N-(1,3-tiazol-2-yl)amides of 2-diphenylmethylenehydrazono-5,5-dimethyl-2,4-dioxohexane acid, demonstrating anti-inflammatory and analgetic activity and method of obtaining

FIELD: chemistry, pharmaceutics.

SUBSTANCE: invention relates to novel compounds N(1,3-tiazol-2-yl)amides of 2-diphenylmethylenehydrazono-5,5-dimethyl-2,4-diooxohexane acid of formula (Ia, b): demonstration anti-inflammatory and analgetic activity. Invention also relates to method of their obtaining.

EFFECT: obtaining novel compounds.

2 cl, 1 tbl, 2 ex

 

The invention relates to the field of organic chemistry, derivatives of acyclic polycarboxylic compounds, namely to new N-(1,3-thiazol-2-yl)Amida 2-diphenylethylenediamine-5,5-dimethyl-2,4-docohexaenoic acid of formula (Ia, b):

exhibiting anti-inflammatory and analgesic activity, which can find application in medicine as a drug. Known structural analogue of the claimed compounds is N-(1,3-thiazol-2-yl)amide 3-hydroxy-5,5-dimethyl-4-oxo-2-hexenoic acid (II), obtained by the interaction evaluierungen acid with 2-aminothiazolo [Berezina B.C., Kozminykh V.O., Hidow NM, Shirinkina SS, Kozminykh E.N., Makhmudov P.P., bocanova E.V., Ukr. body. chemistry. 2001. V.37. No. 4. N.574-581]. The structural analogue synthesis is carried out according to the following scheme:

The disadvantages of this method include the inability to obtain N-(1,3-thiazol-2-yl)amides 2-diphenylethylenediamine-5,5-dimethyl-2,4-docohexaenoic acid.

The objective of the invention is to develop a method of synthesis of previously undescribed N-(1,3-thiazol-2-yl)amides 2-diphenyl-metilgidrata-5,5-dimethyl-2,4-docohexaenoic acid (Ia, b), showing a higher anti-inflammatory and analgesic effects and has a lower toxicity than the known medicines.

The task is carried out by briefly heating 5-tert-butyl-3-diphenylhydrazone-2,3-dihydro-2-furanone (III) [Vasiliev N.N., Hidow NM Herald student society. Perm, PHFA. 2006. No. 1 P.35] 2-aminothiazole or 2-amino-4-phenylthiazole in an environment of absolute toluene under the scheme:

Example obtain the claimed compound Ia:

To a solution of 0.15 g (0,0015 mol) of 2-aminothiazole in 10 ml of absolute toluene is added a solution of 0.5 g (0,0015 mol) of furanone (III) in 40 ml of absolute toluene and heated for 5 minutes. The mixture is left for the day. The solvent is evaporated, the solid residue is crystallized from ethanol or ethyl acetate. Obtain 0.45 g (69%) of colorless crystalline compound (Ia) with Tpl.=175-176°C. C24H24N4SO2. Mm=432,55. IR spectrum, v, cm-1(the crystals):1708 (C=O),1610 (C=N). Range of TMR, δ, ppm, DMSO-d6: 1,09 (N, (CH3)3), 4,07 (2H, CH2), 7,16-7,39 m (N, 2C6H5, thiazolyl), 11,4 ush. s (1H, NH).

Example obtain the claimed compound 1B:

To a solution of 0.26 g (0,0015 mol) 2-amino-4-phenylthiazole in 10 ml of absolute toluene is added a solution of 0.5 g (0,0015 mol) of furanone (III) in 40 ml of absolute toluene and heated for 5 minutes. The mixture is left for the day. The solvent is evaporated, dry OST the current crystallized from ethanol. Obtain 0.51 g (66%) of crystalline compound (Ia) yellow with Tpl.=189-190°C. C30H28N4SO2. Mm=508,63. IR spectrum, v, cm-1(the crystals):1710 (C=O),1618 (C=N). Range of TMR, δ, M. D. DMSO-d6: 1,15 (N, (CH3)3), 4,18 (2H, CH2),? 7.04 baby mortality-7,71 m (N, 3C6H5, thiazolyl), 9,92 ush. s (1H, NH).

The compounds (Ia, b) - substances that are soluble in dimethyl-sulfoxide and dimethylformamide, sparingly soluble in alcohol and ethyl acetate, insoluble in hexane and water.

Study of anti-inflammatory, analgesic activity and acute toxicity were performed in the laboratory of BAS Science Institute of Perm state University.

Acute toxicity (LD50(mg/ml) of compounds (Ia, b) was determined by the method Hendersen [Pershin GN. Methods experimental chemotherapy // M, P.100, 109-117 (1971)]. Compounds (Ia, b) were injected intraperitoneally white mice weighing 16-18 g in the form of a suspension in 2% starch mucus. For the studied compounds (Ia, b) LD50is >1500 mg/kg

According to the classification of the toxicity of preparations of compound (Ia, b) belong to V class practically non-toxic drugs [Izmerov NF, Capocci I., Sidorov, K.K. Settings toxicometric industrial poisons. - M.: Medicine, 1977. - s].

