Pharmacokinetic properties
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In silico screening of alkaloids as potential inhibitors of HER2 protein for breast cancer treatment
his study focused on finding alkaloid compounds collected from Chemfaces database that inhibit HER2 enzyme employing computational methods such as molecular docking and ADMET prediction. Out of 118 phytochemicals docked to the ATP binding site of the HER2 kinase domain, 10 alkaloid compounds exhibited higher binding affinity than the reference inhibitor and satisfied the Lipinski’s rule of five. All compounds have good pharmacokinetic properties.
10p dianmotminh02 03-05-2024 4 3 Download
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Ebook "Reducing drug attrition (Topics in Medicinal chemistry, Volume 11)" is to provide guidance to those persons who are dedicated to the creation and development of new drugs to aid patients. Our aim was to address the key factors that have led to failure of preclinical and clinical drug candidates. Despite the significant scientific advances over the past few decades in the disciplines associated with research and development (R&D), the overall productivity, as measured by new approved drugs, has not improved.
176p tudohanhtau1006 29-03-2024 1 1 Download
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We describe a case of symptomatic bradycardia resulting from ivabradine toxicity by measurement of ivabradine levels, of which there are limited reports in the literature. Measurement of serum ivabradine levels and knowledge of the pharmacokinetic properties of the drug can be utilized to confirm the diagnosis of ivabradine toxicity.
5p vigamora 23-05-2023 5 2 Download
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A series of chiral thioureas (1 - 17) were synthesized from and tested for their anticholinesterase, tyrosinase, and urease enzyme inhibitor activities. Various phenylisothiocyanates were added to solution of ˪-cysteine in methanol: water (1 : 1 v / v) at room temperature and stirred for 24 h. The precipitated solid was recrystallized from n-butanol. Pure compounds were characterized by NMR (1 H and 13C), FTIR, and CHNS.
24p lyhuyenthu 31-01-2023 3 2 Download
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5-fluorocytosine is a pyrimidine and a fluorinated cytosine analog mainly used as an antifungal agent. It is a precursor of 5-fluorouracil, which possesses anticancer properties. To reduce systemic toxicity of 5-fluorouracil during chemotherapy, 5- fluorocytosine can be used as a targeted anticancer agent.
10p vidarwin 23-02-2022 15 1 Download
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With the increasing occurrence of drug shortages, understanding the pharmacokinetics of alternative intrathecal opioid administration has gained importance. In particular, additional data are needed to comprehensively evaluate the analgesic properties of intrathecal hydromorphone in the laboring patient.
4p vampires36 30-12-2021 14 0 Download
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In the present work, a library of fifteen 2-hydroxy benzothiazole-linked 1,3,4 -oxadiazole derivatives have been synthesized and confirmed using different analytical techniques. All of the synthesized compounds have been tested for antibacterial and in silico pharmacokinetic studies for the first time. From the ADME predictions, compound 4 showed the highest in silico absorption percentage (86.77%), while most of the compounds showed more than 70% absorption.
22p tudichquannguyet 29-11-2021 5 1 Download
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Polyethylene glycol (PEG) is a polymer that is widely used as a carrier for drug delivery systems (DDS). A library of N-PEGylated quinoline derivatives of PEG molecular weight 200 was prepared rapidly after the activation of PEGs using maleic anhydride. Quinoline with a polymer backbone is essential as new material. PEG is a water-soluble nonionic polymer approved by food and drug organizations for medicine applications. Because of its nontoxic grapheme, it is widely utilized in numerous biochemical, cosmetic, pharmaceutical, and industrialized applications.
20p tudichquannguyet 29-11-2021 12 1 Download
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Synthesis and structural determination of some 4-aminoquinazoline derivatives containing prop-2-yn-1-yloxy substituents at C-6 position; research and synthesize and determine the hybrid compound structure containing Quinazoline frame; research on carcinogenic activity and inhibition of acetylcholinesterase enzyme of synthetic compounds; studying protein docking and predicting the pharmacokinetic properties of some compounds that inhibit the enzyme acetylcholinesterase.
