| 摘要 |
Described is an N-aminoimidazole or N-aminoimidazolethione derivative, a pharmaceutically acceptable salt, a tautomer, an isomer, an ester or a glycosylation product thereof. The derivative is represented by the general formula I wherein: m is zero or 1; n is zero or 1;Rl is selected from hydrogen, methyl, ethyl, propyl or isopropyl ; R2 is selected from hydrogen and-SH; Q is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2 pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, carboxyl, aminocarbonyl, alkylamino carbonyl, dialkylaminocarbonyl, phenylaminocarbonyl, alkyloxycarbonyl or phenyl ; wherein alkyl is a methyl, ethyl, propyl or isopropyl and phenyl is a substituted or unsubstituted phenyl ring represented by the general formula II wherein o is 1 or 2, and R3 is selected from H, F, Cl, Br, I, hydroxy, alkyloxy, amino, alkylamino, dialkylamino, cyano, nitro, carboxyl, aminocarbonyl, alkylaminocarbonyl, alkyloxycarbonyl, methyl, ethyl, propyl, isopropyl or Cl1-3 haloalkyl; L is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2 pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring represented by the general formula III wherein p is 1 or 2, and R4 is selected from H, F,Cl, Br,I, hydroxy, alkyloxy, amino, alkylamino, dialkylamino, cyano, nitro, carboxyl, aminocarbonyl, alkylaminocarbonyl, alkyloxycarbonyl, methyl, ethyl, propyl, isopropyl or Cl1-3 haloalkyl. A proviso is explained that compound I is not selected from 1- (3-Chlorophenylamino)-2, 3-dihydro-4-methyl-5-phenyl-1H-imidazole-2-thione ;1-(2-Chlorophenylamino)-2, 3-dihydro-4-methyl-5-phenyl-1H-imidazole-2-thione; 1- (4-Chlorophenylamino)-2, 3-dihydro-4-methyl-5-phenyl-1H-imidazole-2-thione ; 1- (phenylamino)-2, 3-Dihydro-4-methyl-5-phenyl- 1H-imidazole-2-thione ; 1- (4-nitrophenylamino)-2, 3-dihydro-4-methyl-5-phenyl-1H-imidazole-2-thione ; 1- (4-methylphenylamino)-2, 3-dihydro-4-methyl-5-phenyl-1H-imidazole-2-thione ; 1- (4-methyloxyphenylamino)-2, 3-dihydro-4-methyl-5-phenyl-lH-imidazole-2-thione ;1-(benzylamino)-2, 3-dihydro-4-methyl-5-phenyl-lH-imidazole-2-thione ; 4-Methyl-5-phenyl-1-phenylamino-1H-imidazole ; 4-Methyl-5-phenyl-1- (4-nitrophenyl) amino-1H-imidazole ; 4-Methyl-5-phenyl-1- (4-chlorophenyl) amino-1H-imidazole ; 4-Methyl-5-phenyl-1- (4-methylphenyl) amino-1H-imidazole ; or 4-Methyl-5-phenyl-1- (4-methyloxyphenyl) amino-1H-imidazole. Also described are processes for preparing a derivative of the general formula I, and a pharmaceutical composition comprising the compound with antiviral activity against HIV (Human Immunodeficiency Virus) and other viruses.
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