Novel synthesis of phthalazine derivatives as antimicrobial agents

Issac, Yvette A.; El-Karim, Eman; Donia, S.A.Abou; Behalow, Mohamed

doi:10.1080/02786110213977

Cited by 19 publications

(14 citation statements)

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“…The key precursor 1-hydrazino-4-phenoxathiin-2-yl-phthalazine (1) was prepared in high yield upon refluxing equimolar amounts of 1-chloro-4-phenoxathiin-2-yl-phthalazine 10 and hydrazine hydrate in ethanol.…”

Section: Resultsmentioning

confidence: 99%

Synthesis of S-triazolo[3, 4a] phthalazine and Related Polynuclear Heterocyclic Systems

Aly

El-karim

2005

Phosphorus, Sulfur, and Silicon and the Related Elements

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The applicability and synthetic potency of the novel reagent 1-hydrazinophthalazine 1 to develop an expeditious convenient synthetic route via the annelation reactions with appropriate reagents for polyfunctionally substituted triazoles, pyrazoles, tetrazoles, and polycyclic condensed systems are reported. Chemical and spectroscopic study for the structures of the newly synthesized compounds are investigated. The prepared compounds were tested in vitro for their antimicrobial activity.

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Section: Resultsmentioning

confidence: 99%

Synthesis of S-triazolo[3, 4a] phthalazine and Related Polynuclear Heterocyclic Systems

Aly

El-karim

2005

Phosphorus, Sulfur, and Silicon and the Related Elements

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“…In view of these considerations and in continuation of our research interest for the synthesis of biologically active heterocycles, [24][25][26][27] the present work proceeded with the synthesis of new heterocyclic systems including pyridazine moiety and triazole, thiazolidine, imidazolidine, oxazine, and quinazoline moieties.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of novel pyridazine derivatives as potential antimicrobial agents

Behalo

El-karim

Issac

et al. 2014

Journal of Sulfur Chemistry

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A series of novel pyridazine derivatives incorporated with triazole, thiazolidine, imidazolidine, oxazine, and quinazoline moieties was synthesized by the reaction of [6-(4-phenoxyphenyl)pyridazin-3-yloxy]acetyl isothiocyanate with variety of nucleophilic reagents. The structures of all products were confirmed and characterized by the elemental analysis and spectroscopic studies (IR, MS, 1 H NMR). Also, the products were investigated for their antibacterial and antifungal activities and were compared with the standard drugs. Most of the synthesized compounds demonstrated potent to weak antimicrobial activity.

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“…Phthalazine derivatives were announced to acquire anticonvulsant , antitumor , antihypertensive, antithrombotic , antidiabetic , antitrypanosomal , anti‐inflammatory , cardiotonic , and vasorelaxant activities. Therefore, various strategies have been accounted for the synthesis of phthalazine derivatives . Regardless of the detailed manufactured strategies, the development of innovative proficient synthesis of phthalazine derivatives is considered an exciting trial ; the newest of O ‐substituted‐4‐benzylphthalazin‐1‐ol possessing different alkyl groups bound via acetyl‐flexible linker as anticancer agents was synthesized by incorporation of methylene (CH 2 ) domains bridge at C‐4 position of the phthalazine moiety to afford a litheness that increase their anticancer activity against three human tumor cells .…”

Section: Introductionmentioning

confidence: 99%

Design, Regiospecific Green Synthesis, Chemical Computational Analysis, and Antimicrobial Evaluation of Novel Phthalazine Heterocycles

Rizk

Abdelwahab

El‐Badawy

2019

Journal of Heterocyclic Chem

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Phthalazines have received considerable attention for their wide antimicrobial activity. Regiospecific nucleophilic attack of 4‐benzylphthalazin‐1‐ol by the 1‐oxo rather than the aza group on different alkyl halides gave novel phthalazine heterocyclic derivatives. Moreover, a variety of nucleosides bonded to electron‐withdrawing groups were synthesized using 4‐benzylphthalazine‐1‐ol. The density functional theory has been used to investigate the electronic structure of the synthesized compounds. All of the synthesized derivatives showed remarkable activity when tested against Gram‐positive and Gram‐negative bacteria, Aspergillus niger, and Candida albicans. The reactivity of these nucleosides was expected to arise from their bonding with the lone pair of N‐atom of the macromolecules of bacteria. These bonding were expected to inhibit the enzyme by forming highly stable complex with lower highest occupied molecular orbital energy. The structures of these synthesized derivatives were established by Fourier transform infrared, 1H‐NMR, and 13C‐NMR spectroscopic evidence.

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Novel synthesis of phthalazine derivatives as antimicrobial agents

Cited by 19 publications

References 0 publications

Synthesis of S-triazolo[3, 4a] phthalazine and Related Polynuclear Heterocyclic Systems

Synthesis of S-triazolo[3, 4a] phthalazine and Related Polynuclear Heterocyclic Systems

Synthesis of novel pyridazine derivatives as potential antimicrobial agents

Design, Regiospecific Green Synthesis, Chemical Computational Analysis, and Antimicrobial Evaluation of Novel Phthalazine Heterocycles

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