Browsing Faculty of Health Sciences by Title
Now showing items 2161-2180 of 2386
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Synthesis and in vitro antileishmanial efficacy of benzyl analogues of nifuroxazide
(Wiley, 2020)Leishmaniasis is a vector‐borne parasitic disease that mostly affects populations in tropical and subtropical countries. There is currently no vaccine to protect against and only a handful of drugs are available to treat ... -
Synthesis and in vitro antileishmanial efficacy of novel quinazolinone derivatives
(Wiley, 2020)Currently available drugs being used to treat leishmaniasis have several shortcomings, including high toxicity, drug administration that requires hospitalization, and the emergence of parasite resistance against clinically ... -
Synthesis and in vitro antimalarial activity of a series of bisquinoline and bispyrrolo[1,2a]quinoxaline compounds
(Elsevier, 2012)Series of bisquinolines 4e15 and bispyrrolo[1,2a]quinoxalines 16e20 containing various polyamine linkers were synthesized. The aqueous solubility and distribution coefficient were experimentally determined. The compounds ... -
Synthesis and in vitro antimycobacterial and antileishmanial activities of hydroquinone-triazole hybrids
(Springer, 2020)Infectious diseases such as tuberculosis and leishmaniasis are leading causes of human death. One of the major factors contributing to the poor control of these diseases is primarily the reduced effectiveness of the existing ... -
Synthesis and in vitro antiplasmodial activity of quinoline-ferrocene esters
(Thieme, 2011)New 4-aminoquinoline-derived esters containing the redox-active ferrocene group brought in by either ferrocenyformic or 4-ferrocenylbutanoic acids were synthesized and tested in vitro for their antiplasmodial activity. The ... -
Synthesis and in vitro biological activities of ferrocenyl-chalcone amides
(Springer, 2016)A series of aminoferrocenyl–chalcone amides 11–19 were synthesized through condensation of a carboxylic acid-functionalized chalcone 10 with ferrocenylamines, using 1,1′-carbonyldiimidazole as the coupling agent. The ... -
Synthesis and in vitro biological evaluation of aminoacridines and artemisinin-acridine hybrids
(Elsevier, 2014)During this study, 9-aminoacridine and artemisinin–acridine hybrid compounds were synthesized and the in vitro for antimalarial activity against both the chloroquine sensitive but also gametocytocidal strain (NF54), and ... -
Synthesis and in vitro biological evaluation of dihydroartemisinyl-chalcone esters
(Elsevier, 2015)A series of dihydroartemisinyl-chalcone esters were synthesized through esterification of chalcones with dihydroartemisinin (DHA). The hybrids were screened against chloroquine (CQ) sensitive (3D7) and CQ resistant (W2) ... -
Synthesis and in vitro evaluation of 2-heteroarylidene-1-tetralone derivatives as monoamine oxidase inhibitors
(Thieme, 2018)The present study investigates the human monoamine oxidase (MAO) inhibition properties of a series of twelve 2-heteroarylidene-1-tetralone derivatives. Also included are related cyclohexylmethylidene, cyclopentylmethylidene ... -
Synthesis and in vitro evaluation of pteridine analogues as monoamine oxidase B and nitric oxice synthase inhibitors
(Elsevier, 2009)Monoamine oxidase B (MAO-B) and nitric oxide synthase (NOS) have both been implicated in the pathology of neurodegenerative diseases. In an attempt to design dual-target-directed drugs that inhibit both these enzymes, a ... -
Synthesis and in vitro human skin penetration of oligo- and polymeric ethylene glycol carbonates of zidovudine and stavudine
(Thieme, 2010)In continuation of studies focusing on the transdermal delivery of antiretroviral (ARV) drugs, the skin permeation ability of synthesized homologous series of both oligomeric and polymeric ethylene glycol (PEG) carbonates ... -
Synthesis and in vitro Leishmania promastigote growth inhibition efficacy of novel 4(3H)-quinazolinone derivatives
(ARKAT USA, 2020)Molecular hybridization is an increasingly important strategy in rational drug design and development. A series of novel quinazolinone-triazole hybrids have been synthesized and their antileishmanial activity investigat ... -
Synthesis and in vitro transdermal penetration of methoxypoly(ethylene glycol) carbonate derivatives of stavudine (3TC)
(Bentham Science, 2009)The objective of this study was to synthesize derivatives of the anti-HIV drug stavudine (d4T) with more favourable physicochemical properties for transdermal delivery in an effort to increase transdermal penetration of ... -
Synthesis and structure activity relationships of chalcone based benzocycloalkanone derivatives as adenosine a 1 and/or a 2a receptor antagonists
(Thieme, 2020)Adenosine A1 and/or A2A receptor antagonists hold promise for the potential treatment of neurological conditions, such as Parkinson’s disease. Herein, a total of seventeen benzocycloalkanone derivatives were synthesised ... -
Synthesis and transdermal penetration of stavudine-5'-esters.
(Bentham Science, 2010)The aim of this study was to investigate the effects of different ester groups in position 5’ of stavudine on the transdermal penetration with and without the use of Pheroid™ as the delivery system. Six esters were prepared ... -
Synthesis and transdermal permeation of novel N4-methoxypoly(ethylene glycol) carbamates of cytarabine
(Taylor & Francis, 2010)Background: Cytarabine is a deoxycytidine analogue commonly used in the treatment of hematological malignant diseases. Its clinical utility, however, is severely limited by its short plasma half-life because of the catabolic ... -
Synthesis and transdermal properties of acetylsalicylic acid and selected esters
(Elsevier, 2006)The primary aim of this study was to determine the transdermal penetration of acetylsalicylic acid and some of its derivatives, to establish a correlation, if any, with selected physicochemical properties and to determine ... -
Synthesis of methodxypoly (ethylene glycol) carbonate prodrugs of zidovudine and penetration through human skin in vitro
(Wiley, 2009)The aim of this study was to synthesise a series of novel methoxypoly(ethylene glycol) carbonate prodrugs of the antiretroviral drug zidovudine (azidothymidine, AZT) in an attempt to enhance the physicochemical properties ... -
Synthesis, 68Ga-radiolabeling, and preliminary in vivo assessment of a depsipeptide-derived compound as a potential PET/CT infection imaging agent
(Hindawi, 2015)Noninvasive imaging is a powerful tool for early diagnosis and monitoring of various disease processes, such as infections. An alarming shortage of infection-selective radiopharmaceuticals exists for overcoming the ... -
Synthesis, antimalarial activities and cytotoxicities of amino-artemisinin-1,2-disubstituted ferrocene hybrids
(Elsevier, 2018)Artemisinin-ferrocene conjugates incorporating a 1,2-disubstituted ferrocene analogous to that embedded in ferroquine but attached via a piperazine linker to C10 of the artemisinin were prepared from the piperazine artemisinin ...