FIELD: pharmaceuticals.
SUBSTANCE: present invention relates to novel inhibitors of hepatitis B virus (HBV) as chemotherapeutic agents for treatment of HBV. These compounds bind HBV cor-antigen and cause the formation of aberrant viral capsids that do not carry the viral genome, which leads to the formation and secretion of defective (avirulent) virus particles. According to the invention, HBV inhibitor is a compound of the general formula 1, 1.3 and 2
,
wherein R is hydrogen or methyl; n=1, 2 or 3,
,
.
Compound of formula 2 is new. Process for preparation of compounds 1, 2 and 1.3 is the acylation of 3-chloroaniline (E1) or 4-methoxy-3-chloroaniline, respectively, with 1-methyl-4-sulfamoyl-1H-pyrrole-2-carboxylic acid of the general formula E2 or 3-cyclopentylsulfamoyl-4-fluorobenzoic acid E3
E2: R is hydrogen and methyl; n=1, 2 or 3.
EFFECT: new inhibitors of the hepatitis B virus (HBV) were proposed.
13 cl, 6 tbl, 8 ex
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