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diaminoquinazoline

 
National Institutes of Health

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2019
2019
Diaminoquinazoline MMV675968 from Pathogen Box inhibits Acinetobacter baumannii growth through targeting of dihydrofolate reductase
Antibiotic resistance in Acinetobacter baumannii is a major global health threat. New drugs with novel chemical structures are… Expand
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2018
2018
Development of a Photo-Cross-Linkable Diaminoquinazoline Inhibitor for Target Identification in Plasmodium falciparum.
Diaminoquinazolines represent a privileged scaffold for antimalarial discovery, including use as putative Plasmodium histone… Expand
2018
2018
Activation of 2,4-Diaminoquinazoline in Mycobacterium tuberculosis by Rv3161c, a Putative Dioxygenase
The diaminoquinazoline series has good potency against Mycobacterium tuberculosis. Resistant isolates have mutations in Rv3161c… Expand
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Highly Cited
2015
Highly Cited
2015
Rational targeting of active-site tyrosine residues using sulfonyl fluoride probes.
This work describes the first rational targeting of tyrosine residues in a protein binding site by small-molecule covalent probes… Expand
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Highly Cited
2014
Highly Cited
2014
Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
A new series of dihydrofolate reductase (DHFR) inhibitors, the 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines, were designed and… Expand
2014
2014
Development of Diaminoquinazoline Histone Lysine Methyltransferase Inhibitors as Potent Blood‐Stage Antimalarial Compounds
Modulating epigenetic mechanisms in malarial parasites is an emerging avenue for the discovery of novel antimalarial drugs… Expand
2012
2012
Design, synthesis, and biological evaluation of new diaminoquinazolines as β-catenin/Tcf4 pathway inhibitors.
More than 50 new diaminoquinazoline derivatives have been synthesized and evaluated in a colon carcinoma cell growth inhibition… Expand
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Highly Cited
1998
Highly Cited
1998
Computation of affinity and selectivity: Binding of 2,4-diaminopteridine and 2,4-diaminoquinazoline inhibitors to dihydrofolate reductases
Binding energy calculations for complexes of mutant and wild-type human dihydrofolate reductases with 2,4-diaminopteridine and 2… Expand
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1994
1994
Structurally distinct MDR modulators show specific patterns of reversal against P-glycoproteins bearing unique mutations at serine939/941.
The mechanism by which P-glycoprotein (P-gp) interacts with a number of structurally unrelated substrates or inhibitors remains… Expand
1977
1977
Potent inhibitory activity of trimethoxyquine (tmq), "nonclassical" 2,4, diaminoquinazoline, on mammalian dna synthesis. Abstr.
 
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