Syntheses of 2,4,6-trisubstituted pyrimidine derivatives as a new class of antifilarial topoisomerase II inhibitors

Katiyar, Sanjay Babu; Bansal, Iti; Saxena, Jitendra Kumar; Chauhan, Prem M. S.

doi:10.1016/j.bmcl.2004.10.046

Cited by 36 publications

(7 citation statements)

References 10 publications

(9 reference statements)

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“…In similar study Ciprofloxacin was shown antifilarial activity against Brugia malayi parasite [23]. Novobiocin antibiotics also found to be active in many experiment against Brugia malayi [24,25]. These results revealed that some active molecules present in this plant extract might be responsible for the real antifilarial effect.…”

Section: Disscusionmentioning

confidence: 57%

Antifilarial activity of Butea monosperma L. leaves extracts against Setaria cervi

Deshmukh¹,

Sahare²,

Patidar³

et al. 2014

Trends Vector Res Parasitol

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Background: Usage of herbal drugs in traditional medicine is quite well known but largely empirical. Hence the present study was designed to screen the in vitro antifilarial effect of Butea monosperma L. plant leaves against Setaria cervi. Methods: Antifilarial activity of Methanol/Hexane-ethanol extracts of Butea monosperma L. (leaves) and Ciprofloxacin was explored against adult of Setaria cervi after incubation for 24 hrs with concentration range of 0.25 to 20 mg/ml for possible antifilarial effect by comparing with suitable control, in terms of motility inhibition assay and MTT reduction assay. Results: Butea monosperma L. plant leaves showed significant antifillarial activity against adult as compared to controls whereas activity demonstrated by Ciprofloxacin was comparatively less significant. Inhibitory concentrations (IC50) for the plant extracts with significant antifilarial activity against Setaria cervi adult in vitro system have been derived to be 1.25, 3.6 and 7.5 mg/ml Methanol, Hexane-ethanol extracts and Ciprofloxacin respectively. Conclusion: The present research investigation proved to be an additional frame in recording the plant extract's antifilarial activity. Methanol and Hexane-ethanol extracts of Butea monosperma L. plant leaves which shown significant antifilarial activity. The present research data highlights the importance of further depth research in this area.

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Section: Disscusionmentioning

confidence: 57%

Antifilarial activity of Butea monosperma L. leaves extracts against Setaria cervi

Deshmukh¹,

Sahare²,

Patidar³

et al. 2014

Trends Vector Res Parasitol

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“…Structure activity relationship of most active compounds have given clear indication that amino group and 4-aminophenyl group at position-2 are very crucial in exerting topoisomerase II inhibitory activity against filarial parasite Setaria cervi than standard antifilarial drug (DEC) and enzyme topoisomerase II inhibitors (novobiocin, nalidixic acid) (Table 52 , Fig. 14 ) [ 62 ].…”

Section: Biological Significance Of Pyrimidine Scaffoldsmentioning

confidence: 99%

Therapeutic potential of heterocyclic pyrimidine scaffolds

Kumar

2018

Chemistry Central Journal

148

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Heterocyclic compounds offer a high degree of structural diversity and have proven to be broadly and economically useful as therapeutic agents. Comprehensive research on diverse therapeutic potentials of heterocycles compounds has confirmed their immense significance in the pathophysiology of diseases. Heterocyclic pyrimidine nucleus, which is an essential base component of the genetic material of deoxyribonucleic acid, demonstrated various biological activities. The present review article aims to review the work reported on therapeutic potentials of pyrimidine scaffolds which are valuable for medical applications during new generation.

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“…384 Certain pyrimidines and annulated pyrimidine derivatives are also known to display anticancer, [385][386] antimalarial, 387 antileishmanial 388 and antifilarial activities. 389 Recently, novel ninhydrin-creatinine heterocyclic condensation products 345-347 were synthesized with different solvent systems (Scheme 111). 390 It was observed that in polar solvents, such as acetic acid or water, the reaction of ninhydrin 1 with creatinine 344 yields the initial condensation product 345 which is then converted into 346.…”

Section: Pyrimidinesmentioning

confidence: 99%

Ninhydrin in synthesis of heterocyclic compounds

Ziarani¹,

Lashgari²,

Azimian³

et al. 2015

Arkivoc

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Ninhydrin has been utilized in many heterocyclic preparations and considered as an important building block in organic synthesis. There is a wide range of reactions that include ninhydrin in the synthesis of heterocyclic compounds. This review highlights the advances in the use of ninhydrin as starting material in the synthesis of various organic compounds and drugs in a fully comprehensive way, from its first isolation in 1910 to the end of 2013. There is also a diversity of multi-component reactions of ninhydrin and we highlight the recent reports in this review.

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Syntheses of 2,4,6-trisubstituted pyrimidine derivatives as a new class of antifilarial topoisomerase II inhibitors

Cited by 36 publications

References 10 publications

Antifilarial activity of Butea monosperma L. leaves extracts against Setaria cervi

Antifilarial activity of Butea monosperma L. leaves extracts against Setaria cervi

Therapeutic potential of heterocyclic pyrimidine scaffolds

Ninhydrin in synthesis of heterocyclic compounds

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