Molecular drug design, synthesis and pharmacophore site identification of spiroheterocyclic compounds: Trypanosoma crusi inhibiting studies

Hadda, Taïbi Ben; Kerbal, Abdelali; Bennani, Brahim; Houari, Ghali Al; Daoudi, Maria; Leite, Ana Cristina Lima; Masand, Vijay H.; Jawarkar, Rahul D.; Charrouf, Zoubida

doi:10.1007/s00044-012-0010-5

Cited by 24 publications

(13 citation statements)

References 26 publications

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“…In addition, the spiroisoxazoline scaffold forms an integral part of many beneficial biologically active compounds. Indeed, spiroisoxazolines exhibit an extensive array of biological and pharmacological activities such as antiviral 13 , anticancer 14,17,18 , antimalarial 15 , antituberculosis 16 , antibacterial 17,19 and antiparasitic 20 .…”

Section: Introductionmentioning

confidence: 99%

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Synthesis of new spiroheterocycles-fused isoxazoline from 2-arylidenes-3-phenyl-1-indanones through a regio-and diastereospecific 1,3-dipolar cycloaddition

Mahfoud¹,

Kerbal²,

Nakkabi³

et al. 2021

Mediterr.J.Chem.,

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<p>New spiroisoxazolines <strong>3</strong> have been synthesized by 1,3-dipolar cycloaddition of arylnitrile oxides with 2-arylidenes-3-phenyl-1-indanones. The reaction occurs in a regiospecific and diastereospecific manner and leads to one cycloadduct in all the cases. The proposed structure of the obtained cycloadducts was established based on spectroscopic data and confirmed by radiocrystallographic study. The spectral data were in favor of the observed regiochemistry and diastereoselectivity of this reaction.</p>

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Section: Introductionmentioning

confidence: 99%

“…Spiroisoxazolines synthesized in our laboratory in 2005 have been patented for their antituberculosis and anti-HIV properties 21,22 . Since then, we have been further developing these highly promising molecules 16,20 .…”

Section: Introductionmentioning

confidence: 99%

Synthesis of new spiroheterocycles-fused isoxazoline from 2-arylidenes-3-phenyl-1-indanones through a regio-and diastereospecific 1,3-dipolar cycloaddition

Mahfoud¹,

Kerbal²,

Nakkabi³

et al. 2021

Mediterr.J.Chem.,

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“…Chagas disease or sleeping sickness is a neglected disease with high occurrence in Western Africa, especially in Sub-Saharan region. The causative agent 'Trypanosoma cruzi' (T. cruzi) is a protozoan kinetoplastid parasite [1][2][3]. This parasite gets transmitted to humans by an insect of the family reduviidae, commonly known as the 'kissing bug'.…”

Section: Introductionmentioning

confidence: 99%

“…This parasite gets transmitted to humans by an insect of the family reduviidae, commonly known as the 'kissing bug'. Unfortunately, there is no vaccine, and the existing available drugs, benznidazole and nifurtimox, were discovered decades ago [1][2][3]. The recent studies suggest that these drugs are inefficient to cure the disease for all patients due to emergence of resistance, inefficacy in chronically infected subjects, higher economical burden and long treatment duration.…”

Section: Introductionmentioning

confidence: 99%

“…The recent studies suggest that these drugs are inefficient to cure the disease for all patients due to emergence of resistance, inefficacy in chronically infected subjects, higher economical burden and long treatment duration. Therefore, there is a need to develop a new drug for this disease [1][2][3]. Recently, Fleau et al [1] reported a good number of acylaminobenzothiazole derivatives as Trypanosoma cruzi inhibitors to cure Chagas disease.…”

Section: Introductionmentioning

confidence: 99%

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AcylAminoBenzothiazole Series as Inhibitors of Trypanosoma Cruzi : A Pharmacophore Modelling Approach

Parihar¹

2019

IJRASET

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Modern drug designing incorporates smart use of computer-aided techniques like QSAR, Molecular docking, pharmacophore modelling, etc. In the present work, pharmacophore modelling has been accomplished for acylaminobenzothiazole series as inhibitors of Trypanosoma cruzi. The selected dataset consists of acylaminobenzothiazole derivatives having variety of substituents. The structures were drawn, optimized (MMFF94), aligned and later used to generate a robust consensus pharmacophore model. The results indicate that aromatic rings, H-bond donor/acceptor and lipophilic moieties govern the anti-Chagas activity of selected acylaminobenzothiazole derivatives. The results could be used for future optimization of acylaminobenzothiazole derivatives as Trypanosoma cruzi inhibitors.

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Synthesis of Spiro[benzofuran‐2,2'‐benzo[b]thiophene]‐3,3'‐diones via PIDA/CuBr‐Mediated Spirocyclization

Liang

Yang

et al. 2020

Eur J Org Chem

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A phenyliodine(III) diacetate (PIDA)/CuBr‐mediated construction of the novel 3H,3'H‐spiro[benzofuran‐2,2'‐benzo[b]thiophene]‐3,3'‐dione skeleton was realized from the reaction of (Z)‐3‐hydroxy‐1‐(2‐hydroxyphenyl)‐3‐(2‐halogenphenyl)prop‐2‐en‐1‐ones with potassium ethylxanthate in the presence of 1,10‐phen. The reaction sequence was postulated to encompass a PIDA‐mediated oxidative C–O bond formation followed by a CuBr‐mediated spirocyclization step.

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Molecular drug design, synthesis and pharmacophore site identification of spiroheterocyclic compounds: Trypanosoma crusi inhibiting studies

Cited by 24 publications

References 26 publications

Synthesis of new spiroheterocycles-fused isoxazoline from 2-arylidenes-3-phenyl-1-indanones through a regio-and diastereospecific 1,3-dipolar cycloaddition

Synthesis of new spiroheterocycles-fused isoxazoline from 2-arylidenes-3-phenyl-1-indanones through a regio-and diastereospecific 1,3-dipolar cycloaddition

AcylAminoBenzothiazole Series as Inhibitors of Trypanosoma Cruzi : A Pharmacophore Modelling Approach

Synthesis of Spiro[benzofuran‐2,2'‐benzo[b]thiophene]‐3,3'‐diones via PIDA/CuBr‐Mediated Spirocyclization

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