• Home
  • Browse Issues
    • In Press
    • Current Issue
    • Special Issue
    • Past Issues
  • About
    • Editorial Board
    • Bibliographic Listings
    • Peer Review Process
    • Open Access Policy
    • Plagiarism Policy
    • Copyright Policy
    • Retraction Policy
    • Editorial Policy
    • Disclaimer
  • Author Guidelines
  • Submit Article
  • Contact

Subscribe to Updates

Get the latest creative news from FooBar about art, design and business.

Facebook Twitter Instagram
International Journal of Pharmaceutical Investigation
Facebook Twitter Instagram
Submit Article Author Guidelines
  • Home
  • Browse Issues
    1. In Press
    2. Current Issue
    3. Special Issue
    4. Past Issues
    5. View All

    A Study of Nitrosamine Impurities and Regulations Governing their Presence in Drug Products

    September 22, 2023

    Phyto-Pharmacological Importance with Nutritional Potential of Eleusine coracana Linn.: A Review

    September 20, 2023

    Type3c Diabetes Mellitus

    September 20, 2023

    A Study on BioBetters: Various Aspects and Regulatory Approval Process

    September 20, 2023

    A Study of Nitrosamine Impurities and Regulations Governing their Presence in Drug Products

    September 22, 2023

    Phyto-Pharmacological Importance with Nutritional Potential of Eleusine coracana Linn.: A Review

    September 20, 2023

    Type3c Diabetes Mellitus

    September 20, 2023

    A Study on BioBetters: Various Aspects and Regulatory Approval Process

    September 20, 2023

    A Study of Nitrosamine Impurities and Regulations Governing their Presence in Drug Products

    September 22, 2023

    Phyto-Pharmacological Importance with Nutritional Potential of Eleusine coracana Linn.: A Review

    September 20, 2023

    Type3c Diabetes Mellitus

    September 20, 2023

    A Study on BioBetters: Various Aspects and Regulatory Approval Process

    September 20, 2023

    A Study of Nitrosamine Impurities and Regulations Governing their Presence in Drug Products

    September 22, 2023

    Phyto-Pharmacological Importance with Nutritional Potential of Eleusine coracana Linn.: A Review

    September 20, 2023

    Type3c Diabetes Mellitus

    September 20, 2023

    A Study on BioBetters: Various Aspects and Regulatory Approval Process

    September 20, 2023

    A Study of Nitrosamine Impurities and Regulations Governing their Presence in Drug Products

    September 22, 2023

    Phyto-Pharmacological Importance with Nutritional Potential of Eleusine coracana Linn.: A Review

    September 20, 2023

    Type3c Diabetes Mellitus

    September 20, 2023

    A Study on BioBetters: Various Aspects and Regulatory Approval Process

    September 20, 2023
  • About
    • Editorial Board
    • Bibliographic Listings
    • Peer Review Process
    • Open Access Policy
    • Plagiarism Policy
    • Copyright Policy
    • Retraction Policy
    • Editorial Policy
    • Disclaimer
  • Author Guidelines
  • Submit Article
  • Contact
International Journal of Pharmaceutical Investigation
Home»JPHI»Vol 11 Issue 1»4-Aminoantipyrine Analogs as Anti-inflammatory and Antioxidant agents: Synthesis, Biological Evaluation and Molecular Docking Studies
Vol 11 Issue 1

4-Aminoantipyrine Analogs as Anti-inflammatory and Antioxidant agents: Synthesis, Biological Evaluation and Molecular Docking Studies

April 1, 2021Updated:June 3, 20232 Mins Read
Share
Facebook Twitter LinkedIn Pinterest WhatsApp Email

International Journal of Pharmaceutical Investigation, 2021, 11, 1, 14-22.
DOI: 10.5530/ijpi.2021.1.4
Published: April 2021
Type: Original Article

Authors: 

Qazi Yasar
Department of Pharmaceutical Chemistry, Y. B. Chavan College of Pharmacy, Rauza Bagh, Aurangabad, Maharashtra, INDIA.

Zahid Zaheer
Department of Pharmaceutical Chemistry, Y. B. Chavan College of Pharmacy, Rauza Bagh, Aurangabad, Maharashtra, INDIA.

