Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine

Objective: Many derivatives of pyrimidine are known for the broad-spectrum biological activities such as antimicrobial, antitumor, antibacterial, antitubercular, anti-inflammatory, and cytotoxic activity. Chalcones with an enone group show potent pharmacological activities such as antiinflammatory, antibacterial, antifungal, and antimalarial activity. A series of pyrimidines from chalcones have been synthesized and screened for anti-inflammatory and cytotoxic activity studies.Methods: Chalcones [1-(4-nitrophenyl)-3-substituted-phenylprop-2-en-1-one] were synthesized from various substituted aldehydes with 4-nitroacetophenone and cyclized with urea and glacial acetic acid to give pyrimidine derivatives [4-(4-nitrophenyl)-6-substituted-phenylpyrimidin-2-ol].Results: Anti-inflammatory and cytotoxic activity studies revealed that some of the synthesized compounds have shown significant activity.Conclusion: The observed results proved that pyrimidines are found to be interesting lead molecules for the synthesis of anti-inflammatory and cytotoxic agents

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Design, synthesis, molecular docking and cytotoxic activity of novel urea derivatives of 2-amino-3-carbomethoxythiophene

Journal of Chemical Sciences ◽

10.1007/s12039-020-01834-w ◽

2020 ◽

Vol 132 (1) ◽

Author(s):

Venugopalarao Vikram ◽

Srinivasa R Penumutchu ◽

Raviraj Vankayala ◽

Suresh Thangudu ◽

Karteek Rao Amperayani ◽

...

Keyword(s):

Molecular Docking ◽

Cytotoxic Activity ◽

Urea Derivatives ◽

Design Synthesis ◽

Derivatives Of

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Synthesis and analgesic activities of urea derivatives of α-amino-N-pyridyl benzene propanamide

European Journal of Medicinal Chemistry ◽

10.1016/0223-5234(94)90070-1 ◽

1994 ◽

Vol 29 (6) ◽

pp. 431-439 ◽

Cited By ~ 2

Author(s):

E Sartori ◽

F Camy ◽

JM Teulon ◽

F Camborde ◽

J Meignen ◽

...

Keyword(s):

Urea Derivatives ◽

Analgesic Activities ◽

Derivatives Of

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Mathematical modelling of the chemotherapy of Plasmodium falciparum malaria with artesunate: postulation of ‘dormancy’, a partial cytostatic effect of the drug, and its implication for treatment regimens

Parasitology ◽

10.1017/s0031182099006332 ◽

2000 ◽

Vol 121 (3) ◽

pp. 237-246 ◽

Cited By ~ 53

Author(s):

M. B. HOSHEN ◽

K. NA-BANGCHANG ◽

W. D. STEIN ◽

H. GINSBURG

Keyword(s):

Falciparum Malaria ◽

Antimalarial Activity ◽

Extended Period ◽

Plasmodium Falciparum Malaria ◽

Clinical Results ◽

Rational Models ◽

Treatment Regimens ◽

Therapeutic Protocol ◽

Stage Specificity ◽

Derivatives Of

Although artesunate, one of the potent derivatives of the qinghaosu family of drugs for treating falciparum malaria, is already in use in the field, its therapeutic protocol has only been developed empirically by hit-or-miss. A pharmacokinetic–pharmacodynamic (PK–PD) model, required for creating such a protocol, is not straightforward. Artesunate presents extremely fast pharmacokinetics. As a result the stage specificity of its action must be treated explicitly. Also, use of standard PK–PD modelling fails to explain the clinical results. Our PK–PD modelling of its activity leads us to the postulation of the existence of a novel effect: a small fraction of the parasites, as a result of chemotherapeutic pressure, become cytostatic, or ‘dormant’. At this stage, the parasite cycle is halted, making them unsusceptible to further dosing until wakening. This slows down the antimalarial activity of the drug, entailing either many frequent doses or an extended period of treatment and surveillance. Based on our modelling, we suggest a method for deciding on rational models of chemotherapy against falciparum malaria.

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