Results 111 to 120 of about 398 (143)

Tetraoxanes as Antimalarials: Harnessing the Endoperoxide

Mini-Reviews in Medicinal Chemistry, 2014
With the emergence of resistance to artemesinin, the need for new antimalarial compounds is pressing. Several research groups have made significant contributions to the exploration of the use of 1,2,4,5-tetraoxanes and 1,2,4- trioxanes as synthetic analogues of artemesinin.
Laura C, Fisher, Margaret A L, Blackie
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Deoxycholic Acid-Derived Tetraoxane Antimalarials and Antiproliferatives

Journal of Medicinal Chemistry, 2007
The synthesis of deoxycholic acid (DCA)- and cholic acid (CA)-derived mixed tetraoxanes revealed that N-(2-dimethylamino)ethyl derivatives are potent antimalarials in vitro and in vivo. The tetraoxanes presented in this paper are dual inhibitors:  besides curing mice in vivo without observed toxic effects, they kill cancer cell lines at very low ...
Terzić-Jovanović, Nataša, Opsenica, Dejan, Milić, Dragana, Tinant, Bernard, Smith, K. S., Milhous, Wilbur K., Šolaja, Bogdan   +6 more
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Synthesis and Antimalarial‐Activity Evaluation of TetraoxaneTriazine Hybrids and Spiro[piperidine‐4,3′‐tetraoxanes]

Helvetica Chimica Acta, 2012
AbstractA series of tetraoxanetriazine hybrids and spiro[piperidine‐4,3′‐tetraoxanes] have been synthesized, and all the compounds were screened forin vitroantimalarial activity against chloroquine‐sensitive (D6) and chloroquine‐resistant (W2) strains ofPlasmodium falciparum.Most of the spiro[piperidine‐4,3′‐tetraoxanes] exhibited moderate to good ...
Nitin Kumar, Shabana I. Khan, Diwan S. Rawat   +2 more
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Tetraoxane Antimalarials and Their Reaction with Fe(II)

Journal of Medicinal Chemistry, 2006
Mixed tetraoxanes 5a and 13 synthesized from cholic acid and 4-oxocyclohexanecarboxylic acid were as active as artemisinin against chloroquine-susceptible, chloroquine-resistant, and multidrug-resistant Plasmodium falciparum strains (IC50, IC90). Most active 13 is metabolically stable in in vitro metabolism studies.
Opsenica, Igor, Terzić-Jovanović, Nataša, Opsenica, Dejan, Angelovski, Goran, Lehnig, Manfred, Eilbracht, Peter, Tinant, Bernard, Juranić, Zorica, Smith, Kirsten S., Yang, Young S., Diaz, Damaris S., Smith, Philip L., Milhous, Wilbur K., Đoković, Dejan, Šolaja, Bogdan   +14 more
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Medicinal Chemistry Perspectives of Trioxanes and Tetraoxanes

Current Medicinal Chemistry, 2011
Trioxane based compounds such as artemisinin and its synthetic and semi-synthetic analogues constitute promising class of antimalarial agents. The pharmaceutical development of artemisinin was started in 1971 after the isolation from Chinese medicinal plant Artemisia annua and this compound has drawn much attention from medical chemist and ...
N, Kumar, M, Sharma, D S, Rawat
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Antimalarial and antiproliferative evaluation of Bis-Steroidal tetraoxanes

Bioorganic & Medicinal Chemistry, 2003
Several cis and trans bis-steroidal 1,2,4,5-tetraoxanes possessing amide terminus were synthesised and evaluated as antimalarials and antiproliferatives. The compounds exhibited submicromolar antimalarial activity against Plasmodium falciparum D6 and W2 strains.
Opsenica Dejan, Angelovski Goran, Pocsfalvi Gabriella, Juranic Zorica, Zizak Zeljko, Kyle Dennis, Milhous Wilbur K, Solaja Bogdan A   +7 more
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Mixed Steroidal 1,2,4,5-Tetraoxanes:  Antimalarial and Antimycobacterial Activity

Journal of Medicinal Chemistry, 2002
Mixed 1,2,4,5-tetraoxanes possessing simple spirocycloalkane and spirocholic acid-derived substituents were prepared and shown to have significantly higher in vitro antimalarial activity than bis-substituted tetraoxanes. Out of 41 synthesized tetraoxanes, 12 were in vitro more potent against Plasmodium falciparum chloroquine-resistant W2 clone than ...
Solaja BA, Terzic N, Pocsfalvi G, Gerena L, Tinant B, Opsenica D, Milhous WK   +6 more
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Mixed tetraoxanes containing the acetone subunit as antimalarials

Bioorganic & Medicinal Chemistry, 2008
Eleven new tetraoxanes possessing cholic acid-derived carrier and isopropylidene moiety were synthesized and were tested in vitro and in vivo. In vitro screening revealed that nine of them were more potent against CQ-resistant W2 than CQ-susceptible D6 strain and that two of them were equally or more potent than artemisinin and mefloquine against multi-
Opsenica, Dejan, Terzić-Jovanović, Nataša, Smith, P.L., Yang, Y., Anova, L., Smith, K. S., Šolaja, Bogdan   +6 more
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Tetraoxane–Pyrimidine Nitrile Hybrids as Dual Stage Antimalarials

Journal of Medicinal Chemistry, 2014
The use of artemisinin or other endoperoxides in combination with other drugs is a strategy to prevent development of resistant strains of Plasmodium parasites. Our previous work demonstrated that hybrid compounds, comprising endoperoxides and vinyl sulfones, were capable of high activity profiles comparable to artemisinin and chloroquine while acting ...
Oliveira, Rudi, Guedes, Rita C., Meireles, Patrícia, Albuquerque, Inês S., Gonçalves, Lídia M., Pires, Elisabete, Bronze, Maria Rosário, Gut, Jiri, Rosenthal, Philip J., Prudêncio, Miguel, Moreira, Rui, O’Neill, Paul M., Lopes, Francisca   +12 more
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Growth and perfection of tetraoxane crystals

Journal of Crystal Growth, 1979
Tetraoxane (-CH2-O-)4 crystals grown by evaporation of solutions in acetone were examined by X-ray topography. Two types of crystals, long rod-shaped and thin plate-like, were obtained. No axial screw dislocation was observed. Dislocations with Burgers vectors 〈010〉 and 12〈110〉 were observed.
Tohru Watanabe, Kunihide Izumi
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