Trimethoprim

Papers

1. Characterization of Candida albicans dihydrofolate reductase. D.P. Baccanari et al. J. Biol. Chem. 264, 1100, (1989)

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2. Effects of conversion of phenylalanine-31 to leucine on the function of human dihydrofolate reductase. N.J. Prendergast et al. Biochemistry 28, 4645, (1989)

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T-lineage cells require the thymus but not VDJ recombination to produce IL-17A and regulate granulopoiesis in vivo. Emily Smith et al J. Immunol. 183, 5685-93, (2010)

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Design, synthesis, and antifolate activity of new analogues of piritrexim and other diaminopyrimidine dihydrofolate reductase inhibitors with omega-carboxyalkoxy or omega-carboxy-1-alkynyl substitution in the side chain. David C M Chan et al J. Med. Chem. 48, 4420-31, (2005)

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Analysis of complexes of inhibitors with Cryptosporidium hominis DHFR leads to a new trimethoprim derivative. Veljko M Popov et al Bioorg. Med. Chem. Lett. 16, 4366-70, (2006)

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Design and synthesis of classical and nonclassical 6-arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as antifolates. Aleem Gangjee et al J. Med. Chem. 50, 3046-53, (2007)

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Novel boron-containing, nonclassical antifolates: synthesis and preliminary biological and structural evaluation. Robert C Reynolds et al J. Med. Chem. 50, 3283-9, (2007)

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Crystal structure of the anthrax drug target, Bacillus anthracis dihydrofolate reductase. Brad C Bennett et al J. Med. Chem. 50, 4374-81, (2007)

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Highly Efficient Ligands for Dihydrofolate Reductase from Cryptosporidium hominis and Toxoplasma gondii Inspired by Structural Analysis. Pelphrey, P.M., et al. J. Med. Chem. 50(5), 940-950, (2007)

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QSAR study on permeability of hydrophobic compounds with artificial membranes. Masaaki Fujikawa et al Bioorg. Med. Chem. 15, 3756-67, (2007)

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Structure-based design, synthesis and preliminary evaluation of selective inhibitors of dihydrofolate reductase from Mycobacterium tuberculosis. Mervat H R I El-Hamamsy et al Bioorg. Med. Chem. 15, 4552-76, (2007)

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Hologram QSAR model for the prediction of human oral bioavailability. Tiago L Moda et al Bioorg. Med. Chem. 15, 7738-45, (2007)

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Clonal diversity and resistance mechanisms in tetracycline-nonsusceptible Streptococcus pneumoniae isolates in Poland. Radosław Izdebski et al Antimicrob. Agents Chemother. 51, 1155-63, (2007)

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Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis. Sang Hyun Cho et al Antimicrob. Agents Chemother. 51, 1380-5, (2007)

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Two new dfr genes in trimethoprim-resistant integron-negative Escherichia coli isolates. M Grape et al Antimicrob. Agents Chemother. 51, 1863-4, (2007)

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Spread of extended-spectrum beta-lactamase CTX-M-producing escherichia coli clinical isolates in community and nosocomial environments in Portugal. Nuno Mendonça et al Antimicrob. Agents Chemother. 51, 1946-55, (2007)

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PhoU is a persistence switch involved in persister formation and tolerance to multiple antibiotics and stresses in Escherichia coli. Yongfang Li et al Antimicrob. Agents Chemother. 51, 2092-9, (2007)

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Interaction of the GraRS two-component system with the VraFG ABC transporter to support vancomycin-intermediate resistance in Staphylococcus aureus. Michael Meehl et al Antimicrob. Agents Chemother. 51, 2679-89, (2007)

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Prevalence and expression of the plasmid-mediated quinolone resistance determinant qnrA1. Xiaogang Xu et al Antimicrob. Agents Chemother. 51, 4105-10, (2007)

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The PhoQ-activating potential of antimicrobial peptides contributes to antimicrobial efficacy and is predictive of the induction of bacterial resistance. Jason Kindrachuk et al Antimicrob. Agents Chemother. 51, 4374-81, (2007)

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In vitro efficacy of new antifolates against trimethoprim-resistant Bacillus anthracis. Esther W Barrow et al Antimicrob. Agents Chemother. 51, 4447-52, (2007)

