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РЖ ВИНИТИ 34 (BI48) 96.05-04Т2.300

Rosowsky, Andre.
Synthesis and antifolate activity of 2,4-diamino-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine analogues of trimetrexate and piritrexim [Text] / Andre Rosowsky, Clara E. Mota, Sherry F. Queener // J. Heterocycl. Chem. - 1995. - Vol. 32, N 1. - P335-340 . - ISSN 0022-152X
Перевод заглавия: Синтез и антифолатная активность 2,4-диамино-5,6,7,8-тетрагидропиридо [4,3-d]пиримидина - аналога триметрексата и пиритрексима
Аннотация: 2,4-Diamino-5,6,7,8-tetrahydropyrido [4,3-d]pyrimidines with di- and trimethoxyaralkyl substitution at the 6-position were synthesized from the N{6}-unsubstituted compound and appropriate aralkyl bromides in N.N-dimethylformamide solution containing a catalytic amount of sodium iodide. An improved method of preparation of 2,4-diamino-5,6,7,8-tetrahydropyrido[4.3-d]pyrimidine from 2-amino-6-benzyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4 (3H)-one was also developed. In assays of the ability of the products to inhibit dihydrofolate reductase from Pneumocystis carinii, and Toxoplasma gondii, and rat liver the most active of the compounds tested was 2,4-diamino-6-(2'-bromo-3',4',5'-trimethoxybenzyl)-5,6,7,8- tetrahydropyrido[4,3-d]pyrimidine (I). The concentration of this compound needed to inhibit enzyme activity by 50% was 0.51 'мю'M against the P.carinii enzyme, 0.09 'мю'M against the T.gondii enzyme, and 0.35 'мю'M against the rat enzyme. Thus, there was selectivity of binding to T.gondii enzyme, but not P.carinii enzyme, relative to rat enzyme. I showed greater selectivity than trimetrexate or piritrexim for the P.carinii and T.gondii enzyme, but was less selective than trimethoprim or pyrimethamine. However its molar potency against both enzymes was greater than that of trimethoprim, the antifolate most commonlt used, in combination with sulfamethoxazole, for initial treatment of opportunistic P.carinii and T.gondii infections in patients with AIDS and other disorders of the immune system. США, Dep. of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115. Библ. 45

ГРНТИ	34.45.21

ВИНИТИ 341.45.21.95.41.99
Рубрики: ПРОТИВОПРОТОЗОЙНЫЕ СРЕДСТВА
2,4-ДИАМИНО-5,6,7,8-ТЕТРАГИДРОПИРИДО [4,3D]ПИРИМИДИН
СИНТЕЗ
АНТИФОЛАТНАЯ АКТИВНОСТЬ
ДИГИДРОФОЛАТРЕДУКТАЗЫ ИНГИБИТОРЫ
PNEUMOCYSTIS CARINI
TOXOPLASMA GONDII
ПЕЧЕНЬ КРЫС
ОППОРТУНИСТИЧЕСКИЕ ИНФЕКЦИИ
СПИД

Доп.точки доступа:
Mota, Clara E.; Queener, Sherry F.

"Электронные каталоги и базы данных библиотек СО РАН"

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