26p capheviahe27 23-02-2021 34 3 Download
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NipahVirus (NiV) is a zoonotic Virus which infects several animals and humans worldwide. Currently, there is no specific drug or vaccine to treat or control NiV infections. The present study is aimed to identify novel inhibitors of NiV from Indian medicinal plants. Glycoprotein was taken as target protein. Around 600 phytocompounds were taken from 10 Indian medicinal plants and subjected to Virtual Screening by using Libdock module from Discovery Studio 4.0. From these, the best 20 compounds were screened and evaluated for their Pharmacokinetic properties by using ADMETSAR and pKCSM tools.
14p trinhthamhodang9 16-12-2020 9 2 Download
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Paracetamol/Orphenadrine is a fixed dose combination containing 35 mg orphenadrine and 450 mg paracetamol. It has analgesic and muscle relaxant properties and is widely available as generics.
13p vivientiane2711 30-06-2020 16 1 Download
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Rivaroxaban is a direct inhibitor of coagulation factor Xa and is used for venous thromboembolic disorders. The rivaroxaban interaction with BSA was studied to understand its PK and PD (pharmacokinetics and pharmacokinetics) properties.
9p vijiraiya2711 27-05-2020 14 1 Download
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Capsaicin has multiple pharmacological activities including antioxidant, anticancer, and antiinflammatory activities. However, its clinical application is limited due to its poor aqueous solubility, gastric irritation, and low oral bioavailability. This research was aimed at preparing sustained-release matrix pellets of capsaicin to enhance its oral bioavailability.
11p caothientrangnguyen 09-05-2020 7 0 Download
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Instantly dissolving buccal films have gained attention owing to their easy administration and capability to surmount the hepatic first pass effect of drugs. Dapoxetine hydrochloride (DPX) has a low oral bioavailability due to significant hepatic first pass metabolism. In addition, DPX is a weakly basic drug with a pH dependent solubility that could limit its dissolution in the body neutral fluids.
10p partimesinhvien 08-05-2020 15 1 Download
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Advances in antibody engineering provide strategies to construct recombinant antibody-like molecules with modified pharmacokinetic properties. Multermerization is one strategy that has been used to produce antibody-like molecules with two or more antigen binding sites.
8p vihamax2711 21-04-2020 13 1 Download
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Several countries have used pegylation technology to improve the pharmacokinetic properties of essential drugs. Recently, a novel interferon alfa-2b protein conjugated to four-branched 12 kDa polyethylene glycol molecules was developed jointly between Cuba and Brazil.
8p vimax2711 30-03-2020 8 2 Download
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Deflazacort is a synthetic corticosteroid characterized by a favourable pharmacokinetic profile, peculiar pharmacodynamic properties and a good safety profile.
8p vienzym2711 30-03-2020 15 2 Download
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Very few therapeutic options are available from the time of emergence of MRSA. Macrolide lincosamide streptogramin B (MSLB) antibiotics can be used in such scenarios with clindamycin being the preferred agent due to its excellent pharmacokinetic properties. Staphylococcal resistance to clindamycin may be inducible (iMLSB - inducible MacrolideLincosamide Streptogramin B resistance) or constitutive. The treatment of patients harbouring iMLSB Staphylococci with clindamycin leads to the development of constitutive resistance, subsequently leading to therapeutic failure.
8p kequaidan2 13-12-2019 32 0 Download
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Recently, carbon dots (CDs) have attracted great attention due to their superior properties, such as biocompatibility, fluorescence, high quantum yield, and uniform distribution. These characteristics make CDs interesting for bioimaging, therapeutic delivery, optogenetics, and theranostics. Photoluminescence (PL) properties enable CDs to act as imaging-trackable gene nanocarriers, while cationic CDs with high transfection efficiency have been applied for plasmid DNA and siRNA delivery.
13p caygaocaolon1 13-11-2019 7 0 Download
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Understanding the basics of pharmacology is an essential nursing responsibility. Pharmacology is the science that deals with the physical and chemical properties, and biochemical and physiologic effects, of drugs. It includes the areas of pharmacokinetics, pharmacodynamics, pharmacotherapeutics, pharmacognosy, and toxicodynamics.
1266p hocmaytinh2011 02-10-2011 151 40 Download