N-aminoimidazole derivative for inhibiting HIVAn N-aminoimidazole or N-aminoimidazolethinone derivative, a pharmaceutically acceptable salt, a tautomer, an isomer, an ester or glycosylation product thereof, said derivative being represented by general formula (1): wherein m=zero or 1,n=zero or 1, R is selected from hydrogen, methyl or ethyl, R is selected from hydrogen, SH or -SR wherein R is methyl, benzyl or glucose residue; Q is selected from 1-naphthyl, 2-naphthyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring, wherein the substitutio nof understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ether or isopropyl; L is selected from 1-naphyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring wherein the substitution is understood as being one or two substituents selected from H, F< Cl, Br, I methyl, ethyl or isopropyl. This invention further relates to the use of compounds of formula (I) as agents having biological activity, especially against viral infections.The derivative of n-aminooimidazole or n-aminooimidazole thioketones, its pharmacy acceptable salt, tautomer, isomers, ester or glycosylation product is characterized in that, described derivative is the compound with following general formula (i) expression:wherein:m is 0 or 1;n is 0 or 1;r 1be selected from hydrogen, methyl, ethyl, propyl group or sec.-propyl; r 2be selected from hydrogen and-sh; q is selected from 1-naphthyl, 2-naphthyl, xenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, carboxyl, aminocarbonyl, alkylamino-carbonyl, dialkyl aminocarbonyl, phenylamino carbonyl, alkoxy carbonyl or phenyl;wherein, alkyl is methyl, ethyl, propyl group or sec.-propyl, and phenyl is replacement or the unsubstituted phenyl ring with general formula (ii) expressionwherein, o is 1 or 2, r 3be selected from h, f, cl, br, i, hydroxyl, alkoxyl group, amino, alkylamino, dialkyl amido, cyano group, nitro, carboxyl, aminocarbonyl, alkyl amino carbonyl, alkoxy carbonyl, methyl, ethyl, propyl group, sec.-propyl or c 1-3haloalkyl, wherein haloalkyl comprises 1-4 halogen atom, and alkyl is selected from methyl, ethyl, propyl group or sec.-propyl; replacement or unsubstituted phenyl ring that l is selected from 1-naphthyl, 2-naphthyl, xenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl or represents with general formula (iii)wherein, p is 1 or 2, r 4be selected from h, f, cl, br, i, hydroxyl, alkoxyl group, amino, alkylamino, dialkyl amido, cyano group, nitro, carboxyl, aminocarbonyl, alkyl amino carbonyl, alkoxy carbonyl, methyl, ethyl, propyl group, sec.-propyl or c 1-3haloalkyl, wherein, haloalkyl comprises 1-4 halogen atom, and alkyl is selected from methyl, ethyl, propyl group or sec.-propyl; condition is that compound (i) is not selected from1-(3-chloro-phenyl-amino)-2,3-dihydro-4-methyl-5-phenyl-1h-imidazoles-2-thioketones;1-(2-chloro-phenyl-amino)-2,3-dihydro-4-methyl-5-phenyl-1h-imidazoles-2-thioketones;1-(4-chloro-phenyl-amino)-2,3-dihydro-4-methyl-5-phenyl-1h-imidazoles-2-thioketones;1-(phenyl amino)-2,3-dihydro-4-methyl-5-phenyl-1h-imidazoles-2-thioketones;1-(4-nitrophenyl amino)-2,3-dihydro-4-methyl-5-phenyl-1h-imidazoles-2-thioketones;1-(4-aminomethyl phenyl amino)-2,3-dihydro-4-methyl-5-phenyl-1h-imidazoles-2-thioketones;1-(4-p-methoxy-phenyl amino)-2,3-dihydro-4-methyl-5-phenyl-1h-imidazoles-2-thioketones;1-(benzylamino)-2,3-dihydro-4-methyl-5-phenyl-1h-imidazoles-2-thioketones;4-methyl-5-phenyl-1-phenyl amino-1h-imidazoles;4-methyl-5-phenyl-1-(4-nitrophenyl) amino-1h-imidazoles;4-methyl-5-phenyl-1-(4-chloro-phenyl-) amino-1h-imidazoles;4-methyl-5-phenyl-1-(4-aminomethyl phenyl) amino-1h-imidazoles; or4-methyl-5-phenyl-1-(4-p-methoxy-phenyl) amino-1h-imidazoles.
