Synthesis of certain pyrazolol [3,4-d] pyrimidine derivatives of potential anti-inflammatory activity

The synthesis of twenty nine novel derivatives of pyrazolol [3,4-d] pyrimidines as non acidic nonsteroidal anti-inflammatory drugs has been achieved via reaction of 4-chloro-l-phenylpyrazolo [3,4-d] pyrimidine with different substituents including 4-amino-3-methylphenol, 4-phenylene diamine and 4-acetamidophenol. The anti-inflammatory activity of thirteen representative compounds have been screened compared to indomethacin as a reference drug. The results revealed that all the tested compounds showed anti-inflammatory activity with the exception of 10a.

Synthesis and antimicrobial activity of some novel 2,3-disubstituted Quinazolin-4[3H] ones

3-Amino-2-[substituted phenoxymethyl / propyl] quinazolin-4 [3 H] ones 4a-c have been prepared. Refluxing 4 with 5-nitro-2-fur- aldehyde / 4-nitrobenzaldehyde afforded the corresponding substituted methylidene-ammo derivatives 5 and 6 respectively. Reaction of 4 -with isatin yielded the indolylideneamino derivatives 7. Refluxing 4 with ofloxacin acid chloride furnished the corresponding carboxamides 8, Reaction of chloroacetyl chloride with 4c produced the 3-chloroacetylamino derivative 9 which upon further reaction with the potassium salts of some antibacterial acids gave the corresponding carboxylate derivatives 10. Sixteen compounds were screened for their antibacterial and antifungal activities. Thirteen compounds were found to possess [high to moderate] activity against Pseudomonas aerugenosa and some of them were also active against Escherichia coli. Only one compound was found to exhibit moderate antifungal activity against Candida albicans