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1
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H H H H H H H H H H H H H H H H H H
-> >
4 1
6 7
S S S S
S
S
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S
11 12 13
14 1.i 16 17 1s 19 20
21 22 23 24 2.5 26 27 2s 29 30 :3 1 32
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34 3 .i
36 ::7
S S
s S S S
S S S S
4x1
S
4-C1
S
4-C1 4-C1
S
S
S
6-OCHa 6-OCH1 6-OCHa 6-OCHa 6-OCHa 6-OCHa 6-OCH3 6-OCHa 6-OCHa 6-OCH3 6-OCH3
s
6-OCHa
S S S
S S
S 8 8 8
S S
s
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39 40 41 42
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43 44 4 .i
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17 1s 4! 1 .i(I .i1 32
53 54
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6-OCH3 .i,6-(CH,)z .i,G-(CHs)? 3 6-(CH3)2 .i,G-(CH$)a 3,6-(CHj)? .5,6-(CH3)2 .i,G-(CH3)2 3,6-( CH3)? d,6-(CH3)2 3,6-(CH3)2 5,6-(CH31% .i,6-(CH3)~ .i,6-(CH3)1 2,.j-(CHa)s 2,6-(CHa)2 H H II H Tetrahydro Tet rahydro 're1 rallycllo H H H
R
H
H H H H H H H
H H H H H H H H H H H H H H H H H H H H H H H H H H H H
H H H H H
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Alp, " C
333-33.5 278-2x0 315-3 16 329-330 333-336 316-317 327-3211 341-34'2 333-333 -3 290-291 309-310 >400 333-336 327-328 328-329 272 331-332 319-320 265-270 256-255 266-268 219-220 321-322 297-298 3 10-3 11 306-307 314-3 15 313-314 270-272 299-301 278-279 297-29h 209-210 311-31'2 304-306 370-372 35-336 2.59-260 363 333-3.54 331-332 333-354 35j-356 324-323 328-329 349-330 349-3.50 340-341 360-36 1 331-3.32 95 174-17.5 140-141 118-1 19 318-319 257-258 21s-21 !I 192-193 232-23.5 162-1 6J
mdkr
>113 28 >100 >60 >loo 49 < 16 SS
:3 S 19 32 120 4 .i 64 .i2 >12s 64 l.i9
s7 12s 20 23 < 16 2s 26
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10 S2
>1u0 19 60 27
ss s1 68 2S
27 64 36 22 1!1
17 10:; >12s >128 85 >1zx >128 32 > 12s :1 20 9 .i
Drug level (mel'kp X :3) fur fourfold or greater immunosuppression
6.2 50.0 6.2 1.6 .io. 0 12. ci 1 2 , ti 2.5.0 6.2 >100.0 ?iO.0 6.2 -50.0 100,0 .io . 0 >loo. 0 >100.0 100,0
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.io.0 3 ,1
6.2 6.2 12..j 100.0 .io, 0 2.i. 0 >100.0 100,0 >100.0 >lull,(l
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12 . .i 100.0
.io. 0
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