Design, synthesis, biological evaluation, and computational studies of novel thiazolo-pyrazole hybrids as promising selective COX-2 inhibitors: Implementation of apoptotic genes expression for ulcerogenic liability assessment.

doi:10.1016/J.BIOORG.2021.104883

Journal ArticleDOI

Design, synthesis, biological evaluation, and computational studies of novel thiazolo-pyrazole hybrids as promising selective COX-2 inhibitors: Implementation of apoptotic genes expression for ulcerogenic liability assessment.

Adel A. Marzouk, +6 more

- 31 Mar 2021 -

Bioorganic Chemistry

- Vol. 111, pp 104883-104883

TLDR

In this article, a series of thiazolo-pyrazole hybrids has been prepared and assessed for their in vitro COX-1/COX-2 inhibitory activity.

About:

This article is published in Bioorganic Chemistry.The article was published on 2021-03-31. It has received 9 citations till now.

Citations

PDF

Open Access

More filters

Journal ArticleDOI

Synthesis, Characterization and Molecular Docking of Novel Lonazolac Analogues 3-(3-Hydroxy-5-methyl-1H-pyrazol-4-yl)-3-arylpropanoic Acid Derivatives: Highly Potential COX-1/COX-2, Matrix Metalloproteinase and Protein Denaturation Inhibitors

Varsha K. Pawar, +4 more

- 01 Mar 2022 -

Journal of Molecular Structure

TL;DR: In this paper , the anti-inflammatory activity of two new series of lonazolac analogue: 2a-p and 2n and 2g was evaluated against standard celecoxib and aspirin, the results obtained are much better than the standard.

...read moreread less

Journal ArticleDOI

Design, Synthesis, Biological Evaluation, and Computational Studies of Novel Fluorinated Candidates as PI3K Inhibitors: Targeting Fluorophilic Binding Sites.

Ahmed H. Tantawy, +6 more

- 18 Nov 2021 -

Journal of Medicinal Chemistry

TL;DR: In this paper, high-fluorinated candidates containing anticancer pharmacophores like thiosemicarbazone (5a-e) and its cyclic analogues hydrazineylinositol 3kinase (PI3K) enzyme inhibition were synthesized, and their cytotoxic activity was assayed against 60 tumor cell lines.

...read moreread less

Journal ArticleDOI

Novel 5,6-diphenyl-1,2,4-triazine-3-thiol derivatives as dual COX-2/5-LOX inhibitors devoid of cardiotoxicity.

Poorvi Saraf, +7 more

- 01 Sep 2022 -

Bioorganic Chemistry

TL;DR: In this paper , a series of 5,6-diphenyl-1,2,4-triazine-3-thiol derivatives were designed, synthesized, and screened for their inhibitory potential against COX-2 and 5-LOX enzymes.

...read moreread less

Journal ArticleDOI

Catalyst and base free aza-Michael addition reaction: Synthesis of poly-substituted 4-pyrazole based benzopyrans

Tapaswini Pradhan Ashok Kumar Das, +3 more

- 01 Mar 2022 -

Tetrahedron Letters

TL;DR: In this paper , an efficient and catalyst free protocol has been disclosed for aza-Michael addition reaction of pyrazoles with 2-aryl-3-nitro-2H-chromene derivatives.

...read moreread less

Journal ArticleDOI

Novel Thiadiazol Derivatives; Design, Synthesis, Biological Activity, Molecular Docking and Molecular Dynamics

Derya Osmaniye, +4 more

- 01 Sep 2022 -

Journal of Molecular Structure

TL;DR: In this article , 16 thiadiazole derivatives (3a-3p) were designed, synthesized and biologically evaluated for their COX-1 and COX2 inhibitory potential using the in vitro fluorometric method.

...read moreread less

References

PDF

Open Access

More filters

Book

Theory and Practice of Histological Techniques

John D. Bancroft, +1 more

TL;DR: Light Microscopy, Enzyme Histochemistry, and Immunocytochemical Techniques: Diagnostic Cytopathology, Specimen Collection and Preparation.

...read moreread less

Journal ArticleDOI

SwissADME: A free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules

Antoine Daina, +4 more

- 03 Mar 2017 -

Scientific Reports

TL;DR: The new SwissADME web tool is presented that gives free access to a pool of fast yet robust predictive models for physicochemical properties, pharmacokinetics, drug-likeness and medicinal chemistry friendliness, among which in-house proficient methods such as the BOILED-Egg, iLOGP and Bioavailability Radar are presented.

...read moreread less

Journal ArticleDOI

Gastrointestinal toxicity of nonsteroidal antiinflammatory drugs.

