Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Z Zhao, X Dai, C Li, X Wang, J Tian, Y Feng… - European journal of …, 2020 - Elsevier
The pyrazolone structural motif is a critical element of drugs aimed at different biological end-
points. Medicinal chemistry researches have synthesized drug-like pyrazolone candidates …

A critical review on recent trends on pharmacological applications of pyrazolone endowed derivatives

G Mustafa, M Zia-ur-Rehman, SH Sumrra… - Journal of Molecular …, 2022 - Elsevier
Pyrazolone is a well-known influential synthon for the synthesis of many molecules which
hold remarkable potential in the advancement of functional materials, coordination …

Discovery of novel pyrazole and pyrazolo[1,5‐a]pyrimidine derivatives as cyclooxygenase inhibitors (COX‐1 and COX‐2) using molecular modeling simulation

R Ayman, AM Radwan, AM Elmetwally… - Archiv der …, 2023 - Wiley Online Library
Searching for effective and selective anti‐inflammatory agents, our study involved designing
and synthesizing new pyrazole and pyrazolo [1, 5‐a] pyrimidine derivatives 4–11. The …

Recent advancement in the discovery and development of COX-2 inhibitors: Insight into biological activities and SAR studies (2008–2019)

V Sharma, P Bhatia, O Alam, MJ Naim, F Nawaz… - Bioorganic …, 2019 - Elsevier
Cyclooxygenase-2 is a very important physiological enzyme playing key roles in various
biological functions especially in the mechanism of pain and inflammation, among other …

Progress in the development of TRPV1 small-molecule antagonists: Novel Strategies for pain management

K Zhu, L Wang, TT Liao, W Li, J Zhou, Y You… - European journal of …, 2023 - Elsevier
Transient receptor potential vanilloid 1 (TRPV1) channels are widely distributed in sensory
nerve endings, the central nervous system, and other tissues, functioning as ion channel …

Synthetically-tailored and nature-derived dual COX-2/5-LOX inhibitors: Structural aspects and SAR

MA Meshram, UO Bhise, PN Makhal, VR Kaki - European Journal of …, 2021 - Elsevier
Inflammation is a most complex pathological process that gives birth to different diseases.
Different inflammatory mediators are released during an inflammation responsible for acute …

Novel pyrazole-based COX-2 inhibitors as potential anticancer agents: Design, synthesis, cytotoxic effect against resistant cancer cells, cell cycle arrest, apoptosis …

PA Halim, SMZ Sharkawi, MB Labib - Bioorganic chemistry, 2023 - Elsevier
Novel differently substituted pyrazole derivatives were designed, synthesized and evaluated
for their anticancer activity. All compounds selectively inhibited COX-2 enzyme (IC 50 …

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 …

Acyl pyrazole sulfonamides as new antidiabetic agents: synthesis, glucosidase inhibition studies, and molecular docking analysis

A Ahmed, S Zaib, MA Bhat, A Saeed, MZ Altaf… - Frontiers in …, 2024 - frontiersin.org
Diabetes mellitus is a multi-systematic chronic metabolic disorder and life-threatening
disease resulting from impaired glucose homeostasis. The inhibition of glucosidase …

Optimization of pyrazole-based compounds with 1, 2, 4-triazole-3-thiol moiety as selective COX-2 inhibitors cardioprotective drug candidates: Design, synthesis …

KRA Abdellatif, EKA Abdelall, HAH Elshemy… - Bioorganic …, 2021 - Elsevier
The cardiovascular side effects associated with COX-2 selective drugs were the worst for
coxibs leading to their withdrawal from the market a few years after their discovery …