Abstract: A class of novel 2-.beta.-D-ribofuranosylselenazole-4-carboxamide nucleoside and nucleotide compounds and methods for their production are provided. Compounds of the class typically have pharmacological properties, especially antitumor and antiviral properties, and are well tolerated, being useful, for example, in treating tumors and viral infections in warm blooded animals.

Abstract: 2-.beta.-D-Ribofuranosylthiazole-4-carboxamidine (I) and salts are provided as well as a means for their production and use. The compounds typically show unique pharmacological activity, especially antienzyme and cytotoxic activity.

Abstract: Certain 9-(.beta.-D-Ribofuranosyl)purine-6-carboxamide and other related compounds are prepared and are useful as antiviral agents.

Abstract: Imidazo[1,2-a]-s-triazines including the base, the nucleoside, derivatives of the nucleoside, and the 5' nucleotide are prepared and are useful as antiviral Agents against RNA viruses.

Abstract: The compound 1-B-D-ribofuranosyl-1,2,4-triazole-3-carboxamide is used to treat diseases in humans which are caused by viral infections.

Abstract: Compounds of the structure ##STR1## wherein Y is O, NH or NAc; X is H, .beta.-D-ribofuranosyl or 2,3,5-tri-O-Ac-.beta.-D-ribofuranosyl and Ac is acetyl; are useful as antimicrobal agent.

Abstract: 3,5,7-Trisubstituted pyrazolo[1,5-a]pyrimidines are disclosed of the general formula ##STR1## wherein R.sub.1 is CF.sub.3 or C.sub.1 -C.sub.9 alkyl; R.sub.2 is CF.sub.3 or C.sub.1 -C.sub.9 alkyl; and R.sub.3 is halogen. Such compounds are useful as inhibitors of 3',5'-cyclic AMP phosphodiesterase enzyme.

Abstract: Compounds of formula ##STR1## wherein X is --NR.sub.1 R.sub.2, --Cl, --Br or SR; Y is --X, --OH or --NH.sub.2 ; Z is hydrogen or --NH.sub.2 ; and R' is hydrogen or C.sub.1 -C.sub.18 acyl; R being hydrogen, aryl, aralkyl, substituted aryl, substituted aralkyl, or C.sub.1 -C.sub.7 alkyl; and R.sub.1 and R.sub.2 being independently selected from the group consisting of hydrogen, phenyl, C.sub.7 -C.sub.10 aralkyl, C.sub.1 -C.sub.7 alkyl, C.sub.1 -C.sub.10 branched chain alkyl, C.sub.1 -C.sub.7 unsaturated alkyl or lower alkyl joined to form a 5 or 6-membered heterocyclic ring, with the proviso that when one of R.sub.1 and R.sub.2 are hydrogen, the other is not. The compounds variously exhibit phosphodiesterase inhibition, protein kinase activation, positive inotropic effects, adenyl cyclase inhibition and other biological activities.

Abstract: Ribofuranosyl derivatives of 3-deazaguanine including the 5'-phosphate, 3',5'-cyclic phosphate and 5'-deoxy, useful as antiviral agents and antibacterial agents, are disclosed.

Abstract: N.sup.6 -Carbamoyl and -carbonyl analogs of adenosine 3',5'-cyclic phosphate (cAMP) are prepared and variously demonstrated to exhibit kinase, adrenal steroidogenisis and lipolysis activation superior to cAMP, inhibit phosphodiesterase, and found to increase cardiac output or, in particular cases, to lower blood pressure.

Abstract: Antiviral 1-(G)-1,2,4-triazole carboxamides, thiocarboxamides and carboxamidines wherein G is an acid labile hydrocarbon moiety, e.g., 1-(.alpha.-alkoxyalkyl), are prepared by, e.g., the acid-catalyzed addition reaction of appropriately substituted 1,2,4-triazole and an .alpha.,.beta.-unsaturated ether.

Abstract: Phosphate and carboxylic acid esters of 1-(.beta.-D-ribofuranosyl)-1,2,4-triazoles are prepared by a variety of methods and their antiviral activity reported.

Abstract: The use of 1,2,4-triazole-3-carboxamide and 1,2,4-triazole-3-thiocarboxamide and physiologically compatible salts thereof as antiviral agents is disclosed. A process for synthesizing 1-.beta.-D-ribofuranosyl-1,2,4-triazole-3-carboxamide is also disclosed.

Abstract: Novel compounds of the general formula ##SPC1##Wherein X is H or NH.sub.2 ; R' is C.sub.1 to C.sub.8 alkyl, C.sub.1 to C.sub.8 substituted alkyl, benzyl, C.sub.1 to C.sub.8 acyl, benzoyl, carbamoyl, are disclosed as well as a novel free radial alkylation and acylation process for making such compounds. The compounds of the invention display activity comparable to or superior to their naturally occurring analogue while resisting phosphodiesterase degradation. In some cases the compounds of this invention actually inhibit enzymatic degradation of the natural analogue.

Abstract: Novel substituted 1,2,3-triazole nucleosides such as 4-R'-2-.beta.-D-ribofuranosyl-1,2,3-triazole wherein R' is a nitro, carboxylic acid ester, cyano, carboxamide or thiocarboxamide group are prepared by a procedure entailing fusion of an appropriately substituted 1,2,3-triazole with a tetra-0-acyl blocked ribofuranose. The resulting compounds exhibit significant antimicrobial activity in in vitro testing or are useful in preparing compounds which exhibit such activity.

Abstract: A 5-hydroxy-1,2,3-triazole-4-carboxamide nucleoside, related to the C-nucleoside pyrazomycin, is facilely synthesized by condensation of acyl-blocked ribofuranose with trimethylsilylated 5-hydroxy-1,2,3-triazole-4-carboxamide or, alternatively, by cycloaddition of suitably blocked .beta.-D-ribofuranosyl azide and the anion of ethyl malonamate, and demonstrated to exhibit antiviral properties. The triazole precursor of the former route, as well as certain of its novel salts, are also disclosed as potential antiviral agents.

Abstract: Described herein are novel 6-alkylthio and 6-arylalkylthio purine 3',5' cyclic nucleotides variously exhibiting adenyl cyclase and (in animal studies) tumor inhibitory properties, interferon potentiation, antiviral activity, and the ability to activate adenosine 3',5'-cyclic phosphate-dependent protein kinase while enjoying resistance to phosphodiesterase hydrolysis superior to that of its naturally occuring analog. The compounds are obtained by alkylation of the corresponding 6-thio nucleotide, which is in turn provided by a novel synthetic route.

Abstract: As antiviral agents and intermediates therefor, 3-substituted 1-(.beta.-D-glycosyl)-1,2,4-triazoles, O-acylated analogs thereof, and 5'- and 3',5'-cyclic phosphates of the triazole nucleosides, "glycosyl" being .[.a pentofuranosyl moiety, preferably one whose 2'-oxygen is trans to the triazole aglycon, e.g., xylofuranosyl,.]. ribofuranosyl, .[.2-0-methylribofuranosyl, etc.,.]. the triazole aglycon being 3-substituted with cyano, methylcarboxylate, carboxamidoxime, carboxamido-, thiocarboxamido, or carboxamidine. Preparation of these nucleosides is by silylation of the substituted triazole followed by glycosylation with the appropriate blocked glycosyl halide. Alternatively, acid-catalyzed fusion of the requisite 1,2,4-triazole with an O-acylated pentofuranose yields the nucleosides.