Patenton — panteon of patents

(19)

RU

(11)

2 218 399

(13)

C2

(51)

IPC

(21) (22)

Application

2001134733/13, 2001-12-24

(24)

Start date

2001-12-24

(22)

Actual filing date

2001-12-24

(45)

Published

2003-12-10

(72)

Inventor

Pjatakova N.V.Khropov Ju.V.Mikhajlitsyn F.S.Gavrilova S.A.Onufriev M.V.Postnikov A.B.Seliverstov V.O.Guljaeva N.V.Severina I.S.

(73)

Holder

Biologicheskij Fakul'Tet Moskovskogo Gosudarstvennogo Universiteta Im. M.V. Lomonosova

INHIBITOR OF NO-DEPENDENT ACTIVATION OF SOLUBLE FORM OF GUANYLATE CYCLASE Russian patent published in 2003 - IPC

Abstract RU 2218399 C2

FIELD: organic chemistry, biochemistry, enzymes. SUBSTANCE: invention can be used in biochemistry for study of regulatory effects of nitrogen oxide and mechanism of action of peroxide-containing sesquiterpenoids of artemisinine order on activity of soluble form of guanylate cyclase (sGC). Invention relates to artemisinine and its derivatives of the general formula (I): wherein if is a simple bond then R is OH, (lower alkyl)-hydroxy-group or OC(O)CH2CH2C(O)ONa; or if is a double bond then R is oxygen atom. These compounds in the concentration 1-100 mcM show inhibitory effect of NO-dependent activation of sGC partially purified from human platelets caused by donor of nitrogen oxide - sodium nitroprusside. Concentration of artemisinine providing 50% of reduction of activating effect of sodium nitroprusside (IC50) is 4.2 mcM being "basal" activity of enzyme (in the absence of sodium nitroprusside) is increased insignificantly (by 20-24%). Methylene blue as the nearest structural analogue in the concentration 10 mcM under the same conditions inhibits NO-dependent activation of sGC by 27% and reduces "basal" activity of enzyme by 10- 15%. Peroxide-containing sesquiterpenoids of artemisinine order of the general formula (I) are new effective inhibitors of NO-dependent activation of sGC. EFFECT: valuable biochemical properties of inhibitor, expanded assortment of modulating agents for this enzyme. 2 dwg, 1 tbl, 4 ex

