Anti-Inflammatory Activity of Quinazolinoformazans

Kalsi, R.; Pande, Kalpana; Bhalla, T. N.; Barthwal, J. P.; Gupta, G.P.; Parmar, Surendra S.

doi:10.1002/jps.2600790409

Cited by 36 publications

(27 citation statements)

References 11 publications

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“…Obviously, the rotation about the N-CO bond seems to be fast on NMR time scale. The disappearance of C O stretching frequency around 1710 cm -1 and the presence of C N stretching frequency confirm the formation of hydrazone derivatives (14)(15)(16)(17)(18)(19). The weak band appeared at 3420 cm -1 corresponds to the -NH stretching mode of the thiazole moiety.…”

Section: Analytical Resultsmentioning

confidence: 65%

“…The in vitro activities of compounds (14)(15)(16)(17)(18)(19) were tested in Sabourauds dextrose broth (SDB) (Himedia, Mumbai) for fungi and nutrient broth (NB) (Himedia, Mumbai) for bacteria by the disc diffusion method. MIC values were determined by twofold serial dilution method (Dhar et al, 1968).…”

Section: In Vitro Antibacterial and Antifungal Activitymentioning

confidence: 99%

“…The synthesized compounds (14)(15)(16)(17)(18)(19) were tested for their in vitro antibacterial activity against selected Gram positive and Gram negative pathogens. (E)-(4-(2-(benzo[d]thiazol-2-yl)hydrazono)-3-methyl-2,6-diphenylpiperidin-1-yl)(phenyl)methanone (14)(15)(16)(17)(18)(19) derivatives exhibited a wide spectrum of antibacterial profile in In vitro against all the tested organisms as shown in Table 3.…”

Section: Antibacterial Activitymentioning

confidence: 99%

“…(E)-(4-(2-(benzo[d]thiazol-2-yl)hydrazono)-3-methyl-2,6-diphenylpiperidin-1-yl)(phenyl)methanone (14)(15)(16)(17)(18)(19) derivatives exhibited a wide spectrum of antibacterial profile in In vitro against all the tested organisms as shown in Table 3. Table 3.…”

Section: Antibacterial Activitymentioning

confidence: 99%

“…The utility of substituent's at second, third and sixth positions, particularly aromatic substituent at second and/or sixth positions with regard to its biological activity have well documented by many workers [7][8]. Hydrazone derivatives have been claimed to exhibit appreciable antimicrobial [9][10][11][12] antitubercular [13] anticonvulsant [14] antiviral [15] and anti-inflammatory [16] activities.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis, Biological Evaluation and Docking Studies of some Novel (E)-(4-(2-(Benzo[d]Thiazol-2-yl)Hydrazono)Methyl-2,6-Diphenylpiperidin-1-yl)(Phenyl)Methanone Derivatives

Rajaraman

Sundararajan

Krishnasamy

2015

ILCPA

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ABSTRACT.A series of biologically active some novel (E)-(4-(2-(benzo [d] thiazol-2-yl)hydrazono)-3-methyl-2,6-diphenylpiperidin-1-yl)(phenyl)methanone derivatives (14-19) were synthesized and characterized by IR, 1 H NMR, 13C NMR and HSQC spectral analysis. Molecular docking studies were also carried out for compounds 14-19 using the crystal structure of Ribonucleotide Reductase to disclose the binding mode and orientation of target molecule into the active site of respective receptors. The synthesized compounds were also screened for their antimicrobial activity against selected panel strains Antimicrobial studies revealed that the synthesized compound 14 exhibited noticeable activity against B.cerus whereas compounds17 and 18 displayed appreciable activity against K.pneumoniae. Bromo substituted phenyl group at C-2 and C-6 of piperidine ring showed excellent antibacterial activity against K.pneumoniae and B.cerus at MIC of 25μg/ml. The antifungal studies revealed that compounds 17, 18 and 19 exposed significant antifungal activity against the pathogenic strains used in this study. In particular compound 19 are showed excellent antifungal activity against C.albicans and A.niger.

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Section: Analytical Resultsmentioning

confidence: 65%

Section: In Vitro Antibacterial and Antifungal Activitymentioning

confidence: 99%

Section: Antibacterial Activitymentioning

confidence: 99%

Section: Antibacterial Activitymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Synthesis, Biological Evaluation and Docking Studies of some Novel (E)-(4-(2-(Benzo[d]Thiazol-2-yl)Hydrazono)Methyl-2,6-Diphenylpiperidin-1-yl)(Phenyl)Methanone Derivatives

Rajaraman

Sundararajan

Krishnasamy

2015

ILCPA

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References

1996

Chemistry of Heterocyclic Compounds: A Series of Monographs

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Synthesis, DFT, computational exploration of chemical reactivity, molecular docking studies of novel formazan metal complexes and their biological applications

Khan

Rızwan

Shahid

et al. 2020

Applied Organom Chemis

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The computational exploration of chemical reactivity and molecular docking of the synthesized formazan compounds (S1‐S6) were studied. Further, their antimicrobial activity against bacterial strains (S. epidermidis, B. cereus, K. pneumoniae and P. aeruginosa) and against fungal strains (T. mentagrophytes, C. albicans, A. niger, S. cerevisiae and C. glabrata) using agar diffusion method and antioxidant activity following DPPH inhibition assays were evaluated. Anticancer activity was executed in vitro model of human breast carcinoma (MCF‐7) cell line. The superior and enhanced antibacterial and antimycotic activities were exhibited by formazan compound (S4) by presenting maximum ZOIs and MICs values. While enhanced antioxidant in terms of percentage inhibition of DPPH and cytotoxic effect on human breast carcinoma‐cells demonstrated by formazan compound (S1) which was further validated by the results of molecular docking studies of (S1) with the human estrogen receptor protein. In order to compute quantum chemical reactivity descriptors from conceptual density functional theory (CDFT) point of view of this system, including chemical potential (μ), chemical hardness (η), electrophilicity (ω), condensed Fukui function and dual descriptors are calculated at the same level of calculation. The most active sites of these molecules are determined and correlated with experimental data. The present investigation displays that formazans compounds could be potential drug candidate that constrains the growth of microbial strains, possess ability to cause cytotoxic effect on carcinoma cells and act as effective scavenger for free radical species.

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Anti-Inflammatory Activity of Quinazolinoformazans

Cited by 36 publications

References 11 publications

Synthesis, Biological Evaluation and Docking Studies of some Novel (E)-(4-(2-(Benzo[d]Thiazol-2-yl)Hydrazono)Methyl-2,6-Diphenylpiperidin-1-yl)(Phenyl)Methanone Derivatives

Synthesis, Biological Evaluation and Docking Studies of some Novel (E)-(4-(2-(Benzo[d]Thiazol-2-yl)Hydrazono)Methyl-2,6-Diphenylpiperidin-1-yl)(Phenyl)Methanone Derivatives

References

Synthesis, DFT, computational exploration of chemical reactivity, molecular docking studies of novel formazan metal complexes and their biological applications

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