ArticleRSC advances2020
Design, synthesis and biological evaluation of new 2-aminothiazole scaffolds as phosphodiesterase type 5 regulators and COX-1/COX-2 inhibitors.
Article in RSC advances, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
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Who cites it
18 citing papers in PubMed, 48 citations in OpenAlex.
- Recent advances in thiazole-based derivatives targeting diverse anti-inflammatory pathways.RSC advances · 2026Review
- Synthesis and quantum chemical studies of polyfunctionally substituted pyridines incorporating pyrimidine moiety for corrosion Inhibition.Scientific reports · 2026Article
- Recent Advances in the Therapeutic Prospective of Heterocyclic Derivatives as COX-2 Inhibitors (2019-Present).Mini reviews in medicinal chemistry · 2026Review
- An overview on pharmaceutical applications of phosphodiesterase enzyme 5 (PDE5) inhibitors.Molecular diversity · 2025Review
- UV-Induced Photodegradation of 2-Aminothiazole-4-Carboxylic Acid: Identification of New Carbodiimide Molecules.Molecules (Basel, Switzerland) · 2025Article
- Novel di-aryl chalcone derived pyrazole linked to methane sulfonyl pharmacophore as potent selective COX-2 inhibitors; design, synthesis, molecular modeling,Future medicinal chemistry · 2025Article
- Genetically proxied inhibition of Phosphodiesterase-5 and cancer risks: A drug-target Mendelian randomization analysis.Scientific reports · 2025Article
- Discovery and optimization of 4-(imidazo[1,2-a]pyrimidin-3-yl)thiazol-2-amine derivatives as novel phosphodiesterase 4 inhibitors.Molecular diversity · 2025Article
- Design, synthesis and biological evaluation of thienopyridine derivatives as c-Met kinase inhibitors.Molecular diversity · 2025Article
- An Efficient Synthesis of Novel Aminothiazolylacetamido-Substituted 3,5-Bis(arylidene)-4-piperidone Derivatives and Their Cytotoxicity Studies.ACS omega · 2024Article
- New 1,2,3-triazole/1,2,4-triazole hybrids linked to oxime moiety as nitric oxide donor selective COX-2, aromatase, B-RAFJournal of enzyme inhibition and medicinal chemistry · 2023Article
- Direct selenosulfonylation of unsaturated compounds: a review.RSC advances · 2022Review
- Non-steroidal anti-inflammatory drugs: recent advances in the use of synthetic COX-2 inhibitors.RSC medicinal chemistry · 2022Review
- Synthesis, characterization,RSC advances · 2022Article
- Novel Hybrid Compounds Containing Benzofuroxan and Aminothiazole Scaffolds: Synthesis and Evaluation of Their Anticancer Activity.International journal of molecular sciences · 2021Article
- An Overview on Synthetic 2-Aminothiazole-Based Compounds Associated with Four Biological Activities.Molecules (Basel, Switzerland) · 2021Review
- Multifunctional Isosteric Pyridine Analogs-Based 2-Aminothiazole: Design, Synthesis, and Potential Phosphodiesterase-5 Inhibitory Activity.Molecules (Basel, Switzerland) · 2021Article
- Amino Acid Conjugates of Aminothiazole and Aminopyridine as Potential Anticancer Agents: Synthesis, Molecular Docking and in vitro Evaluation.Drug design, development and therapy · 2021Article
Corrections and comments
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Authors and funding
8 authors at 4 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A new series of 2-aminothiazole derivatives was designed and prepared as phosphodiesterase type 5 (PDE5) regulators and COX-1/COX-2 inhibitors. The screening of the synthesized compounds for PDE5 activity was carried out using sildenafil as a reference drug. Strikingly, compounds 23a and 23c were found to have a complete inhibitory effect on PDE5 (100%) at 10 μM without causing hypotension and the limited side effect of PDE5 inhibitors, suggest a distinctive therapeutic role of these derivatives in erectile dysfunction. On the other hand, compounds 5a, 17, 21 and 23b increased the PDE5 activity (PDE5 enhancers) at 10 μM. In addition, the study includes the screening of the COX-1/COX-2 inhibition induced by the synthesized compounds. All tested compounds have an inhibitory effect against COX-1 activity (IC
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.