ABSTRACT

Objectives: A novel series of 4-aminoantipyrine derivatives were designed and efficiently synthesized from Gewald, triphosgene and various substituted aromatic/ aliphatic/heterocyclic amines. Methods: The synthesized derivatives were characterized by IR, NMR, Mass and elemental analysis. The synthesized derivatives were evaluated for their anti-inflammatory activity using in vitro protein denaturation assay and antioxidant activity by using the 1,1-diphenyl-1-picrylhydrazyl free radical scavenging method. To establish the selectivity and safety profile of the drug, the most active compounds 4a and 4b were further screened for cytotoxicity against HeLa and MCF-7 cell lines using the sulforhodamine-B assay. The synthesized compounds were also analyzed for ADME properties and a docking study was done into the active site of oxidoreductase, cyclooxygenase-1 and cyclooxygenase-2 enzymes in an attempt to understand their binding mode using Auto Dock Vina. Results: Among the series Compounds 4a and 4b showed potent anti-inflammatory activity and antioxidant activity as compared with standard diclofenac and Ascorbic acid respectively. The results of in silico ADME Screening showed that compounds could be exploited as an oral drug candidate. The most prominent compound 4a and 4b showed no significant cytotoxic activity against HeLa and MCF-7 cell lines. The molecular docking study of most active compounds had shown good binding interactions against oxidoreductase, cyclooxygenase-1 and cyclooxygenase-2 enzymes. Conclusion: Results of in vitro anti-inflammatory, antioxidant activities and docking study showed that synthesized compounds had potential antiinflammatory and antioxidant activities and can be further optimized and developed as a lead compound.

Keywords: 2-Aminothiophenes, Auto Dock, Cyclooxygenase-1 and Cyclooxygenase-2, Sulforhodamine-B assay.

Original Article
Previous ArticleEffects of Operational Parameters on the Removal of Tetracycline from Aqueous Solutions by Electrocoagulation
Next Article Application of Green Silver Nanoparticles Synthesized using Leaf Extract of Tridax procumbens for Preparation of Clinical Antimicrobial Bandages

Related Posts

Impact of Mobile Radiations on Gliclazide Tablet Formulation

July 21, 2023

Formulation and in vitro Evaluation of pH Dependent Colon Targeted Controlled Release Tablet of Mesalamine Containing Cyamopsis tetragonoloba Gum and Sodium Alginate

July 21, 2023

Formulation, Development and Characterization of Liposome-based Gel of Eberconazole Nitrate for Topical Delivery

July 21, 2023
Download PDF
Cite this Article
Citation Output

Read in Readcube
  • Download PDF
  • ReadCube
Citations & Metrics
Article Metrics
  • Dimensions Metrics
  • Page Views
  • Related
Total Views 0
Last Month Views 0
Click for PLUM.MX Metrics Search this article in Google Scholar Related Articles in Google Scholar Search related in PUBMED


About
About

publishing peer-reviewed scholarly reviews, themed issues and research articles within the entire scope of the Pharmaceutical field. The journal particularly aims to foster the dissemination of scientific information by publishing manuscripts related to Pharmacy and Related Fields.

We're accepting new submissions right now.

Facebook Twitter RSS
Editor Picks

Overview on Evolving Variants of Novel Coronavirus and Control Measures in India

July 5, 2023

An Overview of the Various Appropriate Types of Cell Lines for the Production of Monoclonal Antibodies

July 5, 2023

Ashwagandha: A Flagship Herb of Ayurveda from Past to Present Nano Era

July 5, 2023

Dental Pulp Stem Cells: Biology and Promise for Regenerative Medicine

July 5, 2023
STAY CONNECTED

Contact Editor-In-Chief
Editor, International Journal of Pharm Investigation
#9, Vinnse Tower, Wheeler Road Extn.
St. Thomas Town, 560084, Bangalore, INDIA
Email: editor@jpionline.org

© 2023 Phcog.Net | Published by : EManuscript.
  • Home
  • Submit Article
  • Disclaimer
  • Contact

Type above and press Enter to search. Press Esc to cancel.