Π‘ΠΈΠ½ΡΠ΅Π· ΠΏΠ΅ΠΏΡΠΈΠ΄ΠΎΠΌΠΈΠΌΠ΅ΡΠΈΠΊΠΎΠ² β ΠΈΠ½Π³ΠΈΠ±ΠΈΡΠΎΡΠΎΠ² ΡΠ΅ΡΠΈΠ½ΠΎΠ²ΡΡ ΠΏΡΠΎΡΠ΅ΠΈΠ½Π°Π·
Π’Π°ΠΊ ΠΊΠ°ΠΊ ΡΡΠΎΠΌΠ±ΠΈΠ½ ΠΈ ΠΏΠ»Π°Π·ΠΌΠΈΠ½ ΠΎΡΡΡΠ΅ΡΡΠ²Π»ΡΡΡ ΠΏΡΠΎΡΠΈΠ²ΠΎΠΏΠΎΠ»ΠΎΠΆΠ½ΡΠ΅ ΡΡΠ½ΠΊΡΠΈΠΈ Π² ΡΠΈΡΡΠ΅ΠΌΠ΅ Π³Π΅ΠΌΠΎΡΡΠ°Π·Π°, ΡΠ΅Π»Π΅Π½Π°ΠΏΡΠ°Π²Π»Π΅Π½Π½ΠΎΠ΅ Π²ΠΎΠ·Π΄Π΅ΠΉΡΡΠ²ΠΈΠ΅ Π½Π° ΠΎΠ΄ΠΈΠ½ ΠΈΠ· ΡΡΠΈΡ ΡΠ΅ΡΠΌΠ΅Π½ΡΠΎΠ² ΠΈΠ³ΡΠ°Π΅Ρ Π²Π°ΠΆΠ½ΡΡ ΡΠΎΠ»Ρ Π² Π»Π΅ΡΠ΅Π½ΠΈΠΈ ΠΊΠ°ΠΊ ΡΡΠΎΠΌΠ±ΠΎΠ·ΠΎΠ², ΡΠ°ΠΊ ΠΈ Π³Π΅ΠΌΠΎΡΡΠ°Π³ΠΈΠΉ. ΠΠΎΠΊΠ°Π·Π°Π½ΠΎ, ΡΡΠΎ Π² ΠΊΠ°ΡΠ΅ΡΡΠ²Π΅ Π°ΡΠΈΠ»-Π°ΠΊΡΠ΅ΠΏΡΠΎΡΠ° Π² ΠΊΠ°ΡΠ°Π»ΠΈΠ·ΠΈΡΡΠ΅ΠΌΠΎΠΌ ΡΡΠ±ΡΠΈΠ»ΠΈΠ·ΠΈΠ½ΠΎΠΌ ΡΠΈΠ½ΡΠ΅Π·Π΅ ΠΌΠΎΠ³ΡΡ Π²ΡΡΡΡΠΏΠ°ΡΡ Π΄Π΅Π·ΠΎΠΊΡΠΈΡΠΈΠ±ΠΎΠ½ΡΠΊΠ»Π΅ΠΎΠ·ΠΈΠ΄Ρ. Π ΡΡΠΎΠΌ ΡΠ»ΡΡΠ°Π΅ Ρ Π΅ΠΌΠΎΡΠ΅Π»Π΅ΠΊΡΠΈΠ²Π½ΠΎ Π°ΡΠΈΠ»ΠΈΡΡΠ΅ΡΡΡ Π'-Π Π°ΡΠΎΠΌ ΡΠ°Ρ Π°ΡΠ½ΠΎΠ³ΠΎ ΠΎΡΡΠ°ΡΠΊΠ°. ΠΠΎΠ΄ΠΎΠ±ΡΠ°Π½Ρ… Π§ΠΈΡΠ°ΡΡ Π΅ΡΡ >
- Π‘ΠΎΠ΄Π΅ΡΠΆΠ°Π½ΠΈΠ΅
- ΠΡΠ΄Π΅ΡΠΆΠΊΠ°
- ΠΠΈΡΠ΅ΡΠ°ΡΡΡΠ°
- ΠΡΡΠ³ΠΈΠ΅ ΡΠ°Π±ΠΎΡΡ
- ΠΠΎΠΌΠΎΡΡ Π² Π½Π°ΠΏΠΈΡΠ°Π½ΠΈΠΈ
Π‘ΠΎΠ΄Π΅ΡΠΆΠ°Π½ΠΈΠ΅
- Π‘ΠΠΠ‘ΠΠ Π‘ΠΠΠ ΠΠ©ΠΠΠΠ
