当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY期刊下所有文献 > Abenzyl 10-formyl-trideazafolic acid (abenzyl 10-formyl-TDAF): an effective inhibitor of glycinamide ribonucleotide transformylase.

Abenzyl 10-formyl-trideazafolic acid (abenzyl 10-formyl-TDAF): an effective inhibitor of glycinamide ribonucleotide transformylase.

Abstract：

:The synthesis of N-[7-(2-amino-3,4-dihydro-4-oxo-quinazolin-6-yl) -6-formyl-1-oxo-heptyl]-L-glutamic acid (2, abenzyl 10-formyl-5,8,10-trideazafolic acid) as a potential enzyme-assembled tight binding inhibitor of glycinamide ribonucleotide transformylase (GAR Tfase) or aminoimidazole carboxamide ribonucleotide transformylase (AICAR Tfase) is reported. The inhibitor was prepared by a convergent synthesis utilizing the sequential alkylations of acetaldehyde dimethylhydrazone with 6 and 8. The agent exhibited effective inhibition of GAR Tfase (Ki = 4.5 +/- 0.3 microM) and more modest inhibition of AICAR Tfase (Ki = 42 +/- 11 microM).

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Boger DL,Haynes NE,Warren MS,Ramcharan J,Marolewski AE,Kitos PA,Benkovic SJ

doi

10.1016/s0968-0896(97)00123-5

subject

Has Abstract

pub_date

1997-09-01 00:00:00

pages

1847-52

issue

9

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(97)00123-5

journal_volume

5

pub_type

杂志文章

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