Synthesis and antimicrobial activity of some 2-[1-(4-oxo-3,4-dihydrophthalazine-1-yl)alkyl]-1H-isoindole-1,3(2H)-dione and their imidoxy derivatives

Salvi, Vijay Kumar; Bhambi, Dinesh; Jat, Jawahar L.; Talesara, G. L.

doi:10.3998/ark.5550190.0007.e15

Cited by 5 publications

(2 citation statements)

References 4 publications

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“…Filtered the reaction mixture, precipitate obtained was dissolved in water (200 ml) and ltered to remove any undissolved matter and this ltrate was basi ed with concentrated ammonia solution. The precipitate obtained was ltered, dried and recrystallized using ethanol: water (80:20) mixture [24]. 2.2.2.…”

Section: Methods B: Bt 2-5mentioning

confidence: 99%

Synthesis, Molecular Docking and Antimicrobial Evaluation of Some Benzothiazoles

Pawar¹,

Kale²,

Zori³

et al. 2021

Preprint

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The new series of 2-(substituted amino)-N-(6- substituted-1,3-benzothiazol-2yl) acetamide BTC(a-t) has been synthesized by appropriate synthetic route from substituted 2-amino benzothiazole. The synthesized compounds were screened experimentally for its antimicrobial property against gram positive, gram negative bacteria and fungi. Zone of inhibition and minimum inhibitory concentration of compounds was determined against selected bacterial and fungal strains. Compound BTC-j N-(6-methoxy-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide and compound BTC-r N-(6-nitro-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide found to have good antimicrobial potential. The compound BTC-j has shown good antibacterial activity against S. aureus at MIC of 12.5 µg/ml, B. subtilis at MIC of 6.25µg/ml, E. coli at MIC of 3.125µg/ml and P. aeruginosa at MIC of 6.25µg/ml. No statistical difference in antimicrobial activity of standard and test compounds was found indicating test compounds have comparable activity. Further docking study was carried out to check the probable interactions with the selected protein using V-life MDS 3.5 software. (DNA gyrase, PDB: 3G75). The dock score of compounds and antimicrobial activity found to be consistent.

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Section: Methods B: Bt 2-5mentioning

confidence: 99%

Synthesis, Molecular Docking and Antimicrobial Evaluation of Some Benzothiazoles

Pawar¹,

Kale²,

Zori³

et al. 2021

Preprint

View full text Add to dashboard Cite

show abstract

“…Phthalazine derivatives are biologically important heterocycles and are known to possess variety of biological activities such as antitumor (Fedorov et al 2014), anticonvulsant (Sun et al 2011;), anti-inflammatory (Abd alla et al 2010Liu et al 2016;Sun, Hu, et al 2010), antidiabetic (Awadallah, El-Eraky, and Saleh 2012), antihypertensive (Olmo et al 2006), muscle relaxant (Haack et al 2005) and antimicrobial (Holló et al 2014;Khalil, Berghot, and Gouda 2009;Salvi et al 2006). Phthalazine scaffold is in the core structure of many commercially available drugs (Asif 2012) like, zopolrestat, azelastine, hydralazine and budralazine, the first is antidiabetic, the second is antihistaminic while the third and the last are vasodilating.…”

Section: Introductionmentioning

confidence: 99%

Triazolophthalazine Incorporating Piperazine Derivatives: Synthesis and in Vitro Anticancer Evaluation Study

Abulkhair

2020

Al-Azhar Journal of Pharmaceutical Sciences

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Cancer remains as one of the top leading causes of death worldwide in the last decade. In an attempt to develop a potent anticancer agent, herein we are reporting the synthesis of two novel series of piperazinyltriazolophthalazines as potential anticancer agents with potential inhibitory activity against PARP-1. All the newly synthesized compounds were evaluated for their anti-proliferative activity against four human cancer cell lines namely; Hepatocellular carcinoma (HePG-2), Mammary gland breast cancer (MCF-7), Human prostate cancer (PC3) and Colorectal carcinoma (HCT-116)). The results of cytotoxicity evaluation showed that most of the synthesized compounds displayed moderate cytotoxic activity against the selected cell lines. Compound 23 showed the highest inhibitory effect followed by compound 24 against hepatocellular carcinoma (HePG2) with IC 50 values of 15.05 and 17.23 µM respectively. The same two compounds also showed moderate activity against colorectal carcinoma cell line (HCT-116) with IC 50 values of 21.93 and 24.06 µM respectively.

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Study of Various Pyridazine and Phthalazine Drugs with Diverse Therapeutical and Agrochemical Activities

Imran

Asif

2020

Russ J Bioorg Chem

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Synthesis and antimicrobial activity of some 2-[1-(4-oxo-3,4-dihydrophthalazine-1-yl)alkyl]-1H-isoindole-1,3(2H)-dione and their imidoxy derivatives

Abstract: In this study, a series of 2-[(4-substituted phthalazine-1-yl

Cited by 5 publications

References 4 publications

Synthesis, Molecular Docking and Antimicrobial Evaluation of Some Benzothiazoles

Synthesis, Molecular Docking and Antimicrobial Evaluation of Some Benzothiazoles

Triazolophthalazine Incorporating Piperazine Derivatives: Synthesis and in Vitro Anticancer Evaluation Study

Study of Various Pyridazine and Phthalazine Drugs with Diverse Therapeutical and Agrochemical Activities

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