- I. ΠΠΠ’ΠΠ ΠΠ’Π£Π ΠΠ«Π ΠΠΠΠΠ
- I. 1 ΠΠ½Π³ΠΈΠ±ΠΈΡΠΎΡΡ ΠΏΡΠΎΡΠ΅ΠΈΠ½Π°Π· ΡΠΈΡΡΠ΅ΠΌΡ Π³Π΅ΠΌΠΎΡΡΠ°Π·Π°
- 1. 1. 1. Π’ΡΠΎΠΌΠ±ΠΈΠ½ ΠΈ ΠΏΠ»Π°Π·ΠΌΠΈΠ½ — ΠΊΠ»ΡΡΠ΅Π²ΡΠ΅ ΡΠ΅ΡΠΌΠ΅Π½ΡΡ ΡΠΈΡΡΠ΅ΠΌΡ Π³Π΅ΠΌΠΎΡΡΠ°Π·Π°
- 1. 1. 2. ΠΡΠΈΡΠΎΠ΄Π½ΡΠ΅ ΠΈΠ½Π³ΠΈΠ±ΠΈΡΠΎΡΡ ΡΠ΅ΡΠΌΠ΅Π½ΡΠΎΠ² ΡΠΈΡΡΠ΅ΠΌΡ Π³Π΅ΠΌΠΎΡΡΠ°Π·Π°
- 1. 1. 3. ΠΠΈΡΡΠ½ΠΊΡΠΈΠΎΠ½Π°Π»ΡΠ½ΡΠ΅ ΡΠΈΠ½ΡΠ΅ΡΠΈΡΠ΅ΡΠΊΠΈΠ΅ ΠΈΠ½Π³ΠΈΠ±ΠΈΡΠΎΡΡ ΡΡΠΎΠΌΠ±ΠΈΠ½Π°
- 1. 1. 4. Π‘Π°ΠΉΡ-Π½Π°ΠΏΡΠ°Π²Π»Π΅Π½Π½ΡΠ΅ ΡΠΈΠ½ΡΠ΅ΡΠΈΡΠ΅ΡΠΊΠΈΠ΅ ΠΈΠ½Π³ΠΈΠ±ΠΈΡΠΎΡΡ ΡΡΠΎΠΌΠ±ΠΈΠ½Π°
- 1. 1. 5. ΠΠ½Π³ΠΈΠ±ΠΈΡΠΎΡΡ ΠΏΠ»Π°Π·ΠΌΠΈΠ½Π°
- 1. 1. 5. 1. ΠΡΠΈΡΠΎΠ΄Π½ΡΠ΅ ΠΈΠ½Π³ΠΈΠ±ΠΈΡΠΎΡΡ ΠΏΠ»Π°Π·ΠΌΠΈΠ½Π°
- 1. 1. 5. 2. Π‘ΠΈΠ½ΡΠ΅ΡΠΈΡΠ΅ΡΠΊΠΈΠ΅ ΠΈΠ½Π³ΠΈΠ±ΠΈΡΠΎΡΡ ΠΏΠ»Π°Π·ΠΌΠΈΠ½Π°
- 1. 1. 6. ΠΠ½Π³ΠΈΠ±ΠΈΡΠΎΡΡ Π΄ΡΡΠ³ΠΈΡ ΠΏΡΠΎΡΠ΅ΠΈΠ½Π°Π· ΡΠΈΡΡΠ΅ΠΌΡ Π³Π΅ΠΌΠΎΡΡΠ°Π·Π°
- II. 1. Π‘ΠΈΠ½ΡΠ΅Π· N-Π°ΡΠΈΠ»-Π°-Π°ΠΌΠΈΠ½ΠΎΠ°Π»ΡΠ΄Π΅Π³ΠΈΠ΄ΠΎΠ²
- 11. 2. Π‘ΠΈΠ½ΡΠ΅Π· ΡΠΈΠΊΠ»ΠΈΡΠ΅ΡΠΊΠΈΡ Π°ΠΌΠΈΠ΄ΠΎΠ² Π°ΠΌΠΈΠ½ΠΎΠΊΠΈΡΠ»ΠΎΡ
- 11. 3. Π‘ΠΈΠ½ΡΠ΅Π· Π²ΡΠΎΡΠΈΡΠ½ΡΡ Π°ΠΌΠΈΠ΄ΠΎΠ² ΠΏΠ΅ΠΏΡΠΈΠ΄ΠΎΠ²
