Design and synthesis of neoteric benzylidene amino-benzimidazole scaffolds for antioxidant and anti-inflammatory activity

Article Chemistry, Physical

Transition metal complexes of imidazole derived Schiff bases: Antioxidant/anti-inflammatory/antimicrobial/enzyme inhibition and cytotoxicity properties

G. Anjali Krishna et al.

Summary: A flexible class of Ni(II) and Zn(II) complexes were synthesized with a novel Schiff base ligand containing an imidazole moiety. The compounds were characterized structurally and tested for their biochemical properties.

JOURNAL OF MOLECULAR STRUCTURE (2023)

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Article Chemistry, Medicinal

Novel Benzo[4,5]imidazo[1,2-a]pyrimidine derivatives as selective Cyclooxygenase-2 Inhibitors: Design, synthesis, docking studies, and biological evaluation

Maryam Bayanati et al.

Summary: The present study aimed to synthesize and evaluate a new series of benzo[4,5]imidazo[1,2-a]pyrimidine compounds as COX-2 inhibitors. Molecular modeling studies demonstrated that the methylsulfonyl group as a pharmacophore was well-placed into the COX-2 active site. In vitro and in vivo tests showed that the synthesized compounds exhibited significant COX-2 inhibitory effects and dose-dependent anti-nociceptive activity.

MEDICINAL CHEMISTRY RESEARCH (2023)

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Review Cardiac & Cardiovascular Systems

Inflammation Resolution: Implications for Atherosclerosis

Amanda C. Doran

Summary: This article discusses the major failures of resolution in atherosclerosis and explores new potential regulators that are of translational significance.

CIRCULATION RESEARCH (2022)

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Article Biochemistry & Molecular Biology

Drug Design, Synthesis and Biological Evaluation of Heterocyclic Molecules as Anti-Inflammatory Agents

Jignasa Savjani et al.

Summary: This study developed a novel series of indomethacin analogues with potential anti-inflammatory properties and fewer side effects. Through various scientific approaches, the binding interactions between these analogues and COX-2 protein were evaluated, and the top-scoring complex was selected. In vitro and in vivo evaluations demonstrated that certain compounds exhibited strong COX-2 inhibition and anti-inflammatory potential without ulcerogenic liability.

MOLECULES (2022)

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Article Infectious Diseases

A Review on the Antimicrobial Activity of Schiff Bases: Data Collection and Recent Studies

Jessica Ceramella et al.

Summary: Schiff bases have a wide range of applications in various fields and their conjugation with chitosan can enhance chitosan's antibacterial activity. The use of Schiff base nanoparticles can also improve their antimicrobial effects.

ANTIBIOTICS-BASEL (2022)

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Review Pharmacology & Pharmacy

Anti-Inflammatory Activities of Betulinic Acid: A Review

Jose Fernando Oliveira-Costa et al.

Summary: Inflammatory diseases have a high prevalence and pose a significant burden on the healthcare system worldwide. Betulinic acid and its derivatives show potential as lead compounds for the development of new anti-inflammatory treatments.

FRONTIERS IN PHARMACOLOGY (2022)

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Article Chemistry, Multidisciplinary

Design, Synthesis, and Molecular Modeling Studies of a Novel Benzimidazole as an Aromatase Inhibitor

Ulviye Acar Cevik et al.

Summary: In this study, a series of novel 1,3,4-oxadiazole-benzimidazole derivatives were designed and synthesized. Their cytotoxic activities against five cancer cell lines were evaluated, and compounds 5b,c showed satisfactory potencies and higher anticancer activity compared to the reference drug doxorubicin. Enzymatic inhibition assays of aromatase enzymes were performed, and molecular docking and dynamics simulations were used to understand the structure-activity connections and mechanism of action of the aromatase inhibitors.

ACS OMEGA (2022)

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Article Chemistry, Medicinal

Synthesis and Anti-Inflammatory Activity Evaluation of Some Benzimidazole Derivatives

Alok Kumar Moharana et al.

Summary: This study synthesized three new small molecule compounds with anti-inflammatory properties and demonstrated their non-toxicity through in vitro and in vivo experiments. Two of the compounds were found to have significant anti-inflammatory properties and in silico analysis suggested their potential as orally administered drugs.

PHARMACEUTICAL CHEMISTRY JOURNAL (2022)

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Article Pharmacology & Pharmacy

Anti-inflammatory, anti-oxidant and cardio-protective properties of novel fluorophenyl benzimidazole in L-NAME-induced hypertensive rats

Hina Iqbal et al.

EUROPEAN JOURNAL OF PHARMACOLOGY (2022)

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Article Biochemistry & Molecular Biology

Inhibition of Tumor Growth and Modulation of Antioxidant Activity of Rhodoxanthin Isolated from Taxus baccata Aril against B16F10 Murine Malignant Melanoma

Daria-Antonia Dumitras et al.

Summary: The study found that rhodoxanthin has anti-tumor and antioxidant effects on murine melanoma, significantly reducing tumor growth and weight, as well as lowering epidermal growth factor activity and DNA oxidation.

ANTIOXIDANTS (2022)

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Article Chemistry, Medicinal

Design, Synthesis, and Anti-Inflammatory Activity of Some Coumarin Schiff Base Derivatives: In silico and in vitro Study

Shokhan J. Hamid et al.

