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Literature summary for 1.5.1.3 extracted from

  • Bibi, M.; Qureshi, N.; Sadiq, A.; Farooq, U.; Hassan, A.; Shaheen, N.; Asghar, I.; Umer, D.; Ullah, A.; Khan, F.; Salman, M.; Bibi, A.; Rashid, U.
    Exploring the ability of dihydropyrimidine-5-carboxamide and 5-benzyl-2,4-diaminopyrimidine-based analogues for the selective inhibition of L. major dihydrofolate reductase (2021), Eur. J. Med. Chem., 210, 112986 .
    View publication on PubMed
Search for more literature for 1.5.1.3

Inhibitors

Inhibitors Comment Organism Structure
(2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)glutamic acid 16fold selectivity for Leishmania major enzyme over human enzyme Leishmania major
(2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)leucine 84fold selectivity for Leishmania major enzyme over human enzyme Leishmania major
(2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)phenylalanine 87fold selectivity for Leishmania major enzyme over human enzyme Leishmania major
(2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)tryptophan 10fold selectivity for Leishmania major enzyme over human enzyme Leishmania major
additional information development of antifolates based on 3,4-dihydropyrimidine-2-one and 5-(3,5-dimethoxybenzyl)pyrimidine-2,4-diamine motifs Leishmania major
trimethoprim
-
 Leishmania major

Organism

Organism UniProt Comment Textmining
Leishmania major P07382 bifunctional dihydrofolate reductase-thymidylate synthase, cf. EC 2.1.1.45
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0001
-
 pH 7, temperature not specified in the publication Leishmania major (2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)glutamic acid
0.00013
-
 pH 7, temperature not specified in the publication Leishmania major (2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)leucine
0.00014
-
 pH 7, temperature not specified in the publication Leishmania major (2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)phenylalanine
0.00018
-
 pH 7, temperature not specified in the publication Leishmania major (2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)tryptophan
0.02
-
 pH 7, temperature not specified in the publication Leishmania major trimethoprim