Similar patents RU2218399C2

Title Year Author Number
INHIBITOR OF NO-DEPENDENT ACTIVATION OF GUANYLATE CYCLASE SOLUBLE FORM 2001
  • Pjatakova N.V.
  • Khropov Ju.V.
  • Busygina O.G.
  • Severina I.S.
  • Preobrazhenskaja M.N.
 RU2188865C1
INHIBITOR OF NO-DEPENDENT ACTIVATION OF SOLUBLE FORM OF GUANYLATE CYCLASE 2001
  • Khropov Ju.V.
  • Pjatakova N.V.
  • Gavrilova S.A.
  • Busygina O.G.
  • Krasnoperov R.A.
  • Medvedeva N.A.
  • Severina I.S.
 RU2189392C1
(1,2,3-TRIAZOLYL)-1,2,3-OXADIAZOLE DERIVATIVES POTENTIATING NO-DEPENDENT ACTIVATION OF SOLUBLE FORM OF GUANYLATE CYCLAZE 2000
  • Batog L.V.
  • Rozhkov V.Ju.
  • Khropov Ju.V.
  • Pjatakova N.V.
  • Busygina O.G.
  • Severina I.S.
  • Makhova N.N.
 RU2158265C1
INHIBITOR OF GUANYLATE CYCLASE SOLUBLE FORM 2001
  • Betin V.L.
  • Bakhmedova A.A.
  • Gorjunova O.V.
  • Miniker T.D.
  • Plikhtjak I.L.
  • Ehktova L.V.
  • Postnikov A.B.
  • Khropov Ju.V.
  • Kots A.Ja.
  • Mel'Nik S.Ja.
  • Bulargina T.V.
 RU2196175C2
INCLUSION COMPLEXES OF DERIVATIVES OF 1,2,5-OXA- -DIAZOLE-2-OXIDE WITH POLYCYCLIC DERIVATIVES OF GLUCOPYRANOSE, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION 2001
  • Khropov Ju.V.
  • Kots A.Ja.
  • Postnikov A.B.
  • Bogdanova N.G.
  • Gavrilova S.A.
  • Grafov M.A.
  • Volchkova I.L.
  • Pjatakova N.V.
  • Betin V.L.
  • Kulikov A.S.
  • Ovchinnikov I.V.
  • Zapesochnaja G.G.
  • Matveenko V.N.
  • Makhova N.N.
  • Medvedeva N.A.
  • Severina I.S.
  • Bulargina T.V.
 RU2186782C1
SPECIFIC REGULATOR OF ACTIVITY OF NUCLEOTIDE-DEPENDENT ENZYMES 1997
  • Kots A.Ja.
  • Kulikov A.S.
  • Khropov Ju.V.
  • Ovchinnikov I.V.
  • Belushkina N.N.
  • Busygina O.G.
  • Shmal'Gauzen E.V.
  • Jazykova M.Ju.
  • Mast N.V.
  • Jakimova N.G.
  • Lopina O.D.
  • Makhova N.N.
  • Bulargina T.V.
  • Muronets V.I.
  • Severina I.S.
 RU2130490C1
DERIVATIVES OF TETRAFURAZANO-[3,4-B:3',4'-F:3'',4''-J:3''',- -4'''-N]-[1,4,5,8,9,12,13,16]-OCTAAZABICYCLO-[14,2,2]-EICOSA- -4,8,12-TRIENE AND METHOD OF THEIR SYNTHESIS 2000
  • Sheremetev A.B.
  • Betin V.L.
  • Judin I.L.
  • Kulagina V.O.
  • Khropov Ju.V.
  • Bulargina T.V.
  • Kots A.Ja.
 RU2167161C1
1,2,5-OXADIAZOLO[3,4-D]PYRIDAZINE-5,6-DIOXIDE DERIVATIVES AS ACTIVATORS OF SOLUBLE FORM OF GUANYLATE-CYCLASE AND AGENTS ACTIVE IN TREATMENT OF CENTRAL NERVOUS SYSTEM, AND COMPOSITIONS BASED ON THESE COMPOUNDS 1997
  • Kots A.Ja.
  • Khropov Ju.V.
  • Grafov M.A.
  • Kulikov A.S.
  • Ovchinnikov I.V.
  • Belushkina N.N.
  • Busygina O.G.
  • Gavrilova S.A.
  • Makhova N.N.
  • Medvedeva N.A.
  • Bulargina T.V.
  • Severina I.S.
 RU2165256C2
DONOR OF NITROGEN OXIDE ACTIVATING SOLUBLE FORM OF GUANYLATE CYCLASE, INHIBITING PLATELET AGGREGATION AND EXHIBITING SPASMOLYTIC AND VASODILATING EFFECT 2001
  • Mel'Nikova S.F.
  • Kots A.Ja.
  • Pirogov S.V.
  • Postnikov A.B.
  • Betin V.L.
  • Pjatakova N.V.
  • Grafov M.A.
  • Gavrilova S.A.
  • Seliverstov V.O.
  • Khropov Ju.V.
  • Medvedeva N.A.
  • Severina I.S.
  • Tselinskij I.V.
  • Bulargina T.V.
 RU2208438C1
INHIBITOR OF GUANYLATE CYCLASE SOLUBLE FORM 1999
  • Kots A.Ja.
  • Batog L.V.
  • Betin V.L.
  • Rozhkov V.Ju.
  • Ukraintsev K.Eh.
  • Khropov Ju.V.
  • Epishina M.A.
  • Sheremetev A.B.
  • Makhova N.N.
  • Bulargina T.V.
 RU2151799C1

RU 2 218 399 C2

Authors

Pjatakova N.V.

Khropov Ju.V.

Mikhajlitsyn F.S.

Gavrilova S.A.

Onufriev M.V.

Postnikov A.B.

Seliverstov V.O.

Guljaeva N.V.

Severina I.S.

Dates

2003-12-10—Published

2001-12-24—Filed

download Download PDF read Similar patents