AIMC Topic: Dose-Response Relationship, Drug

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Machine learning prioritizes synthesis of primaquine ureidoamides with high antimalarial activity and attenuated cytotoxicity.

European journal of medicinal chemistry Jan 31, 2018
Primaquine (PQ) is a commonly used drug that can prevent the transmission of Plasmodium falciparum malaria, however toxicity limits its use. We prepared five groups of PQ derivatives: amides 1a-k, ureas 2a-k, semicarbazides 3a,b, acylsemicarbazides 4...
Molecular Structure Antimalarials Malaria, Falciparum Erythrocytes Primaquine Animals Cell Line Antineoplastic Agents Amides Rats Humans Drug Screening Assays, Antitumor Cell Proliferation Structure-Activity Relationship Dose-Response Relationship, Drug Machine Learning Plasmodium falciparum
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Prediction of opioid dose in cancer pain patients using genetic profiling: not yet an option with support vector machine learning.

BMC research notes Jan 27, 2018
OBJECTIVE: Use of opioids for pain management has increased over the past decade; however, inadequate analgesic response is common. Genetic variability may be related to opioid efficacy, but due to the many possible combinations and variables, statis...
Humans Female Aged Male Middle Aged Morphine Receptors, Opioid, mu Polymorphism, Single Nucleotide Gene Frequency Catechol O-Methyltransferase Cancer Pain Receptors, Opioid, delta Genotype Support Vector Machine Dose-Response Relationship, Drug Analgesics, Opioid
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Changes in systemic vascular endothelial growth factor levels after intravitreal injection of aflibercept in infants with retinopathy of prematurity.

Graefe's archive for clinical and experimental ophthalmology = Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie Dec 30, 2017
BACKGROUND: To investigate the levels of VEGF in the systemic circulation of patients with type 1 ROP who received intravitreal injections of 1 mg (0.025 mL) aflibercept (IVA) or 0.625 mg (0.025 mL) bevacizumab (IVB).
Retinopathy of Prematurity Dose-Response Relationship, Drug Vascular Endothelial Growth Factors Intravitreal Injections Biomarkers Recombinant Fusion Proteins Humans Prognosis Receptors, Vascular Endothelial Growth Factor Prospective Studies Female Time Factors Infant, Newborn Enzyme-Linked Immunosorbent Assay Male Angiogenesis Inhibitors Treatment Outcome Follow-Up Studies
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New 1,5 and 2,5-disubstituted tetrazoles-dependent activity towards surface barrier of Candida albicans.

European journal of medicinal chemistry Dec 30, 2017
A series of novel tetrazole derivatives was synthetized using N-alkylation or Michael-type addition reactions, and screened for their fungistatic potential against Candida albicans (the lack of endpoint = 100%). Among them, the selected compounds 2d,...
Antifungal Agents Molecular Structure Tetrazoles Candida albicans Dose-Response Relationship, Drug Cell Survival Humans Caco-2 Cells Microbial Sensitivity Tests Structure-Activity Relationship
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Amino acid conjugated antimicrobial drugs: Synthesis, lipophilicity- activity relationship, antibacterial and urease inhibition activity.

European journal of medicinal chemistry Dec 29, 2017
Present work describes the in vitro antibacterial evaluation of some new amino acid conjugated antimicrobial drugs. Structural modification was attempted on the three existing antimicrobial pharmaceuticals namely trimethoprim, metronidazole, isoniazi...
Dose-Response Relationship, Drug Structure-Activity Relationship Molecular Structure Amino Acids Urease Bacillus Metronidazole Anti-Bacterial Agents Isoniazid Microbial Sensitivity Tests Pseudomonas aeruginosa Trimethoprim Escherichia coli Salmonella typhi Staphylococcus aureus Hydrophobic and Hydrophilic Interactions Enzyme Inhibitors
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Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis.

European journal of medicinal chemistry Dec 28, 2017
Bruton's tyrosine kinase (Btk) is a Tec family kinase with a well-defined role in the B cell receptor (BCR) and Fcγ receptor (FcR) signaling pathways, which makes it a uniquely attractive target for the treatment of autoimmune diseases, such as rheum...
Pyrroles Protein-Tyrosine Kinases Structure-Activity Relationship Rats Models, Molecular Microsomes, Liver Humans Molecular Structure Cell Proliferation Protein Kinase Inhibitors Animals Dogs Rats, Sprague-Dawley Drug Design Pyrimidines Dose-Response Relationship, Drug Mice Agammaglobulinaemia Tyrosine Kinase Cell Line Arthritis, Rheumatoid Haplorhini
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The effect of fasting status on lipids, lipoproteins, and inflammatory biomarkers assessed after hospitalization for an acute coronary syndrome: Insights from PROVE IT-TIMI 22.

Clinical cardiology Dec 28, 2017
BACKGROUND: For decades, fasting for 8 to 12 hours has been recommended for measurement of lipid profiles. The effect of fasting on low-density lipoprotein cholesterol (LDL-C) and triglycerides (TG) has been described in healthy cohorts and those wit...
Lipoproteins Acute Coronary Syndrome Atorvastatin Pravastatin Immunoturbidimetry Female Hospitalization Male Middle Aged Fasting Colorimetry Inflammation Follow-Up Studies Humans Dose-Response Relationship, Drug Biomarkers Lipids Prognosis Retrospective Studies
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Investigation of genotoxic effects of paraben in cultured human lymphocytes.

Drug and chemical toxicology Dec 27, 2017
Paraben is a phenolic derivative of benzoic acid extensively used as preservatives in food, pharmaceutical, and cosmetic industries due to its antimicrobial characteristics. The objective of this study was to evaluate the in vitro genotoxic effects o...
Cells, Cultured Dose-Response Relationship, Drug DNA Damage Lymphocytes Healthy Volunteers Humans Micronuclei, Chromosome-Defective Mitotic Index Sister Chromatid Exchange Parabens Comet Assay Mutagens Micronucleus Tests Chromosome Aberrations
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Chemical findings and in vitro biological studies to uphold the use of Ficus exasperata Vahl leaf and stem bark.

Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association Dec 27, 2017
Ficus exasperata Vahl, commonly known as sandpaper, is a terrestrial Afro-tropical tree used in popular medicine. Despite the existence of some works on the biological activities of this species, its chemical composition is still poorly known. The ai...
Cell Line, Tumor Plant Extracts Nitric Oxide Hypoglycemic Agents Dose-Response Relationship, Drug Dietary Supplements Plant Leaves Drug Screening Assays, Antitumor Plant Bark Chromatography, High Pressure Liquid Humans Reproducibility of Results Ficus Spectrometry, Mass, Electrospray Ionization Spectrophotometry, Ultraviolet Plant Stems Functional Food Inhibitory Concentration 50 Free Radical Scavengers Superoxides
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Peanut testa extracts possessing histone deacetylase inhibitory activity induce apoptosis in cholangiocarcinoma cells.

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie Dec 27, 2017
Previous studies demonstrated that peanut testa extracts (KK4 and ICG15042) containing natural histone deacetylase (HDAC) inhibitors inhibited the growth of several human cancer cell lines via apoptosis induction. The aims of this study were to inves...
Humans Cell Line, Tumor Plant Extracts Apoptosis Dose-Response Relationship, Drug Cell Survival Arachis Cholangiocarcinoma Histone Deacetylase Inhibitors
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