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The synthesis of 5-β-D-ribofuranosylselenophene-3-carboxamide (selenophenfurin) is reported. Selenophenfurin was found active as cytotoxic agent and as inosine monophosphate dehydrogenase inhibitor.

The syntheses and antitumor activity of 2-β-D-ribofuranosylfuran-4-carboxamide (furanfurin) and 2-β-D-ribofuranosylthiophene-4-carboxamide (thiophenfurin) are reported. The X-ray structure of ethyl 2-β-D-ribofuranosylthiophene-4-carboxylate, precursor of thiophenfurin, is also presented. Only thiophenfurin showed activity as an antitumor agent both in vitro and in vivo.

2′,3′-Dideoxy-8-aza-1-deazaadenosine (21) and its α-anomer (20) were synthesized via glycosylation of 7-chloro-3H-1,2,3-triazolo[4,5-b]pyridi-ne with 2,3-dideoxy-5-O-[(1, 1)-dimethylethyl)diphenylsilyl]-D-glycero-o-pen-tofuranosyl chloride. The reaction gave a mixture of α- and β-anomers of N3-, N4- and N1-glycosylated regioisorners (12–15). The α- and β-anomers of the N4-glycosylated isomer 26 and 27 were also synthesized through the glycosylation of 8-aza-1-deazaadenine with 1-acetoxy-2,3-dideoxy-5-O-f(1,1-di-methylethyl)dimethylsilyl]-D-glycero-pentouranose. These dideoxynucleo-sides and a series of previously synthesized 8-aza-1-deazapurine nucleosidcs were tested for activity against several DNA and RNA viruses, HIV-1 included. The α- and β-anomers of 7-chloro-3-(2-deoxy-D-erythro-pentofuranosyl)-3H-1,2,3-triazolo[4,5-b]pyridine (3a and 4) showed activities against Sb-1 and Coxs viruses. The α- and β-anomers of 2′,3′-dideoxy-8-aza-1-deazaadenosine (20 and 21) were found active as inhibitors ...

Using Triton WR-1339-induced hyperlipidaemic rats as an experimental model, we investigated whether compound 1 (N-(3-benzoylphenyl)-1H-indole-2-carboxamide) and 2 (N-(4-benzoylphenyl)-1H-indole-2-carboxamide) novel anti-hyperlipidaemic agents have any effect on plasma triglyceride, total cholesterol (TC) and high-density lipoprotein cholesterol levels (HDL-C) levels. Hyperlipidaemia was developed by intraperitoneal injection of Triton WR-1339 (200 mg/kg body weight). At a dose of 15 mg/kg body weight, compounds 1, 2 and bezafibrate (BF) significantly reduced the elevated plasma triglyceride levels after 7 and 24 h. Furthermore, HDL-C levels were remarkably increased in all treated groups after 7 and 24 h compared with the hyperlipidaemic control group. However, only compounds 1 and 2-treated groups clearly showed a significant reduction in plasma TC levels after 24 h. It is therefore reasonable to assume that compounds 1 and 2 may have a promising potential in the treatment of hyperlipidaemia and coronary heart diseases.