Vladimir Dobričić
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View article: From Chemistry to Pharmacology: Exploring the Anti-Inflammatory and Antioxidant Potential of Novel Dexketoprofen Amide Derivatives
From Chemistry to Pharmacology: Exploring the Anti-Inflammatory and Antioxidant Potential of Novel Dexketoprofen Amide Derivatives Open
In the present study, five novel dexketoprofen amide derivatives with a free carboxyl group in their side chains were synthesized. The in vivo anti-inflammatory potential of dexketoprofen derivatives was evaluated using a carrageenan-induc…
View article: Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel Coumarin–Triazole–Isatin Hybrids as Selective Butyrylcholinesterase Inhibitors
Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel Coumarin–Triazole–Isatin Hybrids as Selective Butyrylcholinesterase Inhibitors Open
A series of 21 novel coumarin–triazole–isatin hybrids was synthesized and evaluated for their potential as multitarget agents in Alzheimer’s disease (AD). The compounds featured variations in alkyl linker length that connects coumarin and …
View article: Stability and Efficacy of Mucoadhesive Eye Drops Containing Olopatadine HCl: Physicochemical, Functional, and Preclinical In Vivo Assessment
Stability and Efficacy of Mucoadhesive Eye Drops Containing Olopatadine HCl: Physicochemical, Functional, and Preclinical In Vivo Assessment Open
Background: The incorporation of polymers into drug delivery vehicles has been shown to be an effective strategy to prolong the residence time of active ingredients in the precorneal tear film and to increase ocular bioavailability. Object…
View article: N-(9-Acridinyl) Amino Acid Derivatives: Synthesis and In Vitro Evaluation of Anti-Toxoplasma gondii Activity
N-(9-Acridinyl) Amino Acid Derivatives: Synthesis and In Vitro Evaluation of Anti-Toxoplasma gondii Activity Open
Background/Objectives: Acridine, an aromatic heterocyclic compound, serves as a basis for the synthesis of potent bioactive derivatives, displaying a broad spectrum of biological activity, such as antibacterial, antitumor, and antiparasiti…
View article: Intravenous Nanoemulsions Loaded with Phospholipid Complex of a Novel Pyrazoloquinolinone Ligand for Enhanced Brain Delivery
Intravenous Nanoemulsions Loaded with Phospholipid Complex of a Novel Pyrazoloquinolinone Ligand for Enhanced Brain Delivery Open
Background/Objectives: The novel pyrazoloquinolinone ligand CW-02-79 shows a unique profile of selective binding to σ2 receptors, but its poor solubility in both water and lipids makes its research and development a burdensome task. We aim…
View article: In Vitro Evaluation of Pharmacokinetic Properties of Selected Dual COX-2 and 5-LOX Inhibitors
In Vitro Evaluation of Pharmacokinetic Properties of Selected Dual COX-2 and 5-LOX Inhibitors Open
Evaluation of pharmacokinetic properties is a significant step at the early stages of drug development. In this study, an in vitro evaluation of the pharmacokinetic properties of five newly synthesized compounds was performed. These compou…
View article: Unveiling Anticancer Potential of COX-2 and 5-LOX Inhibitors: Cytotoxicity, Radiosensitization Potential and Antimigratory Activity against Colorectal and Pancreatic Carcinoma
Unveiling Anticancer Potential of COX-2 and 5-LOX Inhibitors: Cytotoxicity, Radiosensitization Potential and Antimigratory Activity against Colorectal and Pancreatic Carcinoma Open
Apart from cytotoxicity, inhibitors of the COX-2 enzyme have demonstrated additional effects important for cancer treatment (such as radiosensitization of tumor cells and cell antimigratory effects); however, the relationship between the i…
View article: Selectivity of N(2)-substituted oxotriazinoindole aldose reductase inhibitors is determined by the interaction pattern with Pro301-Arg312 loop of aldehyde reductase
Selectivity of N(2)-substituted oxotriazinoindole aldose reductase inhibitors is determined by the interaction pattern with Pro301-Arg312 loop of aldehyde reductase Open
View article: Synthesis, Characterization, and Investigation of Anti-Inflammatory and Cytotoxic Activities of Novel Thiourea Derivatives of Naproxen
Synthesis, Characterization, and Investigation of Anti-Inflammatory and Cytotoxic Activities of Novel Thiourea Derivatives of Naproxen Open
The objective of this study was to synthesize seven novel thiourea derivatives of naproxen (8–14), examine the anti-inflammatory activity of the newly synthesized compounds, investigate the cytotoxic potential of both sets of synthesized c…
View article: Molecular Docking Analysis of Novel Thiourea Derivatives of Naproxen with Potential Antitumor Activity
Molecular Docking Analysis of Novel Thiourea Derivatives of Naproxen with Potential Antitumor Activity Open
