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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Darolutamide has a novel chemical structure compared to the other approved NSAAs. In common with these agents, it contains a phenyl moiety with two ortho-substituted electron withdrawing groups, in this case chlorine and nitrile groups. However, the rest of the molecule is unique and based on two pyrazole rings separated by an ethylamido chain.
Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Feprazone is a pyrazole derivative and nonsteroidal anti-inflammatory drug (NSAID) that has analgesic, anti-inflammatory and antipyretic properties. It is or has been used to treat mild to moderate pain, fever, and inflammation associated with musculoskeletal and joint disorders (1).
Clinical pharmacology: traditional NSAIDs and selective COX-2 inhibitors
Published in Pamela E Macintyre, Suellen M Walker, David J Rowbotham, Clinical Pain Management, 2008
Stephen F Jones, Aidan M O’Donnell
The pyrazole class includes metamizole, azapropazone, phenylbutazone, and oxyphenbutazone. They have largely been withdrawn for human use in the USA and Europe, although continue to be important drugs worldwide. Oxyphenbutazone is the major metabolite of phenylbutazone, differing only in the substitution of a single hydroxyl group in place of a hydrogen atom. It has a longer half-life than the parent drug. All pyrazoles may cause skin reactions, bone marrow suppression and agranulocytosis, and anaphylactoid episodes.
Towards safer anti-inflammatory therapy: synthesis of new thymol–pyrazole hybrids as dual COX-2/5-LOX inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Mostafa M. M. El-Miligy, Ahmed K. Al-Kubeisi, Mohamed G. Bekhit, Saad R. El-Zemity, Rasha A. Nassra, Aly A. Hazzaa
The in vitro inhibition of COX-1/2 and 5-LOX assays and the in vivo anti-inflammatory testing showed that, substitution at para position of phenyl at position 5 of pyrazole by either electron donating group (OCH3) or electron withdrawing group (Br) or unsubstituted did not affect the activity. This could be due to the presence of the phenyl ring out of coplanarity with the pyrazole moiety so could not affect the electronic configuration of the whole molecule hence binding affinity and activity. On the other hand, substitution at N1 of pyrazole affected the activity. The unsubstituted derivative 4a showed in vitro COX-2/5-LOX inhibitory activity and in vivo potent anti-inflammatory activity. Furthermore, the activities of N1 aryl substituted derivatives were affected with the type of substitution at para position of N1 phenyl moiety. The substitution with either sulphonamide group or chloro showed higher in vitro COX-2/5-LOX inhibitory activity and in vivo anti-inflammatory activity than unsubstituted derivatives. This could be due to the importance of sulphonamide and chloro groups in polar and hydrophobic interactions with the active sites of the target COX-2/5-LOX enzymes.
Biofilm and Quorum Sensing inhibitors: the road so far
Published in Expert Opinion on Therapeutic Patents, 2020
Simone Carradori, Noemi Di Giacomo, Martina Lobefalo, Grazia Luisi, Cristina Campestre, Francesca Sisto
Under stressful conditions, bacterial cells block cell replication and DNA synthesis through the modulation of specific cell cycle checkpoints which involve the induction of adaptative responses mediated by RelA to finely modulate the macromolecules synthesis on the basis of the level of nutrients [27]. The starting point is the accumulation of bacterial signaling molecules collectively called (p)ppGpp synthesized by a ribosome-dependent pyrophosphatase transfer (e.g. RelA). Using the PDB file 5IQR (RelA bound to 70S ribosome), the inventors determined the binding affinity within the 1.1 million compounds present in the ChemBridge library [28]. The most promising ones were bought or synthesized to be used in cellular assays against E. coli strain C growth and biofilm (Figure 7). The proposed compounds, belonging to the class of pyrazoles, should prevent the triggering of the stringent response in bacteria avoiding the development of ‘persister’ phenotypes and repotentiating clinically used antibiotics.
Novel heterocyclic hybrids of pyrazole targeting dihydrofolate reductase: design, biological evaluation and in silico studies
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Ismail M. M. Othman, Mohamed A. M. Gad-Elkareem, Abd El-Galil E. Amr, Mohamed A. Al-Omar, Eman S. Nossier, Elsayed A. Elsayed
Pyrazoles are a class of interesting heterocyclic compounds characterised by the presence of two nitrogen atoms adjacent to three carbon atoms in five-membered aromatic ring structure10. Pyrazole derivatives play an imperative role in wide spectrum of biological activities including antibacterial11, antifungal12, anti-inflammatory13–15, analgesic16, oestrogen receptor binding17, neuroprotective18, antineoplastic agents19. Furthermore, several reports exhibited that pyrazoles I–IV and pyrazolo[3,4-d]pyrimidine V (Figure 1) had high bactericidal and fungicidal activity against the reference strains20–24. Additionally, the pyrazole-containing cores (VI–VII) were found to be active as antimicrobial and antimalarial through inhibition of DHFR25–27 (Figure 2). Regarding to their broad spectrum of biological activities, pyrazole ring has been considered as a favourable unit for addition in the field of drug discovery and therefore in the pharmaceutical industry10.