M. Michael Wolfe, +2 more

- 17 Jun 1999 -

The New England Journal of Medicine

TL;DR: One hundred years have passed since Felix Hoffman reported the successful synthesis of acetylsalicylic acid as the first nonsteroidal antiinflammatory drug (NSAID) and numerous reports have corroborated this observation.

...read moreread less

Journal ArticleDOI

A BOILED-Egg To Predict Gastrointestinal Absorption and Brain Penetration of Small Molecules

Antoine Daina, +1 more

- 06 Jun 2016 -

ChemMedChem

TL;DR: The Brain Or IntestinaL EstimateD permeation method (BOILED‐Egg) is proposed as an accurate predictive model that works by computing the lipophilicity and polarity of small molecules.

...read moreread less

Journal ArticleDOI

From 2000 to mid-2010: a fruitful decade for the synthesis of pyrazoles.

Santos Fustero, +3 more

- 01 Aug 2011 -

Chemical Reviews

Collapse

Related Papers (5)

Design and synthesis of pyrimidine-5-carbonitrile hybrids as COX-2 inhibitors: Anti-inflammatory activity, ulcerogenic liability, histopathological and docking studies.

Abdallah M. Alfayomy, +7 more

- 01 Mar 2021 -

Bioorganic Chemistry

New pyrazole derivatives possessing amino/methanesulphonyl pharmacophore with good gastric safety profile: Design, synthesis, cyclooxygenase inhibition, anti-inflammatory activity and histopathological studies.

Khaled R.A. Abdellatif, +6 more

- 01 Jan 2020 -

Bioorganic Chemistry

Thiohydantoin derivatives incorporating a pyrazole core: Design, synthesis and biological evaluation as dual inhibitors of topoisomerase-I and cycloxygenase-2 with anti-cancer and anti-inflammatory activities.

Khaled R.A. Abdellatif, +4 more

- 01 Oct 2019 -

Bioorganic Chemistry

Novel quinoline incorporating 1,2,4-triazole/oxime hybrids: Synthesis, molecular docking, anti-inflammatory, COX inhibition, ulceroginicity and histopathological investigations.

Aliaa M. Mohassab, +6 more

- 01 Dec 2017 -

Bioorganic Chemistry

Design, synthesis, biological evaluation, and computational studies of novel thiazolo-pyrazole hybrids as promising selective COX-2 inhibitors: Implementation of apoptotic genes expression for ulcerogenic liability assessment.

Citations

Synthesis, Characterization and Molecular Docking of Novel Lonazolac Analogues 3-(3-Hydroxy-5-methyl-1H-pyrazol-4-yl)-3-arylpropanoic Acid Derivatives: Highly Potential COX-1/COX-2, Matrix Metalloproteinase and Protein Denaturation Inhibitors

Design, Synthesis, Biological Evaluation, and Computational Studies of Novel Fluorinated Candidates as PI3K Inhibitors: Targeting Fluorophilic Binding Sites.

Novel 5,6-diphenyl-1,2,4-triazine-3-thiol derivatives as dual COX-2/5-LOX inhibitors devoid of cardiotoxicity.

Catalyst and base free aza-Michael addition reaction: Synthesis of poly-substituted 4-pyrazole based benzopyrans

Novel Thiadiazol Derivatives; Design, Synthesis, Biological Activity, Molecular Docking and Molecular Dynamics

References

Theory and Practice of Histological Techniques

SwissADME: A free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules

Gastrointestinal toxicity of nonsteroidal antiinflammatory drugs.

A BOILED-Egg To Predict Gastrointestinal Absorption and Brain Penetration of Small Molecules

From 2000 to mid-2010: a fruitful decade for the synthesis of pyrazoles.

Related Papers (5)

Design and synthesis of pyrimidine-5-carbonitrile hybrids as COX-2 inhibitors: Anti-inflammatory activity, ulcerogenic liability, histopathological and docking studies.

New pyrazole derivatives possessing amino/methanesulphonyl pharmacophore with good gastric safety profile: Design, synthesis, cyclooxygenase inhibition, anti-inflammatory activity and histopathological studies.

Thiohydantoin derivatives incorporating a pyrazole core: Design, synthesis and biological evaluation as dual inhibitors of topoisomerase-I and cycloxygenase-2 with anti-cancer and anti-inflammatory activities.

Novel quinoline incorporating 1,2,4-triazole/oxime hybrids: Synthesis, molecular docking, anti-inflammatory, COX inhibition, ulceroginicity and histopathological investigations.

Synthesis, in vitro and in vivo biological evaluation, COX-1/2 inhibition and molecular docking study of indole-N-acylhydrazone derivatives