New strategy for the synthesis of novel spiro[indoline-3,2'-thiazolo[5,4-e]pyrimido[1,2-a]pyrimidine] derivatives

Dandia, Anshu

doi:10.3998/ark.5550190.0010.e09

Cited by 3 publications

(1 citation statement)

References 11 publications

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“…In the context of antifungal agent development, different chitin synthase inhibitors have been synthesized by a green chemical approach. Previous researchers interest on the green chemical synthesis of biodynamic spiro and annulated derivatives [32,33] using nontraditional approach, an attempt has been made to synthesize various spiro-1,4-DHPs derivatives. A series of novel N-substituted spiro-1,4-DHPs derivatives (4a-4f) (Table 1) has been synthesizes in one pot under microwave irradiation using solvent free conditions and tested for an antidermatophytic activity [29].…”

Section: Resultsmentioning

confidence: 99%

Pharmacological importance of novel spiro derivatives against human pathogenic fungi

Sharma

Saxena

et al. 2023

BIOMED KHIM

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Human mycoses have become a threat to health world-wide. Unfortunately there are only a limited number of antimycotic drugs in use. In the present study, antifungal activity of earlier synthesized spiro-1,4-dihydropyridines (1,4-DHPs) was investigated. The antifungal activity of spiro-1,4-DHPs compounds were screened against Aspergillus flavus, A. fumigatus, and Candida albicans by using Disc Diffusion and Modified Microdilution method. Among six spiro-1,4-DHPs compounds tested all of them showed stronger antifungal activity possibly through inhibiting the synthesis of chitin in cell wall against A. flavus, A. fumigatus, and C. albicans as compared to fluconazole, a standard antifungal drug. The combination of compounds showed that the synthesized compounds had synergistic, additive effects as compared to currently used drugs as an antifungal agent. These results indicated that these designed compounds were potential chitin synthase inhibitors and had excellent antimycotic activity for the treatment of fungal infections.

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Section: Resultsmentioning

confidence: 99%

Pharmacological importance of novel spiro derivatives against human pathogenic fungi

Sharma

Saxena

et al. 2023

BIOMED KHIM

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Novel spiro[indoline-3,2′thiazolo[5,4-e]pyrimido[1,2-a] pyrimidine] derivatives as possible anti-dermatophytic and anti-candidiasis agent

Sharma,

Sharma

2024

BIOMED KHIM

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A novel series of 5′-benzylidene-3′-phenylspiro[indoline-3,2′-thiazolidine]-2,4′(1H)-diones 6a-d and spiro[indoline-3,2′-thiazolo[5,4-e]pyrimido[1,2-a]pyrimidin]-2(1H)-one 9a-d derivatives have been synthesized. All the newly synthesized compounds were evaluated for antifungal and anti-candidiasis activity by using Disc Diffusion and Modified Microdilution methods. The antimicrobial experiments have shown that the synthesized compounds demonstrated broad-spectrum antifungal activity in vitro. Among them, compounds 9a-9d had stronger antifungal activity against Trichophyton rubrum, Trichophyton mentagrophytes, and Candida albicans; compounds 6a-d also showed significant antifungal activity against selected fungal strains as compared to ketoconazole, the reference antifungal drug. The evaluation of antifungal activity against drug-resistant fungal variants showed that the designed compounds had significant antifungal activity against the tested variants. The combination of compounds (6a-d) and (9a-d) exhibited that the synthesized compounds had synergistic effects or additive effects. These results demonstrated that the synthesized compounds were putative chitin synthase inhibitors exhibiting broad spectrum antifungal activities. The present results indicate that novel spiro pyrimidine derivatives can be used as an active pharmaceutical ingredient for novel drug candidate for treatment of dermatophytosis and other fungal agents.

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Synthesis of Some New Tetracyclic Pyrimidine Derivatives Using Exocyclic α,β-Unsaturated Ketone and Evaluation of Their Antitumor Activities

El-mahdy

2016

JAC

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Thiazolopyrimidine 2 was obtained from the reaction of dihydropyrimidinone with chloroacetic acid and benzaldehyde. Thiazolopyrimidine 2 containing an α,β-unsaturated ketonic function [-CH=CH-CO-] has been used as a component of Michael addition with an equimolar amount of dinucleophiles to give a series of novel tetracyclic pyrimidine derivatives. Treatment of thiazolopyrimidine 2 with uracil, aminotriazole, cyanoacetic acid hydrazide, o-phenylenediamine or diaminopyridine afforded the corresponding pyridopyrimidine, triazolopyrimidine, pyrazolone, benzodiazepine and triazepine derivative, respectively. The detailed synthesis, spectroscopic data, and antitumor activity for synthesized compounds were reported.

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New strategy for the synthesis of novel spiro[indoline-3,2'-thiazolo[5,4-e]pyrimido[1,2-a]pyrimidine] derivatives

Cited by 3 publications

References 11 publications

Pharmacological importance of novel spiro derivatives against human pathogenic fungi

Pharmacological importance of novel spiro derivatives against human pathogenic fungi

Novel spiro[indoline-3,2′thiazolo[5,4-e]pyrimido[1,2-a] pyrimidine] derivatives as possible anti-dermatophytic and anti-candidiasis agent

Synthesis of Some New Tetracyclic Pyrimidine Derivatives Using Exocyclic α,β-Unsaturated Ketone and Evaluation of Their Antitumor Activities

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