3-(2'-naphthylmethyl)-piperazine-2 and 1-n-phenyl-3 - ventilationperfusion-2, exhibiting anti-inflammatory activity

 

(57) Abstract:

3-(21-Naphthylmethyl)-piperazine-2 (1) and 1-N-phenyl-3-piperazino-2 (II) formula

< / BR>
where I R = 2-naphthyl; R1= N;

II R = C6H5; R1= C6H5.

can be used in medicine as anti-inflammatory agents. They get interaction arilpirolilor acids with Ethylenediamine and N-phenylethylenediamine, respectively, when heated in ethanol medium in the presence of catalytic amounts of acetic acid according to the scheme

< / BR>
where I R = 2-naphthyl; R1= H;

II R = C6H5; R1= C6H5.

I. The Output Is 78.4%. Tpl.241-242oC.

Found, %: C 72,32; N. Of 5.17; N 10,56%; C16H14N2O2.

Calculated,%: C 72,17; H Of 5.29; N 10,52.

II. Yield 68%. Tpl.140-141oC.

Found, %: C 73,80; N. Of 5.39; N 9,72; C18H16N2O2.

Calculated, %: C 73,95; N 5,52; N 9,58.

The compounds possess anti-inflammatory activity of 45% (I) and 51% (II). Toxicity LD50is more than 1000 mg/kg 1 tab.

The invention relates to new biologically active compounds 2-piperazinone, namely 3-(2=H;

II R C6H5; RIC6H5.

possessing anti-inflammatory activity, suggesting the possibility of their use in medicine as anti-inflammatory drugs.

The closest analogue to the structure with anti-inflammatory activity is 3-(4I-methylbenzylidene)-piperazine-2 formula:

< / BR>
which is used as a prototype [1,2]

The objective of the invention, the search range 2-piperazinone compounds with pronounced anti-inflammatory activity with low toxicity.

This is achieved by the synthesis of 3-(2I-naphthylmethyl)- and 1-N-phenyl-3-ventilationperfusion-2-ions containing 3-substituted and 1,3-substituted 2-piperazinone cycle, which has anti-inflammatory action.

The claimed compounds produced by interaction arilpirolilor acids with Ethylenediamine and N-phenylethylenediamine, respectively, when heated in ethanol medium in the presence of catalytic amounts of acetic acid and subsequent separation of the target products by the known methods.

The reaction scheme:

< / BR>
where I R 2-naphthyl; R1H;

II R C6H5; RIC6H5.

oC.

Found, C 72,32; N. OF 5.17; N 10,56; C16H14N2O2.

Calculated C 72,17; N. Of 5.29; N 10,52.

IR spectrum (VR-20) vaseline oil, cm-1: 3200, 3112 (amino group); 1692 (amide carbonyl); 1608 (-carbonyl).

PMR spectrum (OC-2310, DMCO, GMDS, M. D.): 3,53 (int. m, 4H, CH2- CH2); 6,91 (C. 1H, CH); 8,08 (m N10H7); 8,77 (C. 1H, NH); 11,05 (C. 1H, NH).

Compound II get the same way.

Yield 1.98 g (68%), so pl. 140 -141oC.

Found, C 73,80; N. OF 5.39; N 9,72; C18H16N2O2.

Calculated C 73,95; N 5,52; N 9,58.

IR-spectrum (UR-20) vaseline oil, cm-1: 3376 (amino group); 1692 (amide carbonyl); 1616 (g-carbonyl).

PMR-spectrum (OC-2310, DMSO, GMDS, M. D.): 3,88 (int. m, 4H, CH2CH2); 6,77 (C. 1H, CH); to 7.67 (m, 10H, 2C6H5); 11,12 (C. 1H, NH).

The claimed compounds are yellow crystalline substance, easily soluble in DMSO and DMF, soluble in hot ethanol, benzene, sparingly soluble in water.

The compounds of bilene in oral introduction of the investigated compounds at a dose of 50 mg/kg, ortofena in the dose of 10 mg/kg [3]

About anti-inflammatory activity was judged by the degree of inhibition of the inflammatory response in Aggregate ED50and LD50was carried out according to the method of Litchfield and Wilcoxon signed [4]

The results of studies anti-inflammatory activity are presented in the table.

