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Histone Deacetylase: A Target for Antiproliferative and Antiprotozoal Agents

Current Medicinal Chemistry, 2001
Histone deacetylase (HDAC) and histone acetyltransferase (HAT) are enzymes that influence transcription by selectively deacetylating or acetylating the eta-amino groups of lysines located near the amino termini of core histone proteins. It is well-established that in transcriptionally active chromatin, histones generally are hyperacetylated and ...
P T, Meinke, P, Liberator
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Modes of Action of Antiprotozoal Agents

1986
There are relatively few antiprotozoal agents compared with the many antibiotics available for the treatment of bacterial infections. Similarities in host and eukaryotic parasite metabolism have made development of specific chemotherapeutic agents difficult and have necessitated the use of agents that often exhibit limited specificity for the parasite ...
Douglas L. Looker   +2 more
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New antiprotozoal agents: Their synthesis and biological evaluations

Bioorganic & Medicinal Chemistry Letters, 2013
Here we report identification of new lead compounds based on quinoline and indenoquinolines with variable side chains as antiprotozoal agents. Quinolines 32, 36 and 37 (Table 1) and indenoquinoline derivatives 14 and 23 (Table 2) inhibit the in vitro growth of the Trypanosoma cruzi, Trypanosoma brucei, Trypanosoma brucei rhodesiense subspecies and ...
Upadhayaya, Ram Shankar   +3 more
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Dicationic biphenyl benzimidazole derivatives as antiprotozoal agents

Bioorganic & Medicinal Chemistry, 2004
A series of biphenyl benzimidazoles diamidines 6a-i were synthesized from their respective diamidoximes, through the bis-O-acetoxyamidoxime followed by hydrogenation in glacial acetic acid/ethanol in the presence of Pd-C. The target compounds contain hydroxy and/or methoxy substituted 1,3-phenyl groups as the central spacer between the two amidino ...
Mohamed A, Ismail   +5 more
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Assessing Antiprotozoal Agents

2009
Nitrogen metabolism in the rumen affects both the efficiency of ruminant production and the environmental impact of excreta from ruminant livestock production. Inefficient N retention by rumen microorganisms is compensated in production terms by feeding excessive amounts of dietary protein to the animal to meet required output levels.
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Novel Hydrophilic Riminophenazines as Potent Antiprotozoal Agents

ChemMedChem, 2019
AbstractSAR studies on a set of novel hydrophilic C‐2 aminopyridinyl riminophenazines bearing variously functionalized basic side chains at C‐3 were conducted. The novel compounds were evaluated for in vitro activity against two different species of Leishmania promastigotes, intramacrophage Leishmania amastigotes, chloroquine‐sensitive and chloroquine ...
Ivan Bassanini   +3 more
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Antifungal, antiprotozoal and antiviral agents

1989
In addition to bacterial disease many infections are caused by fungi, viruses and protozoa. Chemotherapy of these infections has been somewhat neglected because of the difficulty in designing safe and selective agents, but in recent years chemical ingenuity has led to some major breakthroughs.
T. J. Franklin, G. A. Snow
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Antiprotozoal and Anthelmintic Agents

2011
Since combination chemotherapy is becoming normal practice in the management of parasitic disease there have been predictions of a vast array of potential interactions caused by drug classes sharing common routes of elimination. This chapter reviews the key interactions likely to occur or those that have been seen to occur when drugs are administered ...
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ChemInform Abstract: New Antiprotozoal Agents.

Chemischer Informationsdienst, 1976
AbstractDie Nitro‐Derivate (IV), (V) und (VI) von Diimidazo‐ [1,2‐a; 2′,l ′‐c]pyrazin und Diimidazol [1,2‐a; 2′, l′‐c][1,4]diazepin werden dargestellt und gegen Trichomonas vaginalis, Entamoeba histolytica und Giardia muris getestet.
PIERO MELLONI   +7 more
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Structure−Activity Study of Pentamidine Analogues as Antiprotozoal Agents

Journal of Medicinal Chemistry, 2009
Diamidine 1 (pentamidine) and 65 analogues (2-66) have been tested for in vitro antiprotozoal activities against Trypanosoma brucei rhodesiense, Plasmodium falciparum, and Leishmania donovani, and for cytotoxicity against mammalian cells. Dications 32, 64, and 66 exhibited antitrypanosomal potencies equal or greater than melarsoprol (IC(50) = 4 nM ...
Bakunova, S. M.   +11 more
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