Naproxen, as a propionic acid derivative, causes serious gastrointestinal side effects due to the presence of free carboxylic group. In that sense, masking of carboxylic group with other pharmacophores may be a promising strategy to decrea…
View article: Discovery of Novel Thiophene/Hydrazones: In Vitro and In Silico Studies against Pancreatic Cancer
Discovery of Novel Thiophene/Hydrazones: In Vitro and In Silico Studies against Pancreatic Cancer Open
Cancer is the disease with the highest mortality. Drug studies contribute to promising treatments; however there is an urgent need for selective drug candidates. Pancreatic cancer is difficult to treat and the cancer progresses rapidly. Un…
View article: Synthesis and Investigation of Anti-Inflammatory Activity of New Thiourea Derivatives of Naproxen
Synthesis and Investigation of Anti-Inflammatory Activity of New Thiourea Derivatives of Naproxen Open
The aim of the study was a synthesis and investigation of the dose-dependent anti-inflammatory effect of new thiourea derivatives of naproxen with selected aromatic amines and esters of aromatic amino acids. The results of the in vivo stud…
View article: Synthesis, Evaluation of Enzyme Inhibition and Redox Properties of Potential Dual COX-2 and 5-LOX Inhibitors
Synthesis, Evaluation of Enzyme Inhibition and Redox Properties of Potential Dual COX-2 and 5-LOX Inhibitors Open
Various dual inhibitors of COX-2 and 5-LOX enzymes have been developed so far in order to obtain more effective and safer anti-inflammatory drugs. The aim of this study was to design and synthesize new dual COX-2 and 5-LOX inhibitors, and …
View article: Can Zeolite-Supporting Acridines Boost Their Anticancer Performance?
Can Zeolite-Supporting Acridines Boost Their Anticancer Performance? Open
Acridine and its derivatives (9-chloroacridine and 9-aminoacridine) are investigated here, supported on FAU type zeolite Y, as a delivery system of anticancer agents. FTIR/Raman spectroscopy and electron microscopy revealed successful drug…
View article: High amount of lecithin facilitates oral delivery of a poorly soluble pyrazoloquinolinone ligand formulated in lipid nanoparticles: Physicochemical, structural and pharmacokinetic performances
High amount of lecithin facilitates oral delivery of a poorly soluble pyrazoloquinolinone ligand formulated in lipid nanoparticles: Physicochemical, structural and pharmacokinetic performances Open
View article: The effects of a selected methoxy substituted chalcone in human melanoma cells irradiated with γ-rays
The effects of a selected methoxy substituted chalcone in human melanoma cells irradiated with γ-rays Open
Given the well-established potential of chalcones in modulating the response of cancer cells to therapeutic interventions, coupled with the growing imperative to enhance their biological attributes, the objective of this study was to synth…
View article: Structural Aspects of N(2)-Substitution in Oxotriazinoindole-Based Aldose Reductase Inhibitors with Regard to Inhibition Efficacy and Selectivity
Structural Aspects of N(2)-Substitution in Oxotriazinoindole-Based Aldose Reductase Inhibitors with Regard to Inhibition Efficacy and Selectivity Open
View article: Synthesis and cytotoxic activity of selected dual COX-2 and 5-LOX inhibitors in HeLa and MIA PaCa-2 human cancer cell lines
Synthesis and cytotoxic activity of selected dual COX-2 and 5-LOX inhibitors in HeLa and MIA PaCa-2 human cancer cell lines Open
Among novel cancer chemotherapy approaches, the use of cyclooxygenases (COXs) and lipoxygenases (LOXs) inhibitors represents a promising mean for cancer treatment showing lesser toxicity comparing to the currently used cytotoxic drugs. Thi…
View article: Biocompatible lipid nanocarriers for improved skin delivery of fluocinolone acetonide: Physicochemical and in vitro performances
Biocompatible lipid nanocarriers for improved skin delivery of fluocinolone acetonide: Physicochemical and in vitro performances Open
In order to improve the delivery of topical corticosteroids into inflammatory skin lesions while reducing the likelihood of adverse effects, lipid nanocarriers have received increasing attention. Hence, this study aimed to develop biocompa…
View article: High-performance liquid chromatography evaluation of lipophilicity and QSRR modeling of a series of dual DNA gyrase and topoisomerase IV inhibitors
High-performance liquid chromatography evaluation of lipophilicity and QSRR modeling of a series of dual DNA gyrase and topoisomerase IV inhibitors Open
Bacterial DNA gyrase and topoisomerase IV control the topological state of DNA during replication and represent important antibacterial drug targets. To be successful as drug candidates, newly synthesized compounds must possess optimal lip…