- 11. 4. Π‘ΠΈΠ½ΡΠ΅Π· Π½ΡΠΊΠ»Π΅ΠΎΠΏΠ΅ΠΏΡΠΈΠ΄ΠΎΠ²
- 11. 5. Π€Π°ΡΠΌΠ°ΠΊΠΎΠ»ΠΎΠ³ΠΈΡΠ΅ΡΠΊΠΈΠ΅ ΠΈΡΡΠ»Π΅Π΄ΠΎΠ²Π°Π½ΠΈΡ
- III. 1. ΠΠ°ΡΠ΅ΡΠΈΠ°Π»Ρ ΠΈ ΠΌΠ΅ΡΠΎΠ΄Ρ
- III. 2. Π‘ΠΈΠ½ΡΠ΅Π· Π°-Π°ΠΌΠΈΠ½ΠΎΠ°Π»ΡΠ΄Π΅Π³ΠΈΠ΄ΠΎΠ²
- 3. 2. 1. 1. Boc-Asp (OlBu)-OH
- 111. 2. 1. 2. Boc-Asp (OlBu)-ONSu
- 111. 2. 1. 3. Boc-AspCO'BiO-ol
- 111. 3. Π‘ΠΈΠ½ΡΠ΅Π· ΡΠΈΠΊΠ»ΠΈΡΠ΅ΡΠΊΠΈΡ Π°ΠΌΠΈΠ΄ΠΎΠ² Π°ΠΌΠΈΠ½ΠΎΠΊΠΈΡΠ»ΠΎΡ
- 111. 3. 1. 3. Π‘ΠΈΠ½ΡΠ΅Π· Lys-Pip*2HCl
- 111. 4. Π€Π΅ΡΠΌΠ΅Π½ΡΠ°ΡΠΈΠ²Π½ΡΠΉ ΡΠΈΠ½ΡΠ΅Π· Π°ΠΌΠΈΠ΄Π° ΠΏΠ΅ΠΏΡΠΈΠ΄Π° ForAlaPheLys-Pip
- 111. 4. 1. ΠΡΠΈΠ³ΠΎΡΠΎΠ²Π»Π΅Π½ΠΈΠ΅ ΠΊΠ°ΡΠ°Π»ΠΈΠ·Π°ΡΠΎΡΠ° (ΡΡΠ±ΡΠΈΠ»ΠΈΠ·ΠΈΠ½Π°-72, ΡΠΎΡΠ±ΠΈΡΠΎΠ²Π°Π½Π½ΠΎΠ³ΠΎ Π½Π° ΡΠΈΠ»ΠΎΡ ΡΠΎΠΌΠ΅ Π‘-80)
- 111. 4. 2. Π‘ΠΈΠ½ΡΠ΅Π· Π°ΠΌΠΈΠ΄Π° ForAlaPheLys-Pip
- 111. 5. Π‘ΠΈΠ½ΡΠ΅Π· Π²ΡΠΎΡΠΈΡΠ½ΡΡ Π°ΠΌΠΈΠ΄ΠΎΠ² ΠΏΠ΅ΠΏΡΠΈΠ΄ΠΎΠ²
- 111. 5. 1. ΠΠ±ΡΠ°Ρ ΠΏΡΠΎΡΠ΅Π΄ΡΡΠ° Π½Π° ΠΏΡΠΈΠΌΠ΅ΡΠ΅ ΡΠΈΠ½ΡΠ΅Π·Π° (ΠΈΠΌΠΈΠ΄Π°Π·ΠΎΠ»-1 -ΠΈΠ»)Π°ΠΌΠΈΠ΄Π° N"'-(Π±Π΅Π½Π·ΠΈΠ»ΠΎΠΊΡΠΈΠΊΠ°ΡΠ±ΠΎΠ½ΠΈΠ»)-Π¬-Π°Π»Π°Π½ΠΈΠ»-Π¬-Π°Π»Π°Π½ΡΡ-Π¬-(0-ΠΌΠ΅ΡΠΈΠ»)-Π³Π»ΡΡΠ°ΠΌΠΈΠ½ΠΎΠ²ΠΎΠΉ ΠΊΠΈΡΠ»ΠΎΡΡ (Cbz-AlaAlaGlu (OMe)-Im)
