Fedosov A. Synthesis transformation and biological activity of 5-methyl-thieno[2,3-d]pyrimidine-6-carboxylic acid and 3-amino-5-methyl-4-oxo-2-thioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidine-6-carboxylic acid derivatives

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0409U001370

Thesis Registration Form

0409U001370.pdf

Applicant for

Fedosov Andrii Igorevich

Specialization

15.00.02 - Фармацевтична хімія та фармакогнозія

Date of defense

20-03-2009

Specialized Academic Board

Д64.605.01

Essay

The methods for synthesis of ethylic ester of 5-methyl-4-thioxo-3,4-di-hydro-thieno[2,3-d]pyrimidine-6-carboxylic acid, the products of its alkylation and its 4-hydrazino-analogue were developed; the reactions of the last one with acylating agents were studied. The series of compounds with 9-R1-8-R2-2,3-di-hydro-thieno[3,2-e][1,2,4]tri-azolo[4,3-c]pyrimidine-3-one moiety was obtained; their alkylation mainly occurs on the N atom in position 2. The esters of 3-amino-2-alkylthio-5-methyl-4-oxo-1,2,3,4-tetrahydro-thie-no-[2,3-d]pyrimidine-6-carboxylic acid, 2-alkyl-6-methyl-5-oxo-5H-[1,3,4]thiadia-zolo[3,2-a]thieno[2,3-d]pyrimidine-7-carboxylates and alkyl 6-meth-yl-5-oxo-2-(3-aryl)-5H-[1,3,4]thiadiazolo[3,2-a]thieno[2,3-d]pyrimidine-7-carb-oxy-lates as well as the derivatives of 7-methyl-6-oxo-2H,6H-thie-no[2',3':4,5]pyrimido[2,1-b]-[1,3,4]-thi-adiazine-8-carboxylic acid were obtained. It was found that 3-amino-5-methyl-2-(4-methylbenzylthio)-4-oxo-3,4-dihyd-ro-thieno[2,3-d]pyrimidine-6-carboxylate displays the high range of analgesic and anti-inflammatory activity; N8-(2-chlorophenyl)-7-methyl-6-oxo-3-phenyl-2H,6H-thi-eno[2',3':4,5]pyrimido[2,1-b][1,3,4]thiadiazine-8-carboxamide (for С. albicans: MBSТC = 15,6 ?g/mL, МBCC = 31,25 ?g/mL) is the most active among the compounds being tested for antimicrobial activity.

Thesis supervisor

Kovalenko Sergei Mikolaevich

Official opponents

Болотов Валерій Васильович
Демченко Анатолій Михайлович

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