159382-39-5Relevant academic research and scientific papers
Conformationally restricted tricyclic analogues of lipophilic pyrido[2,3-d]pyrimidine antifolates [1a,b]
Gangjee,Mavandadi,Queener
, p. 213 - 220 (2007/10/03)
The effect of conformational restriction of the C9-N10 bridge on inhibitory potency and selectivity of trimetrexate against dihydrofolate reductase, was studied. Specifically three nonclassical tricyclic 1,3-diamino-8-(3′,4′,5′-trimethoxybenzyl)-7,9-dihydro- pyrrolo[3,4-c]pyrido[2,3-d]pyrimidin-6(5H,8H)-one (4), 1,3-diamino-8-(3′,4′,5′-trimethoxybenzyl)-9-hydro-pyrrolo [3,4-c]pyrido[2,3-d]pyrimidin-6-(8H)-one (5) and 1,3-diamino-(8H)-(3′,4′,5′-trimethoxybenzyl)-7,9-dihydro- pyrrolo[3,4-c]pyrido[2,3-d]pyrimidine (7) antifolates were synthesized. The tricyclic analogues 4 and 5 were obtained via the regiospecific cyclo-condensation of the β-keto ester 17 with 2,4,6-triaminopyrimidine. The analogue 7 was obtained via reduction of the lactam 4 with borane in tetrahydrofuran. Compounds 4, 5 and 7 were evaluated as inhibitors of dihydrofolate reductase from Pneumocystis carinii, Toxoplasma gondii and rat liven All three compounds were more selective than trimetrexate against Pneumocystis carinii dihydrofolate reductase and significantly more selective than trimetrexate against Toxoplasma gondii dihydrofolate reductase compared with rat liver dihydrofolate reductase.
6,7-dihydropyrrol[3,4-c]pyrido[2,3-d]pyrimidine derivatives
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, (2008/06/13)
The present invention concerns compounds of the formula: STR1 wherein R is a lower alkyl group, an aryl group or an alkylaryl group and X and Y are the same or different, and each is OH, NH2, or SH. The aryl group or the aryl moiety of the alkylaryl group may be unsubstituted, monosubstituted, disubstituted or trisubstituted. If substituted, each substituent may independently be an alkyl group, an alkyloxy group or a halogen. The present invention also provides methods for synthesizing the compounds described above.