Against the inflammatory activity was studied on white Wistar rats weighing 170-200 g Antiexudative effect of compounds (Ia, b) evaluated on the model of acute inflammatory swelling of the feet, caused by subplantar injection of 0.1 ml of 1% solution carragenin. The index action of the studied compounds, administered orally in a dose of 50 mg/kg in 2% solution of starch mucus, served as the amount of swelling of the legs, defined ecometrics. About the power antiexudative action judged by the degree of inhibition of the inflammatory response in % of control [Methodical recommendations on experimental preclinical study non-steroidal anti-inflammatory pharmacological substances. M - 1982. - 17 S. Approved by the Pharmacological Committee of Ministry of health USSR 11 November 1992 Protocol No. 22]. Compared the effect voltaren dose of 10 mg/kg [Neugodova VP, Zaichenko GV, Ryndin S.E. Toxicological evaluation voltaren // Pharmacologist and toxicologist. - 1986. V.49. No. 1 P.123].

Analgesic activity of the compounds (Ia, b) studied in outbred mice weighing 18-22 g with test "hot plate" [Radell Z.O., Selitto J.J. A method for measurement of analgesic activity on inflamed tissue. // Arch. Intermat. Pharmacodun. Et ther. 1957. - Vol.11. No. 4. - S.409-419].

The investigated compounds were administered intraperitoneally in the form of 2% starch mucilage in the dose of 50 mg/kg for 0.5 h before the animals on the premises heated to 53.5°With metal plate. Measure of pain sensitivity was the duration PROPYLENEIMINE on a hot plate until the licking of the hind paws, measured in seconds.

The results of the tests are presented in table

ConnectionAcute toxicity LD50mg/kgAnti-inflammatory effect, karragenana modelAnalgesic effects by the method of "hot plate"through 120 minutes
Dose, mg/kgInhibition of edema, %Dose, mg/kgDefensive reflex,
Ia>15005053,85037,00±2,30

p<0,5
IB>15005057,005036,20±5,18

p<0,5
Voltaren3801053,91026,3

As can be seen from the table, the claimed compounds (Ia, b) have a pronounced anti-inflammatory and analgesic activity, less toxic, than the comparison drug voltaren. Therefore, the claimed compounds (Ia, b) can find application in medical practice as anti-inflammatory and analgesic drugs.

1. N-(1,3-Thiazol-2-yl)amides of 2-diphenylethylenediamine-5,5-dimethyl-2,4-dioxopentanoate sour is you General formula Ia, b

possessing anti-inflammatory and analgesic activity.

2. The method of obtaining N-(1,3-thiazol-2-yl)amides 2-diphenylethylenediamine-5,5-dimethyl-2,4-docohexaenoic acid of General formula Ia, b

characterized in that 5-tert-butyl-3-diphenylhydrazone-2,3-dihydro-2-furanone subjected to interaction with 2-aminothiazole or 2-amino-4-phenylthiazole when heated in an environment of absolute toluene.



 

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12 cl, 1 tbl, 34 ex

FIELD: organic chemistry, biochemistry, medicine, endocrinology.

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8 cl, 6 tbl, 88 ex

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either G1 represents -CH2-X2-(CH2)a-G3, and G2 represents H, or G2 represents -CH2-(CH2)a-G3, and G1 represents H; G3 is selected from group according to general formula 2 ,

group according to general formula 3

and group according to general formula 4 ;

a is 0, 1 or 2; b is 1 or 2; X1 is selected from CH2, S, CF2, CHF and O; X2 is selected from CH2; X3, X4 and X5 are selected from N; X6 is selected from NH; X7 is selected from NH; R1 is selected from H and CN; R2 represents H; R3 is selected from H, Cl, OH, NH2, NH-C1-C10alkyl and N(C1-C10alkyl)2; R4, R5, R6, R7 and R8 are independently selected from H, Br, Cl, F, OH, NO2; R9 represents H; R10, R11, R12, R13 and R14 are independently selected from H, Cl and CF3; R15 and R16 are independently selected from H, C1-C10alkyl, C1-C10alkenyl, C3-C10cycloalkyl, C3-C10cycloalkenyl, quinoline, naphtyl and -CH2-L-R17; R17 is selected from C1-C10alkyl, phenyl, naphtyl, quinolinyl and indolyl; L is selected from covalent bond, CH=CH and -C6H4-; on condition that when R15 and R16 both represent H, and b is 1, then X1 does not represent S or CH2.

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58 cl, 10 tbl, 1705 ex

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