Synthesis of some new 2-[[E]-2-furan-2-yl-vinyl]- 3H- quinazolin-4-one derivatives of expected biological activity

A new series of 2-[[E]-2-furan-2-yl-vinyl]-3H-quinazolin-4-ones incorporated into diverse N, O and S heterocyclic moieties of bioavailability as.5-oxo-4,5-dihydropyrazole 4, 3,5-dimethylpyrazole 5, 5-mercapto-1,2,4-triazole 6, substituted thiazolidinones 8 and 1,3,4-thiadiazole 10, were synthesized by cyclization of the starting quinazolinone acid hydrazide 3 or the acid hydrazide Schiff bases 7 using ethyl acetoacetate, acety I acetone, ammoniumthiocyanate, thioglycolic acid and/or phosphorus pentasulphide, respectively. Other related derivatives such as quinazoline thiosemi - carbazides II and 1,3,4-oxadiazoles 12 were also synthesized. The acid hydrazide 3 showed moderate antimicrobial activity While the starting benzoic acid ethyl ester 2 showed promising anti-inflammatory activity but has no effect on liver carcinoma [HePG2] or brain carcinoma [U251] cell lines

Synthesis and evaluation of novel 2-thiouracil derivatives with analgesic, antiinflamatory and antipyretic activities

This study aims at the synthesis and evaluation of chemotherapeutic activity of a number of 5-substituted 2-thiouracils. Thiourea was reacted with ethyl cyanoacetate or ethyl acetoacetate and benzaldehyde or indole-3 carboxaldehyde in ethanolic sodium ethoxide producing thiouracils 1 and 2. The later was condensed with p-anisaldehyde in alcoholic NaOH giving a chalcone derivative 3 [Claisen-Schemidt reaction]. Compound 1 was chlorinated with POCI3 producing a chloroderivative 4 which inturn was reacted with 4-aminoantipyrine in presence of pyridine giving compound 5. In another pathway 2-thiouracil was chlorosulphonated giving a chlorosulphonyl derivative 6 which was reacted with p-aminobenzoic acid or 4-aminoantipyrine giving compounds 7 and 8 respectively. Finally 2-thiouracil was condensed with Paraformal-dehyde and 4-aminoantipyrine giving the Mannich base 9. The tested compounds were analogous to Metamizole sodium Novalgin and indomethacine, the incorporation of 2-thiouracil ring into antipyrine and indole ring might increase their activities. Here we proved that 2-thiouracil nucleus alone has a potent activity. This is exemplified by compound 7 which satisfied most requirements of analgesic activity

Synthesis of some new 1,8-naphthyridine derivatives of expected biological activity

A series of some new 1,8-naphthyridine derivatives such as, 3-[2-thioxo-l,3,4-thiadiazolin-5-yl]-1,8-naphthyridines, 3-[2-substituted amino-1,3,4-thiadiazol-5-yl]-1,8-naphthyridines, 3-[6-substituted imidazo-[2,1-b]-l,3,4-thiadiazol-2-yl]-1,8-naphthyridines and other nitrogen, sulphur and/or oxygen heterocycles incorporated into 1,8-naphthyridine moities through an amide linkage has been synthesized for the purpose of biological evaluation. Compounds [2, 3, 5, 6, 8d, 10c, 11, 12, 14c] were tested for their antimicrobial activity against Gram +ve and Gram -ve bacteria and against a fungus [Aspergillus niger]. Among of these compounds only compounds 5 and 6 showed moderate activity against Aspergillus niger. Also, compounds 4a and 8c were tested against Ehrlich ascites carcinoma in mice and then measured for their cytotoxic activity against P388 Leukemia cells. Compounds 9b, 10b and 12 were tested against different types of turner cells in [USA]

Studies on ketene s,s,acetals. Part 1. synthesis of new pyrazol [1, 5 - 1] - pyrimidines and pyrazolo [1,5-a] triazines utilizing ketene s,s, acetals

In the present work, the new 3 [p-haloarylamino]4-methoxycarbonyl-5- aminopyrazole [3a-c] were obtained by using ketene S,S,acetal derivatives [1] as good precursors for the synthesis of p- haloarylaminomethoxycarbonyl methyl mercaptal [2a-c], which were prepared through displacement reaction of cyanomethoxycarbonyl ketene dithioacetal [1] with amines. The results of the study were given