ＨＩＶ 억제 Ｎ-아미노이미다졸 유도체 본 발명은 화학식 I의 N-아미노이미다졸 또는 N-아미노이미다졸티온 유도체, 이의 제약상 허용가능한 염, 호변이성체, 이성체, 에스테르 또는 글리코실화 산물에 관한 것이며, 화학식 I에 있어서 m은 0 또는 1이고; n은 0 또는 1이고; R1은 수소, 메틸 및 에틸로부터 선택되고; R2는 수소, -SH 또는 -SR0이고, 여기서, R0 은 메틸, 벤질 또는 글루코스 잔기이고; Q는 1-나프틸, 2-나프틸, 비페닐, 2-피리딜, 3-피리딜, 4-피리딜, 2-피리미딜, 4-피리미딜, 5-피리미딜, 티에닐, 또는 비치환되거나 H, F, Cl, Br, I, 메틸, 에틸 및 이소프로필로부터 선택된 1개 또는 2개의 치환체로 치환된 페닐 환이고; L은 1-나프틸, 2-나프틸, 비페닐, 2-피리딜, 3-피리딜, 4-피리딜, 2-피리미딜, 4-피리미딜, 5-피리미딜, 티에닐, 또는 비치환되거나 H, F, Cl, Br, I, 메틸, 에틸 및 이소프로필로부터 선택된 1개 또는 2개의 치환체로 치환된 페닐 환이다. 또한, 본 발명은 특히 바이러스 감염에 대한 생물학적 활성을 갖는 제제로서의 화학식 I의 화합물의 용도에 관한 것이다. 화학식 I의 N-아미노이미다졸 또는 N-아미노이미다졸티온 유도체, 이의 제약상 허용가능한 염, 호변이성체, 이성체, 에스테르 또는 글리코실화 산물. [화학식 I] [이미지] 상기 화학식 I에서, m은 0 또는 1이고; n은 0 또는 1이고; R1은 수소, 메틸, 에틸, 프로필 및 이소프로필로부터 선택되고; R2는 수소 및 -SH로부터 선택되고; Q는 1-나프틸, 2-나프틸, 비페닐, 2-피리딜, 3-피리딜, 4-피리딜, 2-피리미딜, 4-피리미딜, 5-피리미딜, 티에닐, 카르복실, 아미노카르보닐, 알킬아미노카르보닐, 디알킬아미노카르보닐, 페닐아미노카르보닐, 알킬옥시카르보닐 및 페닐로부터 선택되고; 여기서, 알킬은 메틸, 에틸, 프로필 또는 이소프로필이고, 페닐은 화학식 II의 치환되거나 비치환된 페닐 환이고; [화학식 II] [이미지] 상기 화학식 II에서, o는 1 또는 2이고, R3은 H, F, Cl, Br, I, 히드록시, 알킬옥시, 아미노, 알킬아미노, 디알킬아미노, 시아노, 니트로, 카르복실, 아미노카르보닐, 알킬아미노카르보닐, 알킬옥시카르보닐, 메틸, 에틸, 프로필, 이소프로필 및 C1-3 할로알킬로부터 선택되고, 여기서 할로알킬은 1 내지 4개의 할로겐 원자를 함유하고, 알킬은 메틸, 에틸, 프로필 및 이소프로필로부터 선택되고; L은 1-나프틸, 2-나프틸, 비페닐, 2-피리딜, 3-피리딜, 4-피리딜, 2-피리미딜, 4-피리미딜, 5-피리미딜, 티에닐 및 화학식 III의 치환되거나 비치환된 페닐 환이고; [화학식 III] [이미지] 상기 화학식 III에서, p는 1 또는 2이고, R4는 H, F, Cl, Br, I, 히드록시, 알킬옥시, 아미노, 알킬아미노, 디알킬아미노, 시아노, 니트로, 카르복실, 아미노카르보닐, 알킬아미노카르보닐, 알킬옥시카르보닐, 메틸, 에틸, 프로필, 이소프로필 및 C1-3 할로알킬로부터 선택되고, 여기서 할로알킬은 1 내지 4개의 할로겐 원자를 함유하고, 알킬은 메틸, 에틸, 프로필 및 이소프로필로부터 선택되고; 단 화학식 I의 화합물은 1-(3-클로로페닐아미노)-2,3-디히드로-4-메틸-5-페닐-1H-이미다졸-2-티온; 1-(2-클로로페닐아미노)-2,3-디히드로-4-메틸-5-페닐-1H-이미다졸-2-티온; 1-(4-클로로페닐아미노)-2,3-디히드로-4-메틸-5-페닐-1H-이미다졸-2-티온; 1-(페닐아미노)-2,3-디히드로-4-메틸-5-페닐-1H-이미다졸-2-티온; 1-(4-니트로페닐아미노)-2,3-디히드로-4-메틸-5-페닐-1H-이미다졸-2-티온; 1-(4-메틸페닐아미노)-2,3-디히드로-4-메틸-5-페닐-1H-이미다졸-2-티온; 1-(4-메틸옥시페닐아미노)-2,3-디히드로-4-메틸-5-페닐-1H-이미다졸-2-티온; 1-(벤질아미노)-2,3-디히드로-4-메틸-5-페닐-1H-이미다졸-2-티온; 4-메틸-5-페닐-1-페닐아미노-1H-이미다졸; 4-메틸-5-페닐-1-(4-니트로페닐)아미노-1H-이미다졸; 4-메틸-5-페닐-1-(4-클로로페닐)아미노-1H-이미다졸; 4-메틸-5-페닐-1-(4-메틸페닐)아미노-1H-이미다졸; 및 4-메틸-5-페닐-1-(4-메틸옥시페닐)아미노-1H-이미다졸로부터 선택되지 않는다.