From the table it is seen that the claimed compounds possess anti-inflammatory action, toxicity several times less toxic than used in medicine, the drug may also fuse [5]

Acute toxicity of the claimed compounds was determined in oral introduction connections to white mice. 2% starch mucus, N. Pershin [6] LD50the claimed compounds is more than 1000 mg/kg

Thus, 3-(2I-naphthylmethyl)-piperazine-2 - and 1-N-phenyl-3-ventilationperfusion-2, as shown by experimental studies, have a pronounced anti-inflammatory action. The toxicity of the compounds of more than 1000 mg/kg, equivalent to more than 1000 mg/kg and ortofena 380 mg/kg

3-(21-Naphthylmethyl)-piperazine-2 (I) and 1-N-phenyl-3-ventilationperfusion-2 (II) formula

< / BR>
where I R=2-naphthyl, R'=H;

II R=C6H5; R'=C6H5,

have the

 

Same patents:

The invention relates to the production of 2-piperazinone

-phenylpiperazine)ethyl] benzamide, possessing neuroleptic activity, and 3 - methyl-n-[2-(4-phenylpiperazine)ethyl]benzamide as a starting compound for the synthesis of" target="_blank">

The invention relates to new chemical compounds of the hydrochloride of 3-methyl-N-[2-(4-phenylpiperazine)ethyl]benzo - foreign formula I

< / BR>
(I) possessing neuroleptic activity, and 3-methyl-N-[2-(4-phenylpiperazine)ethyl] benzamide as starting compounds in the synthesis of hydrochloride of 3-methyl-N-[2-(4-phenylpiperazine)ethyl]benzo - Mead

The invention relates to new Daminova compounds and their acid additive salts and cerebral protective medicines containing these compounds or their salts, more particularly to Daminova compounds and their acid additive salts, which are characterized by excellent cerebral protective effect and are used as medicines in the treatment of disorders of cerebral function or to prevent the development of such disorders, and cerebral protective medicines containing diamino compounds or their acid additive salt

The invention relates to new nitrogen-containing heterocyclic compounds, in particular to derive hinzelin or benzodiazepina.beloe acid formula

(I) where R is hydrogen, halogen, lower alkyl or lower alkoxygroup;

And group O or S;

In group-CH2-CH2or СНR1where R1means hydrogen, lower alkyl or hydroxyl;

X is oxygen or the group NH

The Y group of the formula)qwhere R2means lower alkyl, q is 2 or 3, and their salts, in particular physiologically tolerable salts, which possess pharmacological activity, in particular activity antimuskarinovoe act occurs, and therefore can be used to treat diseases of the gastrointestinal tract and respiratory tract

The invention relates to compounds of the formula I

(I) or pharmaceutically acceptable salt accession acids him or stereoisomeric form of the compound, where

-A1= AND2- A3= AND4- bivalent radical having the formula

-CH=CH-CH=CH- (a-1)

-N=CH-CH=CH- (a-2)

-CH=CH-CH=N (a-5) or

-N=CH-N=CH- (and-6),

n=1 or 2

IN - NR4or CH2< / BR>
R4is hydrogen or C1-C6alkyl

L is hydrogen, C1-C6alkyl, C1-C6allyloxycarbonyl, or a radical of the formula

-Alk - R5(b-1),

-Alk - Y - R6(b - 2),

-Alk - Z1- C(=X) - Z2- R7(b-3), or

-CH2- SNON - CH2- O - R8(b-4), where R5is cyano, phenyl optionally substituted C1-C6alkyloxy; pyridinyl; 4,5-dihydro-5-oxo-1-N-tetrazolyl; 2-oxo-3-oxazolidinyl; 2,3-dihydro-2-oxo-1-N-benzimidazolyl; or bicycling radical of formula (C-4-a)

Gwhere G2- CH=CH-CH=CH-, -S-(CH2)3,- -S-(CH2)/2-, -S-CH=CH - or-CH=C(CH3)-O-;

R6- C1-C6-alkyl, pyridinyl optionally substituted by nitro; pyrimidinyl; feast
R7- C1-C6-alkyl; halophenol; 1-methyl-1H-pyrrolyl; furanyl, thienyl, or aminopyrazine;

R8- halophenol;

Y is O or NH;

Z1or Z2each independently NH or a direct link X-O

each Аlk independently - C1-C6alcander

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EFFECT: improved preparing method, valuable biochemical and medicinal properties of compounds.

14 cl, 36 ex

FIELD: medicine, oncohematology.

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EFFECT: higher efficiency of therapy.

1 ex, 5 tbl

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12 cl, 2 ex

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EFFECT: higher efficiency of therapy.

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Endoparasitic agent // 2250779

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6 cl, 7 ex, 7 tbl

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59 cl, 12 dwg, 13 ex, 10 tbl

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or

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1 ex

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EFFECT: improved and valuable medicinal properties of agent.

18 cl, 18 tbl, 7 ex

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