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In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates. Kristi L Frank et al Antimicrob. Agents Chemother. 51, 888-95, (2007)

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Chemical genetics reveals a complex functional ground state of neural stem cells Diamandis, P., et. al. Nat. Chem. Biol. 3(5), 268-273, (2007)

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Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2). Jenny M Pedersen et al J. Med. Chem. 51, 3275-87, (2008)

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The effect of 5-alkyl modification on the biological activity of pyrrolo[2,3-d]pyrimidine containing classical and nonclassical antifolates as inhibitors of dihydrofolate reductase and as antitumor and/or antiopportunistic infection agents. Aleem Gangjee et al J. Med. Chem. 51, 4589-600, (2008)

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Determination of log D via automated microfluidic liquid-liquid extraction. Muhammad Alimuddin et al J. Med. Chem. 51, 5140-2, (2008)

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Potent dual thymidylate synthase and dihydrofolate reductase inhibitors: classical and nonclassical 2-amino-4-oxo-5-arylthio-substituted-6-methylthieno[2,3-d]pyrimidine antifolates. Aleem Gangjee et al J. Med. Chem. 51, 5789-97, (2008)

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Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1. Gustav Ahlin et al J. Med. Chem. 51, 5932-42, (2008)

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N9-substituted 2,4-diaminoquinazolines: synthesis and biological evaluation of lipophilic inhibitors of pneumocystis carinii and toxoplasma gondii dihydrofolate reductase. Aleem Gangjee et al J. Med. Chem. 51, 6195-200, (2008)

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Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors. Lourdes Santana et al J. Med. Chem. 51, 6740-51, (2008)

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Design, synthesis, and biological evaluation of classical and nonclassical 2-amino-4-oxo-5-substituted-6-methylpyrrolo[3,2-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors. Aleem Gangjee et al J. Med. Chem. 51, 68-76, (2008)

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Synthetic and crystallographic studies of a new inhibitor series targeting Bacillus anthracis dihydrofolate reductase. Jennifer M Beierlein et al J. Med. Chem. 51, 7532-40, (2008)

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Support vector machines classification of hERG liabilities based on atom types. Lei Jia et al Bioorg. Med. Chem. 16, 6252-60, (2008)

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Profiling Protein Arginine Deiminase 4 (PAD4): a novel screen to identify PAD4 inhibitors. Bryan Knuckley et al Bioorg. Med. Chem. 16, 739-45, (2008)

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In vitro activity of AR-709 against Streptococcus pneumoniae. W T M Jansen et al Antimicrob. Agents Chemother. 52, 1182-3, (2008)

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Role of the AheABC efflux pump in Aeromonas hydrophila intrinsic multidrug resistance. Mathieu Hernould et al Antimicrob. Agents Chemother. 52, 1559-63, (2008)

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The Lys234Arg substitution in the enzyme SHV-72 is a determinant for resistance to clavulanic acid inhibition. Nuno Mendonça et al Antimicrob. Agents Chemother. 52, 1806-11, (2008)

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Staphylococcus aureus cell wall stress stimulon gene-lacZ fusion strains: potential for use in screening for cell wall-active antimicrobials. Rebecca Steidl et al Antimicrob. Agents Chemother. 52, 2923-5, (2008)

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Spread of OXA-48-positive carbapenem-resistant Klebsiella pneumoniae isolates in Istanbul, Turkey. Amélie Carrër et al Antimicrob. Agents Chemother. 52, 2950-4, (2008)

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Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France. Vincent Cattoir et al Antimicrob. Agents Chemother. 52, 3801-4, (2008)

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Cloning, expression, and characterization of Babesia gibsoni dihydrofolate reductase-thymidylate synthase: inhibitory effect of antifolates on its catalytic activity and parasite proliferation. Gabriel O Aboge et al Antimicrob. Agents Chemother. 52, 4072-80, (2008)

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Characterization of TolC efflux pump proteins from Pasteurella multocida. Tamas Hatfaludi et al Antimicrob. Agents Chemother. 52, 4166-71, (2008)

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Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics. Sreedhar Subramanian et al Antimicrob. Agents Chemother. 52, 427-34, (2008)

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Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus. Daniel R Gentry et al Antimicrob. Agents Chemother. 52, 4507-9, (2008)

