A New Series of 1,3,4-Oxadiazole Linked Quinolinyl-Pyrazole/Isoxazole Derivatives: Synthesis and Biological Activity Evaluation

Basavanna, Vrushabendra; Chandramouli, Manasa; Kempaiah, C.; Bhadraiah, Umesha K.; Chandra,; Gowda, N. S. Linge; Doddamani, Shridevi; Ningaiah, Srikantamurthy

doi:10.1134/s1070363221110128

Cited by 5 publications

(2 citation statements)

References 26 publications

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“…[29] Inhibition of dihydrofolate reductase (DHFR) leads to inhibit folate metabolism which can cause bacterial death. [30] The docking study of similar types of compounds was reported with dihydrofolate reductase (DHFR) [31] and DNA gyrase [32] As compound 4 n was found to be most potent from the invitro antibacterial screening, we studied the possible binding of 4 n with PDB IDs 1KZN and 2W9H. A closer visual inspection of a binding pose of the ligand with protein is depicted in Figures 3A and 3B.…”

Section: Molecular Docking Studymentioning

confidence: 96%

Anomaly of Pyrano[2,3‐c]pyrazole Synthesis towards Pyrazolyl‐aryl‐methyl‐malononitrile Derivatives and Their Antimicrobial Activity

2022

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Our attempt to prepare pyrano[2,3-c]pyrazole derivatives from 2-methyl-5-propyl-1,2-dihydro-pyrazolone, malononitrile and benzaldehyde rather lead to the formation of pyrazolyl-arylmethyl-malononitrile derivatives. Fascinating by this opportunity to branch out the synthesis of substituted pyrazolone derivatives using an efficient multicomponent synthetic approach for pyrazolyl-aryl-methyl-malononitrile derivatives. The synthesis was accelerated using guanidine carbonate as a catalyst in the water reaction medium. The rection has blossomed with the green aspects of synthesis such as organo-catalyst, water as reaction medium and ambient temperature providing clean product in higher yield. The synthesized derivatives have been screened for anti-microbial activity. Compounds 4 c and 4 n showed excellent activity. Six compounds were found to be much effective against the Staphylococcus aureus bacterial strain. The molecular docking study of 4 n showed a high binding affinity with the receptor. Collectively, our study provides eco-friendly synthesis towards pyrazolyl-aryl-methyl-malononitrile derivatives and we evaluated them as a new class of anti-microbial compounds.

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Section: Molecular Docking Studymentioning

confidence: 96%

Anomaly of Pyrano[2,3‐c]pyrazole Synthesis towards Pyrazolyl‐aryl‐methyl‐malononitrile Derivatives and Their Antimicrobial Activity

2022

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“…The direct cyclisation of methyl nicotinoyl hydrazone to 1,3,4-heterocyclic compounds were completed by using various reagents such as acetic anhydride, phosphorus penta oxide, thionyl chloride, and polyphosphoric acid. Increasing bacterial resistance against antibiotics, leading to many drugs interaction and reducing the drug efficacy, such as local tissue irritation, narrow antimicrobial spectrum and Interference with wound healing processes (9,10) . For this reason, there is always a need to develop new types of synthetic agents and reduce the toxic effect by modifying the chemical structure.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Evolution Anticancer and Microbial Activity of Some 1,3,4-Oxadiazoles Analogues

Mohsen¹,

Hadi²

2022

The Egyptian Journal of Hospital Medicine

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Introduction:The need to develop anti-cancer drugs and the increasing bacteria resistance towered many antibiotics have made researchers more interested in testing the ability of synthetic derivatives to inhibit different types of microorganisms, although studying the cytotoxicity effect on various species of cancer cells. Aim: synthesis methyl nicotinate derivatives and evolution their anti-microbial and anti-cancer ability. Material and methods: a series of 1,3,4-oxadiazole heterocyclic compounds were synthesized, a nicotinoyl hydrazine was synthesized by refluxed methyl nicotinate and hydrazine hydrate. a good yield of Schiff bases was isolated by a reaction equimolar quantity of nicotinoyl hydrazine with several aromatic aldehydes. Up on Schiff bases acylation, heterocyclic compounds were collected, and synthetic derivatives were identified using Infra-Red (IR), Hydrogen Nuclear Magnetic Resonance ( 1 HNMR). The methyl thiazolyl tetrazolium (MTT) Method was used for the Evolution of anti-cancer activity. Well diffusion method over agar was used to determine antibacterial activity, gram-positive and gram-negative bacteria were used to test the strength of inhibition for synthesis derivatives. Results: a white solid of nicotinoyl hydrazine was isolated, different Schiff bases were separated in a high yield, and 1,3,4oxadiazole analogues were collected. The inhibition values of the prepared derivatives towards bacterial growth were measured. Cytotoxicity was an accounted for Schiff bases and 1,3,4-oxadiazole analogues. Conclusion: Three oxadiazole heterocyclic compounds show moderate activity. In contrast, two showed excellent inhibition toward cancer cell and bacteria growth greatly depending on the type and position of substituent groups in different hetero cyclic compounds.

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Pyrazole appended hetero-hybrids: Bioisosteric design, synthesis, in silico and in vitro antibacterial and anti-inflammatory evaluations

Anjali

Sangeetha

Nithya

et al. 2023

Journal of Molecular Structure

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A New Series of 1,3,4-Oxadiazole Linked Quinolinyl-Pyrazole/Isoxazole Derivatives: Synthesis and Biological Activity Evaluation

Cited by 5 publications

References 26 publications

Anomaly of Pyrano[2,3‐c]pyrazole Synthesis towards Pyrazolyl‐aryl‐methyl‐malononitrile Derivatives and Their Antimicrobial Activity

Anomaly of Pyrano[2,3‐c]pyrazole Synthesis towards Pyrazolyl‐aryl‐methyl‐malononitrile Derivatives and Their Antimicrobial Activity

Synthesis, Evolution Anticancer and Microbial Activity of Some 1,3,4-Oxadiazoles Analogues

Pyrazole appended hetero-hybrids: Bioisosteric design, synthesis, in silico and in vitro antibacterial and anti-inflammatory evaluations

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