Synthesis of novel 2-pyrazoline analogues with potent anti-inflammatory effect mediated by inhibition of phospholipase A2: Crystallographic, in silico docking and QSAR analysis

Lokeshwari, D. M.; Achutha, Dileep Kumar; Srinivasan, Bharath; Naveen, S.; Krishnappagowda, Lokanath Neratur; Kariyappa, Ajay Kumar

doi:10.1016/j.bmcl.2017.06.063

Cited by 33 publications

(13 citation statements)

References 26 publications

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“…Well‐known samples are Celecoxib (Celebrex) and Sildenafil (Viagra). Products of pyrazoles have been exposed to possess diverse properties including, but not restricted to, being antitumor, antidiabitic, anti‐inflammatory, antiarrhythmic, monoamine oxidase inhibiting, sPLA2‐inhibitory, antipyretic, analgesic, anticonvulsant, and antimicrobial . In fact, preparation method equally represents a pivotal role to discover the biologically active pyrazoles and their belongings.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Reddy

Garcia

Yuvaraja

et al. 2020

Journal of Heterocyclic Chem

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The major diseases spread in the environment only because of microbes. Even, intensive care units in the hospitals are polluted by microorganisms, particularly, Gram-positive bacteria. Although many antibiotics are existed, there is a need to develop up to date microbial-resistant agents. Hence, the current study aimed to develop prominent antimicrobial drug-related compounds. Thus, a novel series of tri-substituted analogs and their intermediates were synthesized. In addition, total new compounds were screened for their antimicrobial assay and identified as the most efficient biologically active compounds. Moreover, minimal inhibitory antimicrobial activity and appropriate structure activity relationships were investigated. From the results it was observed that, viability of Gram-positive bacteria was most powerfully affected by all active compounds. Finally, this research demonstrated that, these biologically energetic amalgams can be utilized for further preclinical studies with the ambition of standing unique inventive drugs.

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Section: Introductionmentioning

confidence: 99%

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Reddy

Garcia

Yuvaraja

et al. 2020

Journal of Heterocyclic Chem

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“…Accumulating evidence has shown that chalcones and their derivatives could inhibit tumor initiation and progression. In view of the above, and as a part of our ongoing research on chalcone derivatives (Naveen et al, 2017;Lokeshwari et al, 2017;Tejkiran et al, 2016), we report herein the synthesis, crystal structure and Hirshfeld surface analysis of the title compound.…”

Section: Chemical Contextmentioning

confidence: 98%

Crystal structure and Hirshfeld surface analysis of (E)-3-(2-chloro-4-fluorophenyl)-1-(2,5-dichlorothiophen-3-yl)prop-2-en-1-one

et al. 2018

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“…Recent analysis of a Food and Drug Administration-approved drug database revealed that 59% of unique small-molecule drugs contain at least one nitrogen heterocycle [2]. Pyrazolines in particular, constitute a class of five-membered heterocycles incorporating a nitrogen-nitrogen (N-N) bond [3], with remarkable pharmacological applications [4] as anticancer [5][6][7][8][9], anti-inflammatory [10][11][12], antimicrobial [13,14], and antimalarial drugs [15].…”

Section: Introductionmentioning

confidence: 99%

(E)-(1-(4-Ethoxycarbonylphenyl)-5-(3,4-dimethoxyphenyl)-3-(3,4-dimethoxystyryl)-2-pyrazoline: Synthesis, Characterization, DNA-Interaction, and Evaluation of Activity Against Drug-Resistant Cell Lines

Matiadis

Mavroidi

Panagiotopoulou

et al. 2020

Molbank

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(E)-1-(4-Ethoxycarbonylphenyl)-5-(3,4-dimethoxyphenyl)-3-(3,4-dimethoxystyryl)-2-pyrazoline was synthesized via the cyclization reaction between the monocarbonyl curcuminoid (2E,6E)-2,6-bis(3,4-dimethoxybenzylidene)acetone and ethyl hydrazinobenzoate in high yield and purity (>95% by High-performance liquid chromatography (HPLC)). The compound has been fully characterized by 1H, 13C NMR, FTIR, UV-Vis and HRMS and its activity was evaluated in terms of its potential interaction with DNA as well as its cytotoxicity against resistant and non-resistant tumor cells. Both DNA thermal denaturation and DNA viscosity measurements revealed that a significant intercalation binding takes place upon treatment of the DNA with the synthesized pyrazoline, causing an increase in melting temperature by 3.53 ± 0.11 °C and considerable DNA lengthening and viscosity increase. However, neither re-sensitisation of Doxorubicin (DO X)-resistant breast cancer and multidrug resistance (MDR) reversal nor synergistic activity with DOX by potentially increasing the DOX cell killing ability was observed.

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Synthesis of novel 2-pyrazoline analogues with potent anti-inflammatory effect mediated by inhibition of phospholipase A2: Crystallographic, in silico docking and QSAR analysis

Cited by 33 publications

References 26 publications

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Crystal structure and Hirshfeld surface analysis of (E)-3-(2-chloro-4-fluorophenyl)-1-(2,5-dichlorothiophen-3-yl)prop-2-en-1-one

(E)-(1-(4-Ethoxycarbonylphenyl)-5-(3,4-dimethoxyphenyl)-3-(3,4-dimethoxystyryl)-2-pyrazoline: Synthesis, Characterization, DNA-Interaction, and Evaluation of Activity Against Drug-Resistant Cell Lines

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