-ones with amines,[2-5], 2-chloromethyl-6- iodobenzoxazin-4-one was synthesized and allowed to react with amines hoping to obtain 4-quinazolinones for evaluation as antimicrobial agents. 5-Iodoanthranilic acid was chloroacetylated to give I which was cyclodehydrated to yield the corresponding 3,1-benzoxazin-4- one II Compound II was allowed to react with different aromatic amines to produce 3-aryl-2-chloromethyl-6-iodoquinazolin-4-ones IIIa-t. Structures of compounds III [Scheme 1] were confirmed by microanalytical and spectroscopic data [Table1 and 2]

Synthesis and pharmacological activity of certain N, arylanthranilic acid esters

Flurbiprofen was formulated into suppository using different suppository bases. The prepared suppository was evaluated viz. uniformity of weight, content uniformity, fracture point and melting point. The in vitro release of the drug from different suppositories in Sorensen's phosphate buffer using USP dissolution tester were investigated. The obtained data were analyzed by BBC microcomputer. The effect of type and concentration of non-ionic surfactant viz Tween 80, Tween 60, Brij 35, and Span 60 on the release rate of drug from the tested bases was studied. Solid dispersions of the drug with PVPK 40, PEG 6000, and urea, sorbital in the ratios drug: polymer 1: 1, 1: 3 and 1: 0.25, 1: 0.5, 1: 1, respectively, were prepared and incorporated in Novata BD base. It is worthy to note that the maximum release obtained from plain base [Novata BD] was 29.13%, while the addition of 10% w/w Brij 35 or solid dispersion PVP 1: 1 to this base increased the drug release to 77.68% and 98.1%, respectively. The anti-inflammatory potency of flurbiprofen suppository suggested formulae were determined in rats and compared to oral and i.p. injection. Results showed that flurbiprofen selected formulae possess significant anti-inflammatory activity and they are significantly better than oral and the commercial brand. Also, a significant correlation was established between the in vivo and in vitro results, linear regression coefficient of 0.94 was calculated