View article: Molecular Docking Analysis of Novel Thiourea Derivatives of Naproxen with Potential Anti-Inflammatory Activity
Molecular Docking Analysis of Novel Thiourea Derivatives of Naproxen with Potential Anti-Inflammatory Activity Open
Administration of current non-steroidal anti-inflammatory drugs is often associated with serious adverse effects. Therefore, there is a constant need to develop new molecules with anti-inflammatory activity. On the other hand, thiourea der…
View article: Influence of spray-drying process on properties of chitosan/xanthan gum polyelectrolyte complexes as carriers for oral delivery of ibuprofen
Influence of spray-drying process on properties of chitosan/xanthan gum polyelectrolyte complexes as carriers for oral delivery of ibuprofen Open
Polyelectrolyte complexes (PECs) are attractive carriers with recognized potential to enhance oral delivery of poorly soluble high-dosed low-molecular-weight drugs. The formulation of solid oral dosage forms requires the drying of PECs, wh…
View article: Design of new telmisartan analogues without AT1 receptor antagonistic activity
Design of new telmisartan analogues without AT1 receptor antagonistic activity Open
Telmisartan is an antihypertensive drug that acts as angiotensin 1 receptor (AT1R) antagonist and a partial peroxisome proliferator activating receptor γ (PPARγ) agonist. Unlike other AT1R antagonists, telmisartan possesses antiproliferati…
View article: Comparative Assessment of In Vitro and In Silico Methods for Aerodynamic Characterization of Powders for Inhalation
Comparative Assessment of In Vitro and In Silico Methods for Aerodynamic Characterization of Powders for Inhalation Open
In vitro assessment of dry powders for inhalation (DPIs) aerodynamic performance is an inevitable test in DPI development. However, contemporary trends in drug development also implicate the use of in silico methods, e.g., computational fl…
View article: Overcoming the Low Oral Bioavailability of Deuterated Pyrazoloquinolinone Ligand DK-I-60-3 by Nanonization: A Knowledge-Based Approach
Overcoming the Low Oral Bioavailability of Deuterated Pyrazoloquinolinone Ligand DK-I-60-3 by Nanonization: A Knowledge-Based Approach Open
Poor water solubility of new chemical entities is considered as one of the main obstacles in drug development, as it usually leads to low bioavailability after administration. To overcome these problems, the selection of the appropriate fo…
View article: Estimation of lipophilicity and design of new 17β-carboxamide glucocorticoids using RP-HPLC and quantitative structure-retention relationships analysis
Estimation of lipophilicity and design of new 17β-carboxamide glucocorticoids using RP-HPLC and quantitative structure-retention relationships analysis Open
Eight 17β-carboxamide glucocorticoids with local anti-inflammatory activity were selected and their retention behavior tested in six RP-HPLC systems (I–VI). logkw , a , and φ 0 parameters were calculated and correlation with previously det…
View article: Biological Evaluation of Oil-in-Water Microemulsions as Carriers of Benzothiophene Analogues for Dermal Applications
Biological Evaluation of Oil-in-Water Microemulsions as Carriers of Benzothiophene Analogues for Dermal Applications Open
During the last decade, many studies have been reported on the design and formulation of novel drug delivery systems proposed for dermal or transdermal administration. The efforts focus on the development of biocompatible nanodispersions t…
View article: Current computer-aided drug design methodologies in discovery of novel drug candidates for neuropsychiatric and inflammatory diseases
Current computer-aided drug design methodologies in discovery of novel drug candidates for neuropsychiatric and inflammatory diseases Open
Drug discovery and development is a very challenging, expensive and time-consuming process. Impressive technological advances in computer sciences and molecular biology have made it possible to use computer-aided drug design (CADD) methods…
View article: Molecular docking analysis of novel thiourea derivatives of naproxen with potential antitumor activity
Molecular docking analysis of novel thiourea derivatives of naproxen with potential antitumor activity Open
In the past few decades, thiourea derivatives have been intensively investigated as potential anticancer drugs. This class of compounds has been recognized as agents with promising inhibitory activity towards human lung adenocarcinoma cell…
View article: Nanocrystal dispersion of DK-I-56–1, a poorly soluble pyrazoloquinolinone positive modulator of α6 GABAA receptors: Formulation approach toward improved in vivo performance
Nanocrystal dispersion of DK-I-56–1, a poorly soluble pyrazoloquinolinone positive modulator of α6 GABAA receptors: Formulation approach toward improved in vivo performance Open