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Reduced Susceptibility of Proteus mirabilis to triclosan. David J Stickler et al Antimicrob. Agents Chemother. 52, 991-4, (2008)

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A domino effect in antifolate drug action in Escherichia coli. Yun Kyung Kwon et al Nat. Chem. Biol. 4, 602-8, (2008)

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Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. R Scott Obach et al Drug Metab. Dispos. 36, 1385-405, (2008)

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Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models. Naomi L Kruhlak et al Toxic. Mech. Methods 18, 217-27, (2008)

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Synthesis and evaluation of 4-acyl-2-thiazolylhydrazone derivatives for anti-Toxoplasma efficacy in vitro. Franco Chimenti et al J. Med. Chem. 52, 4574-7, (2009)

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Physicochemical determinants of human renal clearance. Manthena V S Varma et al J. Med. Chem. 52, 4844-52, (2009)

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Design, synthesis, and X-ray crystal structure of classical and nonclassical 2-amino-4-oxo-5-substituted-6-ethylthieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors and as potential antitumor agents. Aleem Gangjee et al J. Med. Chem. 52, 4892-902, (2009)

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Novel non-active site inhibitor of Cryptosporidium hominis TS-DHFR identified by a virtual screen. W Edward Martucci et al Bioorg. Med. Chem. Lett. 19, 418-23, (2009)

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Discovery and optimization of antibacterial AccC inhibitors. Cliff C Cheng et al Bioorg. Med. Chem. Lett. 19, 6507-14, (2009)

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In vitro biological activity and structural analysis of 2,4-diamino-5-(2'-arylpropargyl)pyrimidine inhibitors of Candida albicans. Janet L Paulsen et al Bioorg. Med. Chem. 17, 4866-72, (2009)

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Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors. Aleem Gangjee et al Bioorg. Med. Chem. 17, 7324-36, (2009)

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Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. Xiaofan Sui et al Eur. J. Med. Chem. 44, 4455-60, (2009)

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Antimicrobial Activity of Prulifloxacin Tested against a Worldwide Collection of Gastroenteritis-Producing Pathogens, Including Those Causing Traveler's Diarrhea Fritsche, T. R.; Biedenbach, D. J., et al. Antimicrob. Agents Chemother. 53, 1221-1224, (2008)

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Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs. Catherine Clark et al Antimicrob. Agents Chemother. 53, 1353-61, (2009)

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New plasmid-mediated quinolone resistance gene, qnrC, found in a clinical isolate of Proteus mirabilis. Minghua Wang et al Antimicrob. Agents Chemother. 53, 1892-7, (2009)

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Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates. Helio S Sader et al Antimicrob. Agents Chemother. 53, 2171-5, (2009)

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Crystal structure of Bacillus anthracis dihydrofolate reductase with the dihydrophthalazine-based trimethoprim derivative RAB1 provides a structural explanation of potency and selectivity. Christina R Bourne et al Antimicrob. Agents Chemother. 53, 3065-73, (2009)

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Novel ABC transporter gene, vga(C), located on a multiresistance plasmid from a porcine methicillin-resistant Staphylococcus aureus ST398 strain. Kristina Kadlec et al Antimicrob. Agents Chemother. 53, 3589-91, (2009)

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In vitro and in vivo properties of dihydrophthalazine antifolates, a novel family of antibacterial drugs. Patrick Caspers et al Antimicrob. Agents Chemother. 53, 3620-7, (2009)

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In vitro activity of antifolate and polymorphism in dihydrofolate reductase of Plasmodium falciparum isolates from the Kenyan coast: emergence of parasites with Ile-164-Leu mutation Kiara S.M. , et al. Antimicrob. Agents Chemother. 9th ed., 53, 3793-3798, (2009)

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Complete nucleotide sequences of plasmids pEK204, pEK499, and pEK516, encoding CTX-M enzymes in three major Escherichia coli lineages from the United Kingdom, all belonging to the international O25:H4-ST131 clone. Neil Woodford et al Antimicrob. Agents Chemother. 53, 4472-82, (2009)

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In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria. Karen E Bowker et al Antimicrob. Agents Chemother. 53, 4949-52, (2009)

