Pyrazole-based analogs as potential antibacterial agents against methicillin-resistance staphylococcus aureus (MRSA) and its SAR elucidation

Preparation and Physicochemical Characterization of Water-Soluble Pyrazole-Based Nanoparticles by Dendrimer Encapsulation of an Insoluble Bioactive Pyrazole Derivative

“…Currently, several studies have been reported on the synthesis and biological activity of pyrazole derivatives worldwide [ 2 ]. Currently, the pyrazole nucleus is present in numerous pharmacological agents belonging to different therapeutic categories, including Celecoxib (potent anti-inflammatory by COX-2 inhibition), Tepoxalin (nonsteroidal anti-inflammatory drugs (NSAIDs)), Crizotimib (anticancer), Surinabant, Difenamizole (anti-obesity), Mepiprazole (tranquillizer), Finopril (insecticide), CDPPB (antipsychotic), Betazole (analgesic), and Fezolamide (H2-receptor agonist and antidepressant agent), confirming the pharmacological potential of the pyrazole nucleus [ 2 , 3 ]. Figure 1 reports some of the marketed and well-established therapeutics containing the pyrazole unit.…”

“…The five membered heterocyclic diazole ring of pyrazole and its derivatives represent versatile template structures for designing potent bioactive agents [ 1 , 2 , 3 ]. In fact, molecules belonging to the pyrazole family have demonstrated possessing numerous biological activities, such as antimicrobial, anti-inflammatory, anticancer, analgesic, anticonvulsant, anthelmintic, antioxidant, and herbicidal effects, mainly due to the planar structure of the aromatic heterocycle [ 1 , 2 , 3 ].…”

“…The five membered heterocyclic diazole ring of pyrazole and its derivatives represent versatile template structures for designing potent bioactive agents [ 1 , 2 , 3 ]. In fact, molecules belonging to the pyrazole family have demonstrated possessing numerous biological activities, such as antimicrobial, anti-inflammatory, anticancer, analgesic, anticonvulsant, anthelmintic, antioxidant, and herbicidal effects, mainly due to the planar structure of the aromatic heterocycle [ 1 , 2 , 3 ]. In particular, the structure of the pyrazole ring presents three carbon atoms and two adjacent nitrogen atoms, and the pyrazole nucleus is also present in natural compounds (although rarely, probably due to difficulty in the formation of the N=N bond by living organisms) [ 4 ].…”

Heterocyclic Compounds: Pharmacology of Pyrazole Analogs From Rational Structural Considerations

“…The hunt for new analogs with desirable pharmacological profiles is a never-ending task in drug discovery programs. With the available literature on pyrazole analogs ( Fadaly et al, 2020 ; Mohamed et al, 2020 ; Azimi et al, 2021 ; Faudzi et al, 2021 ; Verma et al, 2021 ), it is relatively easy for medicinal chemists to proceed with rational synthesis or modification capable of enhancing biological activities. The substitutions, additions, or removal of functional groups are effective strategies for designing biologically important analogs.…”

Generation of truncated derivatives through in silico enzymatic digest of peptide GV30 target MRSA both in vitro and in vivo

“…Previous research indicated that more than 25% of nosocomial infections are associated with the formation of biofilms [8] . Most notably, MRSA has gradually developed drug resistance to most clinically approved antibiotics (including vancomycin) [9] . One of the solutions to these problems is to find a new drug that is different from the traditional single-target antibiotics, so as to break down the threat of MRSA to human health [10] .…”