Pyrazole Schiff Base Hybrids as Anti-Malarial Agents: Synthesis, In Vitro Screening and Computational Study

Aggarwal, Sanjeev; Paliwal, Deepika; Kaushik, Dhirender; Gupta, Girish Kumar; Kumar, Ajay

doi:10.2174/1386207321666180213092911

Cited by 49 publications

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“…Over many decades, imine moiety has been receiving increasing attention due to a wide range of biological activities as well like anti-cancer [ 6 ], antioxidant [ 7 ], antimalarial [ 8 ], antibacterial [ 9 , 10 ] and anti-HIV [ 11 ]. Recently, imine- nanocapsules show a highly effective delivery of an insufficiency soluble cancer drug into tumour cells [ 12 ].…”

Section: Introductionmentioning

confidence: 99%

An efficient synthesis of furan-3(2 H )-imine scaffold from alkynones

et al. 2021

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A novel efficient method to generate spiro furan-3(2 H )-imine derivatives is established by the reaction between the α , β -unsaturated ketones and aniline derivatives. The reaction involves 1,4- addition of aniline followed by the subsequent intramolecular cyclization mediated by tertiary alcohol to produce the furan-3(2 H )-imine. All the synthesized compounds are characterized using nuclear magnetic resonance and high-resolution mass spectrometry (HRMS).

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Section: Introductionmentioning

confidence: 99%

An efficient synthesis of furan-3(2 H )-imine scaffold from alkynones

et al. 2021

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“…On the other hand, pyrazole moiety containing both N-(4-chlorophenyl) and (2-fluorophenyl)acrylamide derivative (VI) produced potent antifungal activity [19]. Recently, there is a growing interest in the synthesis of Schiff bases tethered pyrazole ring because of their importance in biological activities [20][21][22]. For example, Schiff base (VII), bearing imidazole and pyrazole nucleus, showed potency against E. coli [23].…”

Section: Introductionmentioning

confidence: 99%

Discovery of New Schiff Bases Tethered Pyrazole Moiety: Design, Synthesis, Biological Evaluation, and Molecular Docking Study as Dual Targeting DHFR/DNA Gyrase Inhibitors with Immunomodulatory Activity

et al. 2020

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A series of Bis-pyrazole Schiff bases (6a–d and 7a–d) and mono-pyrazole Schiff bases (8a–d and 9a–d) were designed and synthesized through the reaction of 5-aminopyrazoles 1a–d with aldehydes 2–5 using mild reaction condition with a good yield percentage. The chemical structure of newly formed Schiff bases tethered pyrazole core was confirmed based on spectral and experimental data. All the newly formed pyrazole Schiff bases were evaluated against eight pathogens (Gram-positive, Gram-negative, and fungi). The result exhibited that, most of them have good and broad activities. Among those, only six Schiff bases (6b, 7b, 7c, 8a, 8d, and 9b) displayed MIC values (0.97–62.5 µg/mL) compared to Tetracycline (15.62–62.5 µg/mL) and Amphotericin B (15.62–31.25 µg/mL), MBC values (1.94–87.5 µg/mL) and selectivity to tumor cell than normal cells. Immunomodulatory activities showed that the promising Schiff bases increase the immunomodulator effect of defense cell and the Schiff base 8a is the highest one by (Intra. killing activity = 136.5 ± 0.3%) having a pyrazole moiety as well as amide function (O=C-NH2) and piperidinyl core. Furthermore, the most potent one exhibited broad activity depending on both MIC and MBC values. Moreover, to study the mechanism of these pyrazole Schiff bases, two active Schiff bases 8a and 9b from six derivatives were introduced to study the enzyme assay as dihydrofolate reductase (DHFR) on E. coli organism and DNA gyrase with two different organisms, S. aureus and B. subtilis, to determine the inhibitory activities with lower values in the case of DNA gyrase (8a and 9b) or nearly as DHFR compound 9b, while pyrazole 8a showed excellent inhibitory against all enzyme assay. The molecular docking study against dihydrofolate reductase and DNA gyrase were performed to study the binding between active site in the pocket with the two Schiff bases (8a and 9b) that exhibited good binding affinity with different bond types as H-bonding, aren-aren, and arene-cation interaction as well as study the physicochemical and pharmacokinetic properties of the two active Schiff bases 8a and 9b.

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“…So this is a good intermediate in the reaction involving the interaction of an enzyme with an amino or a carbonyl group of the substrate. In addition to this Schiff base are having excellent biological activities such as antimalarial [15], antibacterial [16], antifungal [17], antiviral [18], antitumor [19] and antioxidant [20] activities. At the same time they have stronger binding affinity towards DNA double helix [21].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of novel Schiff bases containing arylpyrimidines as promising antibacterial agents

Nayak

Poojary

2019

Heliyon

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Pursuing our recent interest regarding the antimicrobial activity of Schiff bases derivatives, we have synthesized a series of 6-(substitutedphenyl)- N' -(( E )-(substitutedphenyl)methylidene)-2-methylpyridine-3-carbohydrazides ( 5a-n ) and evaluated their antibacterial activity. Structures of these compounds were confirmed by standard studies of FTIR, 1 H NMR, 13 C NMR, MS and elemental analysis. Antibacterial activity of synthesized molecules was tested against Gram-positive ( S. aureus and E. faecalis ) and Gram-negative ( E. coli and P. aeruginosa ) bacterial strains. Synthesized compounds showed good antibacterial activity at a lower concentration than standard. Most of the compounds ( 5a , 5c , 5i , 5j and 5n ) are potent against all the tested bacterial strains with MIC values ranging from 1.56-12.5 μg/mL.

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Pyrazole Schiff Base Hybrids as Anti-Malarial Agents: Synthesis, In Vitro Screening and Computational Study

Abstract: We provide evidence which implicates pyrazole Schiff base hybrids as potential prototypes for the development of antimalarial agents.

Cited by 49 publications

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An efficient synthesis of furan-3(2 H )-imine scaffold from alkynones

An efficient synthesis of furan-3(2 H )-imine scaffold from alkynones

Discovery of New Schiff Bases Tethered Pyrazole Moiety: Design, Synthesis, Biological Evaluation, and Molecular Docking Study as Dual Targeting DHFR/DNA Gyrase Inhibitors with Immunomodulatory Activity

Synthesis of novel Schiff bases containing arylpyrimidines as promising antibacterial agents

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