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High prevalence of CTX-M-type beta-lactamases among clinical isolates of Enterobacteriaceae in Bamako, Mali. Véronique Duval et al Antimicrob. Agents Chemother. 53, 4957-8, (2009)

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High prevalence of plasmid-mediated quinolone resistance determinants qnr, aac(6')-Ib-cr, and qepA among ceftiofur-resistant Enterobacteriaceae isolates from companion and food-producing animals. Junying Ma et al Antimicrob. Agents Chemother. 53, 519-24, (2009)

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Role of AbeS, a novel efflux pump of the SMR family of transporters, in resistance to antimicrobial agents in Acinetobacter baumannii. Vijaya Bharathi Srinivasan et al Antimicrob. Agents Chemother. 53, 5312-6, (2009)

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Prevalence of sulfonamide resistance genes in bacterial isolates from manured agricultural soils and pig slurry in the United Kingdom. K G Byrne-Bailey et al Antimicrob. Agents Chemother. 53, 696-702, (2009)

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Identification of a novel trimethoprim resistance gene, dfrK, in a methicillin-resistant Staphylococcus aureus ST398 strain and its physical linkage to the tetracycline resistance gene tet(L). Kristina Kadlec et al Antimicrob. Agents Chemother. 53, 776-8, (2009)

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IncA/C plasmid-mediated florfenicol resistance in the catfish pathogen Edwardsiella ictaluri. Timothy J Welch et al Antimicrob. Agents Chemother. 53, 845-6, (2009)

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Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. Jing Yuan et al Nat. Chem. Biol. 5, 765-71, (2009)

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Chemical genomics in Escherichia coli identifies an inhibitor of bacterial lipoprotein targeting. Ranjana Pathania et al Nat. Chem. Biol. 5, 849-56, (2009)

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Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. Manthena V S Varma et al J. Med. Chem. 53, 1098-108, (2010)

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Single agents with designed combination chemotherapy potential: synthesis and evaluation of substituted pyrimido[4,5-b]indoles as receptor tyrosine kinase and thymidylate synthase inhibitors and as antitumor agents. Aleem Gangjee et al J. Med. Chem. 53, 1563-78, (2010)

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How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability? Alex Avdeef et al J. Med. Chem. 53, 3566-84, (2010)

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Thiazole, oxadiazole, and carboxamide derivatives of artemisinin are highly selective and potent inhibitors of Toxoplasma gondii. Christopher P Hencken et al J. Med. Chem. 53, 3594-601, (2010)

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Targeted mutations of Bacillus anthracis dihydrofolate reductase condense complex structure?activity relationships. Jennifer M Beierlein et al J. Med. Chem. 53, 7327-36, (2010)

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Thousands of chemical starting points for antimalarial lead identification. Francisco-Javier Gamo et al Nature 465, 305-10, (2010)

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Efflux-mediated bis-indole resistance in Staphylococcus aureus reveals differential substrate specificities for MepA and MepR. Timothy J Opperman et al Bioorg. Med. Chem. 18, 2123-30, (2010)

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Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. Francisco J Prado-Prado et al Bioorg. Med. Chem. 18, 2225-31, (2010)

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Design, synthesis, biological evaluation and computational investigation of novel inhibitors of dihydrofolate reductase of opportunistic pathogens. Seema Bag et al Bioorg. Med. Chem. 18, 3187-97, (2010)

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2,4-Diamino-5-methyl-6-substituted arylthio-furo[2,3-d]pyrimidines as novel classical and nonclassical antifolates as potential dual thymidylate synthase and dihydrofolate reductase inhibitors. Aleem Gangjee et al Bioorg. Med. Chem. 18, 953-61, (2010)

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Developing structure-activity relationships for the prediction of hepatotoxicity. Nigel Greene et al Chem. Res. Toxicol. 23, 1215-22, (2010)

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Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. Denis Fourches et al Chem. Res. Toxicol. 23, 171-83, (2010)

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Neural computational prediction of oral drug absorption based on CODES 2D descriptors. A Guerra et al Eur. J. Med. Chem. 45, 930-40, (2010)

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Constitutive SoxS expression in a fluoroquinolone-resistant strain with a truncated SoxR protein and identification of a new member of the marA-soxS-rob regulon, mdtG. Anna Fàbrega et al Antimicrob. Agents Chemother. 54, 1218-25, (2010)

