Synthesis of 1,3-diamino-7,8,9,10-tetrahydropyrido[3,2-f]-quinazolines. Inhibitors of Candida albicans dihydrofolate reductase as potential antifungal agents

A series of novel 1,3-diamino-7,8,9,10-tetrahydropyrido[3,2-f]quinazolines were synthesized starting from 6-amino-5-cyanoquinoline (4). These compounds inhibited Candida albicans dihydrofolate reductase with K_i values of ≤0.60 aM. One analogue exhibited moderate in vivo efficacy in a C. albicans-infected mouse model.     

Inhibitors of dihydrofolate reductase: Design,synthesis and antimicrobial activities of 2,4-diamino-6-methyl-5-ethynylpyrimidines

Novel 2,4-diamino-6-methyl-5-ethynylpyrimidines were prepared via palladium catalyzed coupling of 2,4-diamino-5-iodo-6-methyl-pyrimidine with terminal acetylenes. The compounds were inhibitors of dihydrofolate reductase and showed in vitro activity against several species of opportunistic fungi and the protozoan Toxoplasma gondii.     

Structural Properties of Cubic Sets in Regular LA-semihypergroups

In this article we characterize the regular LA-semihypergroups in terms of $({\in }_{\Gamma },{\in }_{\Gamma }\vee q_{\Delta })$-cubic (left, right, two sided, bi, generalized bi, interior, quasi)-hyperideals of LA-semihypergroups. Meanwhile, some illustrative examples are given to show the rationality of the definitions popularized in the present paper.     

Dentin Phosphoprotein Mimetic Peptide Nanofibers Promote Biomineralization

Dentin phosphoprotein (DPP) is a major component of the dentin matrix playing crucial role in hydroxyapatite deposition during bone mineralization, making it a prime candidate for the design of novel materials for bone and tooth regeneration. The bioactivity of DPP‐derived proteins is controlled by the phosphorylation and dephosphorylation of the serine residues. Here an enzyme‐responsive peptide nanofiber system inducing biomineralization is demonstrated. It closely emulates the structural and functional properties of DPP and facilitates apatite‐like mineral deposition. The DPP‐mimetic peptide molecules self‐assemble through dephosphorylation by alkaline phosphatase (ALP), an enzyme participating in tooth and bone matrix mineralization. Nanofiber network formation is also induced through addition of calcium ions. The gelation process following nanofiber formation produces a mineralized extracellular matrix like material, where scaffold properties and phosphate groups promote mineralization. It is demonstrated that the DPP‐mimetic peptide nanofiber networks can be used for apatite‐like mineral deposition for bone regeneration.     

Cytotoxic Tolerance of Healthy and Cancerous Bone Cells to Anti-microbial Phenolic Compounds Depend on Culture Conditions

Applied Biochemistry and Biotechnology - Carnosol and carnosic acid are polyphenolic compounds found in rosemary and sage with known anti-oxidant, anti-inflammatory, and anti-microbial properties....     

Synthesis of 5-(4-substituted benzyl)-2,4-diaminoquinazolines as inhibitors of candida albicans dihydrofolate reductase

Several 5-(4-substituted benzyl)-2,4-diaminoquinazolines were prepared as potentially selective inhibitors of Candida albicans dihydrofolate reductase. These compounds were synthesized by a novel route, which included as a key step the displacement of a fluoro group in 2,6-difluorobenzonitrile by the anions of ethyl or methyl 4-substituted phenylacetates. The resultant diarylacetates were saponified and decarboxylated to the 2-fluoro-6-(4-substituted phenyl)benzonitriles. Ring closure of these benzonitriles with guanidine carbonate gave the 5-(4-substituted benzyl)-2,4-diaminoquinazolines.