Synthesis and In Vitro Antimicrobial, Anthelmintic and Insecticidal Activities Study of 4(4′‐Bromophenyl)‐6‐substituted‐aryl‐1‐acetyl pyrimidine‐2‐thiols

Bamnela, Rita; Shrivastava, S. P.

doi:10.1155/2010/927601

Cited by 9 publications

(2 citation statements)

References 7 publications

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“…A relationship between dependent and independent variables (biological activities and physicochemical descriptors, respectively) was resolved statistically using regression analysis [14]. Linear regression is reached by fitting a best-fit straight line to the data using the least squares method.…”

Section: Multiple Linear Regression Methodsmentioning

confidence: 99%

2d-Qsar Study on Some Novel Dihydropyrimidine-4-Carbonitrile Analogs as an Antifungal Activity

PATEL¹,

PASHA²,

Patel³

2023

Int J Pharm Pharm Sci

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Objective: The present study was designed to study the antifungal activity of Dihydropyrimidine-4-Carbonitrile analogs against the fungi Candida albicans by a 2D quantitative structure-activity relationship (QSAR) model. Methods: The pyrimidine derivatives were produced using lipophilic, electronic, and steric parameters by Quantitative Structure Activity-Relationships (QSAR). A relationship between dependent and independent variables (biological activities and physicochemical descriptors, respectively) was resolved statistically using regression analysis. The F value shows the level of statistical significance of the regression (r2) was used to report the fitness of data. The newly synthesized derivatives were evaluated for in vitro antifungal activity against Candida albicansby Nutrient agar and Seaboard dextrose agar media. Results: Multiple linear regression is a method of crucial importance, it allowed us to obtain a relation between the calculated parameters and the antifungal activity; this we can interpret the variance of the activity by contribution to the calculated descriptors. Quantitative structure-activity relationship (QSAR) model showing a significant activity-descriptors relationship accuracy of 90% (R2 ≥ 0.90) and activity prediction accuracy of 81% (R²cv = 0.81). These values prove that the model obtained is reliable. Out of the three descriptors studied; log P has minimum potency, molar refractivity has more potency and heat of formation has moderate potency. Conclusion: Important structural understanding in the pattern of potent antifungal agents by Quantitative Structure Activity-Relationships (QSAR) study. The acquired physicochemical properties (electronic, topological, and steric) show the important structural features required for antifungal activity against Candida albicans.

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Section: Multiple Linear Regression Methodsmentioning

confidence: 99%

2d-Qsar Study on Some Novel Dihydropyrimidine-4-Carbonitrile Analogs as an Antifungal Activity

PATEL¹,

PASHA²,

Patel³

2023

Int J Pharm Pharm Sci

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“…A new series of 4(4′-bromophenyl)-6-substituted aryl-1-acetylpyrimidine-2-thiol derivatives were synthesized and screened for the in vitro antimicrobial activity. The results showed that all the synthesized compounds ( 154 ) have shown significant, good to moderate antimicrobial activity due to the presence of thio group, which enhanced the respective activities with varied substituent groups, against selected pathogens [ 165 ]. Trantolo et al synthesized a series of N 6 -substituted 6-aminopyrimidines and examined the effects of substituents governing the inhibition of DNA polymerase Ι Ι Ι from B. subtilis.…”

Section: In Vitro Antimicrobial Activity Profilmentioning

confidence: 99%

Significance and Biological Importance of Pyrimidine in the Microbial World

Sharma

Chitranshi

Agarwal

2014

International Journal of Medicinal Chemistry

209

160

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Microbes are unique creatures that adapt to varying lifestyles and environment resistance in extreme or adverse conditions. The genetic architecture of microbe may bear a significant signature not only in the sequences position, but also in the lifestyle to which it is adapted. It becomes a challenge for the society to find new chemical entities which can treat microbial infections. The present review aims to focus on account of important chemical moiety, that is, pyrimidine and its various derivatives as antimicrobial agents. In the current studies we represent more than 200 pyrimidines as antimicrobial agents with different mono-, di-, tri-, and tetrasubstituted classes along with in vitro antimicrobial activities of pyrimidines derivatives which can facilitate the development of more potent and effective antimicrobial agents.

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An environment-friendly methodology for the construction of diversified bicycloacenaphtho[1,2-d]imidazole-8-thione scaffolds using spinel NiFe2O4 nanoparticles as a sustainable catalyst

2022

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Synthesis and In Vitro Antimicrobial, Anthelmintic and Insecticidal Activities Study of 4(4′‐Bromophenyl)‐6‐substituted‐aryl‐1‐acetyl pyrimidine‐2‐thiols

Cited by 9 publications

References 7 publications

2d-Qsar Study on Some Novel Dihydropyrimidine-4-Carbonitrile Analogs as an Antifungal Activity

2d-Qsar Study on Some Novel Dihydropyrimidine-4-Carbonitrile Analogs as an Antifungal Activity

Significance and Biological Importance of Pyrimidine in the Microbial World

An environment-friendly methodology for the construction of diversified bicycloacenaphtho[1,2-d]imidazole-8-thione scaffolds using spinel NiFe2O4 nanoparticles as a sustainable catalyst

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