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A new isatin ribonucleoside (3) was synthesized in a good yield by trimethylsilyl trifluoromethanesulfonate (TMSOTf) catalyzed coupling reaction between the silylated nitrogenated base of 1H-Indole-2,3-dione (1) and 1,2,3,5-tetra-O-acetyl-beta-D-ribfuranose (2). Thiosemicarbazides 4a-e were utilized by the prepared ribonucleoside (3) to give new series of 1H-indole-2,3-dione-3-thiosemicarbazone ribonucleosides 5a-e. All compounds tested as antibacterial agents showed slight inhibitory activity against the selected bacterial strains.

New series of furosalicylic acids 3a-c, furosalicylanilides 6a-n, furobenzoxazines 8a-f, 1-benzofuran-3-arylprop-2-en-1-ones 12a,b, 6-(aryl-3-oxoprop-1-enyl)-4H-chromen-4-ones 16a-c and 6-[6-aryl-2-thioxo-2,5-dihydropyrimidin-4-yl]-4H-chromen-4-ones 17a-c were synthesized. Anti-inflammatory activity evaluation was performed using carrageenan-induced paw edema model in rats and prostaglandin E 2 (PGE 2 ) synthesis inhibition activity. Some of the tested compounds revealed comparable activity with less ulcerogenic effect than Diclofenac at a dose 100 mg/kg. All the synthesized compounds were docked on the active site of cyclooxygenase-2 (COX-2) enzyme and most of them showed good interactions with the amino acids of the active site comparable to the interactions exhibited by Diclofenac.

Many compounds revealed promising anti-inflammatory activity relative to indomethacin especially compounds 4a, 5a, 5b, 6b, 6d, 6f and 7b. They were safe to the gastric mucosa and did not cause toxicity up to tenfolds the anti-inflammatory dose, in addition, all compounds inhibited TNF-α with IC values of 1.7-100 nM.

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Compounds 7c and 11a may be considered as promising CBSI based on their excellent activity and favorable drug likeness profile.

A series of new 9-glycosyl-4,9-dihydropyrano[3,4-b]indole-1(3H)-ones 3 was synthesized in moderate to low yields. 4,9-Dihydropyrano[3,4-b]indole-1(3H)-ones (1) were coupled with different acetobromoglycopyranoses 2 in refluxing toluene in the presence of silver oxide to afford one coupling product of the respective N-glycosides. α-L-Arabinopyranosides 3j and 3m were the most active glycosides among the tested compounds against certain Gram positive and Gram negative bacterial strains.

Synthesis of 1H-Indole-2,3-dione-3-thiosemicarbazone Ribonucleosides as Antibacterial Agents. -All synthesized compounds exhibit slight inhibitory activity against some bacterial strains. -(KASSAB, S. E.; HEGAZY, G. H.; EID, N. M.; AMIN, K. M.; EL-GENDY*, A. A.; Nucleosides, Nucleotides Nucleic Acids 29 (2010) 1, 72-80,