Synthesis and pharmacological evaluation of isoxazole derivatives containing 1,2,4-triazole Moiety

Khanage, Shantaram Gajanan

doi:10.12991/201216411

Cited by 19 publications

(10 citation statements)

References 13 publications

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“…In the next step reaction of compounds(I) a-b with ethyl acetoacetate this reaction known as (Robinson annulations) lead to formation of cyclohexenone derivatives (II) a-d , Scheme-3 explain this mechanism [32]. The FT-IR spectrum, Figure- Finally, The thioxo pyrimidine derivatives (IV) a-b were synthesized by reaction of (I) a-d with thiourea this reaction was catalytic by NaOH , the reaction mechanism for synthesis of thioxo pyrimidine was explained in Scheme-5 [33] . FT-IR, Figure-6, showed strong absorption band in the region (1654-1625)cm -1 for υ C=N of thioxo pyrimidine ring and υNH at 3213 in addition the υC=S band appeared around 1250 cm -1 , Moreover the 1 HNMR spectrum of (IV) c Figure-8 showed the appearance of the singlet signal at the δ 3.75 ppm which was attributed to one proton of SH.…”

Section: Resultsmentioning

confidence: 99%

Synthesis and Characterization of Indazol-3-one and Thioxo Pyrimidines Derivatives from Mono and Twin Chalcones

Ghali

Tomma

2017

ijs

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This work involved synthesis and characterization of new mono and twin fused pyrazolone(indazol-3-one) (IV) a-d and thioxo pyrimidine (III) a-d derivatives from Chalcones (mono(I) a,b and twin(I) c,d ) The synthesis of mono chalcones (I) a,b includes the reaction of (p-methoxy or p-methyl) benzaldehyde with 4-amino acetophenone while the twin acetophenone with p-methoxy benzaldehyde to produce twin chalcones (I) c,d , then converted it by Robinson annulations reaction to form the corresponding derivatives (II) a-d afterward reflux the cyclohexenones with hydrazine and some drops of GAA lead to form indazole derivatives (IV) a-d . Pyrimidines were synthesized via the reaction of chalcones with thiourea in NaOH and 80% ethanol. All these compounds are characterized by FT-IR spectroscopy and some of them by 1 HNMR spectroscopy.

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Section: Resultsmentioning

confidence: 99%

Synthesis and Characterization of Indazol-3-one and Thioxo Pyrimidines Derivatives from Mono and Twin Chalcones

Ghali

Tomma

2017

ijs

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“…In addition, 1,2,4-triazole derivatives are low-toxic, rather simple in synthesis and highly reactive substances. It allows to introduce various pharmacophore fragments into their structure (Khanage et al, 2012). Our analysis of the scientific literature has shown that despite a large number of publications devoted to functional derivatives of 1,2,4-triazole the pharmacological potential of this class of compounds at the present stage is not exhausted.…”

Section: Prediction Of the Antiinflammatory Activity Of New S-alkyl Dmentioning

confidence: 99%

Prediction of the Antiinflammatory Activity of New S-alkyl Derivatives of 1,2,4-triazol-3-thiones Using the PASS Computer Program and Molecular Docking

et al. 2020

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The strategy of rational approaches to the search for selective COX-2 inhibitors as potential antiinflammatory agents has been proposed and elaborated. It is based on the use of PASS-prediction and molecular docking. The choice of the basic structure of 4-amino-3-thio-1,2,4-triazole as a promising object of chemical modification has been substantiated. Using a modification of the primary molecule, a virtual library of S-derivatives of 5-substituted 4-amino(pyrrol)3-thio-4H-1,2,4-triazoles in the amount of 100 compounds (ten groups) has been obtained by introducing various pharmacophore fragments. Based on the analysis of the results of the PASS-prediction and molecular docking, six of the ten planned groups of compounds have been selected for the synthesis as promising selective COX-2 inhibitors. The reliability of the prediction results has already been confirmed for one of the promising group 4-amino-5-(pyridine-4-yl)-1,2,4-triazole (4?)-3-yl-thioacetamides.

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“…Compound 116, 117, 118, 123 and 125 were found to be most potent molecules among the series. The electron withdrawing groups substituted phenyl ring at sixth position of dihydropyrimidine shows marked increase in their anticonvulsant activity [61].…”

Section: Anticonvulsant Activitymentioning

confidence: 99%

Recent synthetic and medicinal perspectives of dihydropyrimidinones: A review

Kaur

Chaudhary

Kumar

et al. 2017

European Journal of Medicinal Chemistry

249

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Dihydropyrimidines are the most important heterocyclic ring systems which play an important role in the synthesis of DNA and RNA. Synthetically they were synthesized using Multi-component reactions like Biginelli reaction and Hantzschdihydropyridine. In the past decades, such Biginelli type dihydropyrimidones have received a considerable amount of attention due to the interesting pharmacological properties associated with this heterocyclic scaffold. In this review, we highlight recent developments in this area, with a focus on the DHPMs, recently developed as anti-inflammatory, anti-HIV, anti-tubercular, antifungal anticancer, antibacterial, antifilarial, antihyperglycemic, antihypertensive, analgesic, anti-convulsant, antioxidant, anti-TRPA1, anti-SARS, and anti-cancer activity and α binding affinity.

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Synthesis and pharmacological evaluation of isoxazole derivatives containing 1,2,4-triazole Moiety

Cited by 19 publications

References 13 publications

Synthesis and Characterization of Indazol-3-one and Thioxo Pyrimidines Derivatives from Mono and Twin Chalcones

Synthesis and Characterization of Indazol-3-one and Thioxo Pyrimidines Derivatives from Mono and Twin Chalcones

Prediction of the Antiinflammatory Activity of New S-alkyl Derivatives of 1,2,4-triazol-3-thiones Using the PASS Computer Program and Molecular Docking

Recent synthetic and medicinal perspectives of dihydropyrimidinones: A review

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