WO2002014295A1 - Derives de thiazines de la formule generale (1) manifestant une action antibacterienne et antivirale - Google Patents

Derives de thiazines de la formule generale (1) manifestant une action antibacterienne et antivirale Download PDF

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Publication number
WO2002014295A1
WO2002014295A1 PCT/RU2000/000344 RU0000344W WO0214295A1 WO 2002014295 A1 WO2002014295 A1 WO 2002014295A1 RU 0000344 W RU0000344 W RU 0000344W WO 0214295 A1 WO0214295 A1 WO 0214295A1
Authority
WO
WIPO (PCT)
Prior art keywords
phenyl
thyazine
compositions
compounds
hydroxy
Prior art date
Application number
PCT/RU2000/000344
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English (en)
Russian (ru)
Other versions
WO2002014295A8 (fr
Inventor
Elena Alexandrovna Izakson
Original Assignee
Elena Alexandrovna Izakson
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Elena Alexandrovna Izakson filed Critical Elena Alexandrovna Izakson
Priority to PCT/RU2000/000344 priority Critical patent/WO2002014295A1/fr
Priority to AU2001213156A priority patent/AU2001213156A1/en
Publication of WO2002014295A1 publication Critical patent/WO2002014295A1/fr
Publication of WO2002014295A8 publication Critical patent/WO2002014295A8/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Definitions

  • the invention is available in medicine, in part - in the form of pharmaceuticals and is intended for use in the market of inadequate and non-compliant medical products.
  • isoniazid hydroazide 4-pyridine acid
  • the claimed compounds are obtained by the following method.
  • the minimum inhibitory concentration was determined by the method of serial dilutions in a liquid medium [6] .. In the process of testing, there was a significant non-hazardous consumption.
  • the data obtained indicate the presence of antimicrobial activity in respect to gamma-positive and gross-negative bacteria.
  • Vegetables were cultivated on a cultivar of Uego cells (sowing dose - 10 ID50 / ml) in an Ebunculus plate at 37 ° C in a C 2 incubator. The tested compounds were distributed in ⁇ . After the daily incubation, the virus was removed, the environment was changed. The final result was taken into account after 36 hours of incubation at 37 ° ⁇ in the ⁇ 2 atmosphere due to the presence of a cytopathic effect. Table 6 - Effect of viral connections
  • the tested compounds tested in Guinea 80 introduced white nonlinear mice weighing 18–20 g with a gastric probe (300 mg / kg) or an internal (100 mg / kg) probe. Each test group included 3 males and 3 females. The state of the animals was observed for 72 hours.

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention relève de la médecine et plus précisément de la pharmacologie; elle concerne de nouveaux produits antimicrobiens et antibactériens, particulièrement efficaces contre les mycobactéries. L'invention consiste à révéler une activité biologique puissante des dérivés des thiazines correspondant à la formule suivante (1) dans laquelle X = OH ou O, Y est sélectionné dans la série (2) Z = Ø (vacant) ou CH2-CH2. On a étudié quatre composés déterminés: 5-(α-phényl-β-carboxyéthylamino)-4-hydroxy-2-phényl-6H-1,3-thiazine-6-one (I), 5-(Π-carboxyphényl-4-hydroxy-2-phényl-6H-1,3-thiazine-6-one (II), 2-phényl-7,8-dihydro-[1,3]-thiazino-[5,4-b][1,4]-oxazine-4(6H)-one (III), 2-phényl-6,7-dihydro-[1,4]-dioxino-[2,3-d][1,4]-thiazine-4-one (IV). L'invention comprend des exemples de la synthèse de ces composés et les résultats de leurs analyses spectrale et chimique ainsi qu'une identification précise. Elle comprend aussi des résultats de l'évaluation pratique de l'activité biologique (action contre les mycobactéries, les bactéries gram-positives et gram-négatives ainsi que contre les virus de l'herpès) de mêmes que des données confirmant leur faible toxicité.
PCT/RU2000/000344 2000-08-16 2000-08-16 Derives de thiazines de la formule generale (1) manifestant une action antibacterienne et antivirale WO2002014295A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
PCT/RU2000/000344 WO2002014295A1 (fr) 2000-08-16 2000-08-16 Derives de thiazines de la formule generale (1) manifestant une action antibacterienne et antivirale
AU2001213156A AU2001213156A1 (en) 2000-08-16 2000-08-16 Thiazine derivatives of general formula (1) having antibacterial and antiviral action

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/RU2000/000344 WO2002014295A1 (fr) 2000-08-16 2000-08-16 Derives de thiazines de la formule generale (1) manifestant une action antibacterienne et antivirale

Publications (2)

Publication Number Publication Date
WO2002014295A1 true WO2002014295A1 (fr) 2002-02-21
WO2002014295A8 WO2002014295A8 (fr) 2002-04-04

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/RU2000/000344 WO2002014295A1 (fr) 2000-08-16 2000-08-16 Derives de thiazines de la formule generale (1) manifestant une action antibacterienne et antivirale

Country Status (2)

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AU (1) AU2001213156A1 (fr)
WO (1) WO2002014295A1 (fr)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU1189066A1 (ru) * 1984-03-11 1990-12-07 Иркутский институт органической химии СО АН СССР Способ получени бензимидазо[2,1-в]-1,3-тиазин-2-онов
SU423355A1 (ru) * 1972-05-19 1995-05-27 Всесоюзный научно-исследовательский химико-фармацевтический институт им.Серго Орджоникидзе Способ получения галогенпроизводных 5н-6,7-дигидроимидазо-[2,1-b]-м-тиазина
RU2127275C1 (ru) * 1993-01-29 1999-03-10 Агурон Фармасьютикалз, Инк. 2-[4-[2-(2-амино-4-оксо-4,6,7,8-тетрагидро-3h-пиримидо[5,4-b] [1,4]тиазин-6- ил)этил] бензоил(или тиенилкарбонил)амино]пентандиовая кислота или ее низший алкиловый эфир, способ ингибирования роста и пролиферации клеток и способ ингибирования фермента
RU2135503C1 (ru) * 1992-06-19 1999-08-27 Басф Акциенгезельшафт N-замещенные производные 3-азабицикло (3.2.0)гептана или их соли с физиологически совместимыми кислотами

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU423355A1 (ru) * 1972-05-19 1995-05-27 Всесоюзный научно-исследовательский химико-фармацевтический институт им.Серго Орджоникидзе Способ получения галогенпроизводных 5н-6,7-дигидроимидазо-[2,1-b]-м-тиазина
SU1189066A1 (ru) * 1984-03-11 1990-12-07 Иркутский институт органической химии СО АН СССР Способ получени бензимидазо[2,1-в]-1,3-тиазин-2-онов
RU2135503C1 (ru) * 1992-06-19 1999-08-27 Басф Акциенгезельшафт N-замещенные производные 3-азабицикло (3.2.0)гептана или их соли с физиологически совместимыми кислотами
RU2127275C1 (ru) * 1993-01-29 1999-03-10 Агурон Фармасьютикалз, Инк. 2-[4-[2-(2-амино-4-оксо-4,6,7,8-тетрагидро-3h-пиримидо[5,4-b] [1,4]тиазин-6- ил)этил] бензоил(или тиенилкарбонил)амино]пентандиовая кислота или ее низший алкиловый эфир, способ ингибирования роста и пролиферации клеток и способ ингибирования фермента

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Publication number Publication date
WO2002014295A8 (fr) 2002-04-04
AU2001213156A1 (en) 2002-02-25

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