Summary: This study aimed to design and synthesize a compound with anti-inflammatory activity while avoiding the side effects of NSAIDs. Through computational and experimental results, compound 7 was found to be a potential lead molecule with strong anti-inflammatory activity and correlation with protein denaturation.

DRUG DESIGN DEVELOPMENT AND THERAPY (2022)

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Article Infectious Diseases

New Pyrazolo-Benzimidazole Mannich Bases with Antimicrobial and Antibiofilm Activities

Christina Zalaru et al.

Summary: A new series of pyrazolo-benzimidazole hybrid Mannich bases were synthesized and characterized. In vitro cytotoxicity tests showed that the compounds were noncytotoxic at a certain concentration and exhibited high biocompatibility. The newly synthesized compounds demonstrated good antibacterial and antibiofilm activity against several bacterial strains.

ANTIBIOTICS-BASEL (2022)

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Article Multidisciplinary Sciences

Synthesis, spectral studies, antioxidant and antibacterial evaluation of aromatic nitro and halogenated tetradentate Schiff bases

Bhagwat Vhanale et al.

Summary: In this study, we synthesized and characterized eleven novel Schiff bases and evaluated their biological properties. The spectral data (FT-IR, H-1 NMR, C-13 NMR, and LC-MS) confirmed the structures of the synthesized compounds. The antibacterial activity against various strains and antioxidant activity were also investigated. The results showed that the substituted compounds exhibited good antibacterial activity and higher antioxidant activity.

HELIYON (2022)

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Article Oncology

A novel inflammatory response-related signature predicts the prognosis of cutaneous melanoma and the effect of antitumor drugs

Jiahua Xing et al.

Summary: This study is the first to use inflammatory response-related genes to build a predictive model for cutaneous melanoma (CM). The study found that a 5-gene model consisting of inflammatory response-related genes can be used to forecast the prognosis and immunological state of CM, providing personalized and precision medicine a new goal and direction.

WORLD JOURNAL OF SURGICAL ONCOLOGY (2022)

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Article Multidisciplinary Sciences

New Schiff base ligand and its novel Cr(III), Mn(II), Co(II), Ni(II), Cu(II), Zn(II) complexes: spectral investigation, biological applications, and semiconducting properties

Mosad A. El-ghamry et al.

Summary: A new Schiff base ligand derived from antiviral valacyclovir and its metal complexes (Cr(III), Mn(II), Co(II), Ni(II), Cu(II), Zn(II)) were synthesized. The type of bonding between the ligand and metal ions was clarified and the complexes showed high thermal stability and antimicrobial and antitumor activity.

SCIENTIFIC REPORTS (2022)

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Article Biochemistry & Molecular Biology

Synthesis, design, and assessment of novel morpholine-derived Mannich bases as multifunctional agents for the potential enzyme inhibitory properties including docking study

Songul Boy et al.

Summary: Novel N-Mannich bases were synthesized through the Mannich reaction, followed by the synthesis of eight new compounds. These compounds exhibited inhibitory activity against AChE, BChE, and GST enzymes, with the most active inhibitors showing interactions through hydrophobic and hydrogen bonding with the enzymes.

BIOORGANIC CHEMISTRY (2021)

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Article Chemistry, Medicinal

HeroMDAnalysis: an automagical tool for GROMACS-based molecular dynamics simulation analysis

Ravi Rawat et al.

Summary: The article introduces an automated tool called HeroMDAnalysis for analyzing GROMACS-based MDS trajectories and generating high-quality images. The tool is simple, semi-automated, and relatively fast, providing a useful method for biochemists and synthetic chemists without command line interface experience.

FUTURE MEDICINAL CHEMISTRY (2021)

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Article Biochemistry & Molecular Biology

Anti-atherogenic effect of Nepitrin-7-O-glucoside: A flavonoid isolated from Nepeta hindostana via acting on PPAR - alpha receptor

Sushma Devi et al.

Summary: The study focused on the use of Nepitrin-7-O-glucoside from the medicinal plant Nepeta hindostana to investigate its beneficial effects on high-fat diet induced atherosclerosis. It was found that Nepitrin significantly improved dyslipidemia by acting on the PPAR-alpha receptor, as confirmed by molecular dynamics studies. The results of the preclinical and molecular dynamics studies were correlated, indicating that Nepitrin acts as a potent antiatherogenic agent by reducing lipid levels and regenerating damaged cells.

STEROIDS (2021)

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Article Chemistry, Multidisciplinary

Synthesis, characterization, and anticancer activity of some metal complexes with a new Schiff base ligand

Thamer A. Alorini et al.

Arabian Journal of Chemistry (2021)

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Article Biochemistry & Molecular Biology

Pyrazoles and Pyrazolines as Anti-Inflammatory Agents

Martha Mantzanidou et al.

Summary: The five-membered heterocyclic group of pyrazoles/pyrazolines plays an important role in drug discovery, presenting a wide range of biological activities. The synthesis and in vitro studies of these derivatives reveal their antioxidant, anti-inflammatory, and lipoxygenase inhibitory activities, with pyrazoline derivatives showing a higher potency than pyrazoles.

MOLECULES (2021)

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Review Neurosciences