Pokaż cały numer - Farmaceutyczny Przegląd Naukowy

Farm Przegl Nauk, 2009,2
Tabela 1.
Pochodne H1-H52 o działaniu hamującym
odwrotną transkryptazę wirusa
HIV-1
4,5,6,7-tetrahydroimidazolo[4,5,1-jk]
[1,4]benzodiazepin-2(1H)-on
56
związek R1 R2 R3 R4 pIC 50
H1 H O CH 2 CO 2 CH 3 5-CH 3 3,04
H2 8-NH 2 O CPM 5-CH 3 3,07
H3 9-NHCOCH 3 O CPM 5-CH 3 3,80
H4 H O CH 2 CH=CHC 6 H 5 5-CH 3 3,91
H5 H O CH 2 -2-furanyl 5-CH 3 3,97
H6 H O CH 2 CH 2 CH 2 CH 3 5-CH 3 4,00
H7 H O CH 2 CH 2 CH 3 5-CH 3 4,05
H8 H O CH 2 CHCH 2 5-CH 3 4,15
H9 H O CH 2 C(CH=CH 2 )=CH 2 5-CH 3 4,15
H10 H O CH 2 C(Br)CH 2 5-CH 3 4,21
H11 9-NH 2 O CPM 5-CH 3 4,22
H12 H O CH 2 CHCHCH 3 5-CH 3 4,24
H13 H O CH 2 CH 2 CHCH 2 5-CH 3 4,30
H14 H O 2-MA 5-CH 3 4,33
H15 H O CPM 5-CH 3 4,36
H16 H O CH 2 C(C 2 H 5 )=CH 2 5-CH 3 4,43
H17 H O CH 2 CHCHCH 3 5-CH 3 4,46
H18 H O CH 2 C(CH 3 )=CHCH 3 5-CH 3 4,54
H19 H O DMA 5-CH 3 4,90
H20 8-NCH 3 O CPM 5-CH 3 5,18
H21 9-N(CH 3 ) 2 O CPM 5-CH 3 5,18
H22 10-OCH 3 O DMA 5-CH 3 5,18
H23 8-CONH 2 O DMA 5-CH 3 5,20
H24 9-CF 3 O DMA 5-CH 3 5,23
H25 10-OCH 3 S DMA 5-CH 3 5,33
H26 H O DMA 5-CH 3 5,48
H27 9-NO 2 S CPM 5-CH 3 5,61
H28 10-Br S DMA 5-CH 3 5,97
H29 8-CH 3 O DMA 5-CH 3 6,00
H30 9-CF 3 S DMA 5-CH 3 6,31
H31 8-CONH 2 S DMA 5-CH 3 6,73
H32 9-Cl O DMA 5-CH 3 6,74
H33 9-Cl S DMA H 6,80
H34 8-OC 2 H 5 S DMA 5-CH 3 7,02
H35 8-I O DMA 5-CH 3 7,06
H36 H S CPM 5-CH 3 7,22
H37 8-CN S DMA 5-CH 3 7,25
H38 8-I S DMA 5-CH 3 7,32
H39 8-Br O DMA 5-CH 3 7,33
H40 8-Cl S DMA H 7,34
H41 H S DMA 5-CH 3 7,36
H42 9-Cl S DMA 5-CH 3 7,47