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Transfer of plasmid-mediated CTX-M-9 from Salmonella enterica serotype Virchow to Enterobacteriaceae in human flora-associated rats treated with cefixime. S Faure et al Antimicrob. Agents Chemother. 54, 164-9, (2010)

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KPC-producing extreme drug-resistant Klebsiella pneumoniae isolate from a patient with diabetes mellitus and chronic renal failure on hemodialysis in South Korea. Ji-Young Rhee et al Antimicrob. Agents Chemother. 54, 2278-9, (2010)

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Antimicrobial resistance of Listeria monocytogenes strains isolated from humans in France. A Morvan et al Antimicrob. Agents Chemother. 54, 2728-31, (2010)

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Identification of the novel dfrK-carrying transposon Tn559 in a porcine methicillin-susceptible Staphylococcus aureus ST398 strain. Kristina Kadlec et al Antimicrob. Agents Chemother. 54, 3475-7, (2010)

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Chromosomally encoded blaCMY-2 located on a novel SXT/R391-related integrating conjugative element in a Proteus mirabilis clinical isolate. Sohei Harada et al Antimicrob. Agents Chemother. 54, 3545-50, (2010)

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Inhibition of antibiotic-resistant Staphylococcus aureus by the broad-spectrum dihydrofolate reductase inhibitor RAB1. C R Bourne et al Antimicrob. Agents Chemother. 54, 3825-33, (2010)

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Molecular and biochemical characterization of the natural chromosome-encoded class A beta-lactamase from Pseudomonas luteola. Benoît Doublet et al Antimicrob. Agents Chemother. 54, 45-51, (2010)

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Antimicrobial resistance testing of verocytotoxin-producing Escherichia coli and first description of TEM-52 extended-spectrum ?-lactamase in serogroup O26. Glenn Buvens et al Antimicrob. Agents Chemother. 54, 4907-9, (2010)

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Subinhibitory concentrations of protein synthesis-inhibiting antibiotics promote increased expression of the agr virulence regulator and production of phenol-soluble modulin cytolysins in community-associated methicillin-resistant Staphylococcus aureus. Hwang-Soo Joo et al Antimicrob. Agents Chemother. 54, 4942-4, (2010)

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LmrS is a multidrug efflux pump of the major facilitator superfamily from Staphylococcus aureus. Jody L Floyd et al Antimicrob. Agents Chemother. 54, 5406-12, (2010)

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Transferable quinolone resistance in Vibrio cholerae. Hong Bin Kim et al Antimicrob. Agents Chemother. 54, 799-803, (2010)

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Identification of a plasmid-borne resistance gene cluster comprising the resistance genes erm(T), dfrK, and tet(L) in a porcine methicillin-resistant Staphylococcus aureus ST398 strain. Kristina Kadlec et al Antimicrob. Agents Chemother. 54, 915-8, (2010)

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A predictive ligand-based Bayesian model for human drug-induced liver injury. Sean Ekins et al Drug Metab. Dispos. 38, 2302-8, (2010)

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Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines. Xiaoming Li et al Bioorg. Med. Chem. Lett. 21, 5171-6, (2011)

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Synthesis and antimicrobial activity of N¹-benzyl or N¹-benzyloxy-1,6-dihydro-1,3,5-triazine-2,4-diamines. Xiang Ma et al Bioorg. Med. Chem. Lett. 21, 5428-31, (2011)

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QSAR-based permeability model for drug-like compounds. Rafael Gozalbes et al Bioorg. Med. Chem. 19, 2615-24, (2011)

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Prediction of drug intestinal absorption by new linear and non-linear QSPR. Alan Talevi et al Eur. J. Med. Chem. 46, 218-28, (2011)

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Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. Nandita Sinha et al Eur. J. Med. Chem. 46, 618-30, (2011)

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Novel apramycin resistance gene apmA in bovine and porcine methicillin-resistant Staphylococcus aureus ST398 isolates. Andrea T Fessler et al Antimicrob. Agents Chemother. 55, 373-5, (2011)

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Translating Clinical Findings into Knowledge in Drug Safety Evaluation - Drug Induced Liver Injury Prediction System (DILIps). Zhichao Liu et al PLoS Comput. Biol. 7, e1002310, (2011)

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Merck 14,9709