[HTML][HTML] A review of the recent development in the synthesis and biological evaluations of pyrazole derivatives

O Ebenezer, M Shapi, JA Tuszynski - Biomedicines, 2022 - mdpi.com
Pyrazoles are five-membered heterocyclic compounds that contain nitrogen. They are an
important class of compounds for drug development; thus, they have attracted much …

Design and Development of COX-II Inhibitors: Current Scenario and Future Perspective

S Chahal, P Rani, Kiran, J Sindhu, G Joshi… - ACS …, 2023 - ACS Publications
Innate inflammation beyond a threshold is a significant problem involved in cardiovascular
diseases, cancer, and many other chronic conditions. Cyclooxygenase (COX) enzymes are …

Novel tetrazole-based selective COX-2 inhibitors: Design, synthesis, anti-inflammatory activity, evaluation of PGE2, TNF-α, IL-6 and histopathological study

MB Labib, AM Fayez, ELN EL-Shaymaa… - Bioorganic …, 2020 - Elsevier
To search for effective and selective COX-2 inhibitors, four novel series of tetrazole
derivatives were designed based on bioisosteric replacement of SO 2 NH 2 in celecoxib with …

Design, synthesis and molecular modeling of novel aryl carboximidamides and 3-aryl-1, 2, 4-oxadiazoles derived from indomethacin as potent anti-inflammatory iNOS …

MFA Mohamed, AA Marzouk, A Nafady… - Bioorganic …, 2020 - Elsevier
The development of NSAIDs/iNOS inhibitor hybrids is a new strategy for the treatment of
inflammatory diseases by suppression of the overproduction of PGE 2 and NO. A novel …

Drug repurposing to enhance antitumor response to PD-1/PD-L1 immune checkpoint inhibitors

X Thuru, R Magnez, H El-Bouazzati, G Vergoten… - Cancers, 2022 - mdpi.com
Simple Summary Novel pharmacological approaches are needed to improve treatments of
advanced cancers, despite the considerable benefit of immunotherapy. New drugs are …

Pyrazole/pyrazoline as an excellent pharmacophore in the design of carbonic anhydrase inhibitors (2018–2022)

A Dorbabu - Archiv der Pharmazie, 2023 - Wiley Online Library
Carbonic anhydrase (CA) is a metalloenzyme that catalyzes the interconversion between
carbon dioxide and water and dissociated ions of carbonic acid. In addition, CA performs …

Synthesis of lathyrane diterpenoid nitrogen-containing heterocyclic derivatives and evaluation of their anti-inflammatory activities

W Wang, L Xiong, Y Li, Z Song, D Sun, H Li… - Bioorganic & Medicinal …, 2022 - Elsevier
As our ongoing work on lathyrane diterpenoid derivatization, three series of lathyrane
diterpenoid derivatives were designed and synthesized based combination principles …

Inhibitory activities of bipyrazoles: a patent review

AA Abbas, MH Abdellattif… - Expert Opinion on …, 2022 - Taylor & Francis
Introduction Bipyrazole is constituted from two pyrazole units either in their fully aromatic or
partially hydrogenated forms. Pyrazoles are widely available in pharmaceutical and …

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

T Das, S Mohapatra, NP Mishra, S Nayak - Tetrahedron Letters, 2022 - Elsevier
An efficient and catalyst free protocol has been disclosed for aza-Michael addition reaction
of pyrazoles with 2-aryl-3-nitro-2H-chromene derivatives, which provides synthetically …

Discovering the inhibition of YAP/TEAD Hippo signaling pathway via new pyrazolone derivatives: synthesis, molecular docking and biological investigations

AA Noser, MM Salem, MH Baren, AI Selim… - Scientific Reports, 2024 - nature.com
Heterocyclic compounds play a crucial role in the drug discovery process and development
due to their significant presence and importance. Here, we report a comprehensive analysis …