- 111. 5. 2. Π‘ΠΈΠ½ΡΠ΅Π· Π²ΡΠΎΡΠΈΡΠ½ΡΡ Π°ΠΌΠΈΠ΄ΠΎΠ² ΠΏΠ΅ΠΏΡΠΈΠ΄ΠΎΠ²
- 111. 6. Π‘ΠΈΠ½ΡΠ΅Π· Π½ΡΠΊΠ»Π΅ΠΎΠΏΠ΅ΠΏΡΠΈΠ΄ΠΎΠ²
- 111. 7. ΠΠ΅ΡΠΎΠ΄Ρ ΡΠ°ΡΠΌΠ°ΠΊΠΎΠ»ΠΎΠ³ΠΈΡΠ΅ΡΠΊΠΈΡ
ΠΈΡΡΠ»Π΅Π΄ΠΎΠ²Π°Π½ΠΈΠΉ
- 111. 7. 1. ΠΠ΅ΡΠΎΠ΄ΠΈΠΊΠ° ΠΎΠΏΡΠ΅Π΄Π΅Π»Π΅Π½ΠΈΡ Π°ΠΊΡΠΈΠ²Π½ΠΎΡΡΠΈ ΡΠ΅ΡΠΈΠ½ΠΎΠ²ΡΡ ΠΏΡΠΎΡΠ΅ΠΈΠ½Π°Π·
- 111. 7. 2. ΠΠ΅ΡΠΎΠ΄ΠΈΠΊΠ° ΠΈΠ½Π³ΠΈΠ±ΠΈΡΠΎΠ²Π°Π½ΠΈΡ ΡΡΠ±ΡΠΈΠ»ΠΈΠ·ΠΈΠ½Π°
- 111. 7. 3. ΠΠ΅ΡΠΎΠ΄ΠΈΠΊΠ° ΠΈΠ½Π³ΠΈΠ±ΠΈΡΠΎΠ²Π°Π½ΠΈΡ ΠΏΠ»Π°Π·ΠΌΠΈΠ½Π°
- 111. 7. 4. ΠΠ΅ΡΠΎΠ΄ΠΈΠΊΠ° ΠΎΠΏΡΠ΅Π΄Π΅Π»Π΅Π½ΠΈΡ Π²ΡΠ΅ΠΌΠ΅Π½ΠΈ ΡΡΠ³Π»ΠΎΠ±ΡΠ»ΠΈΠ½ΠΎΠ²ΠΎΠ³ΠΎ ΡΠ°ΠΊΡΠΎΡ Π₯ΠΠ°-Π·Π°Π²ΠΈΡΠΈΠΌΠΎΠ³ΠΎ Π»ΠΈΠ·ΠΈΡΠ°
- 111. 7. 5. ΠΠ΅ΡΠΎΠ΄ΠΈΠΊΠ° ΠΎΠΏΡΠ΅Π΄Π΅Π»Π΅Π½ΠΈΡ Π²ΡΠ΅ΠΌΠ΅Π½ΠΈ ΠΎΡΡΠ°Π½ΠΎΠ²ΠΊΠΈ ΠΊΡΠΎΠ²ΠΎΡΠ΅ΡΠ΅Π½ΠΈΡ in vivo
- 111. 7. 6. ΠΠ΅ΡΠΎΠ΄ΠΈΠΊΠ° ΠΎΠΏΡΠ΅Π΄Π΅Π»Π΅Π½ΠΈΡ ΠΎΠ±ΡΠ΅ΠΌΠ° ΠΊΡΠΎΠ²ΠΎΠΏΠΎΡΠ΅ΡΠΈ in vivo
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