Browsing Faculty of Health Sciences by Title
Now showing items 2147-2166 of 2377
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The synthesis and evaluation of C7-substituted α-tetralone derivatives as inhibitors of monoamine oxidase
(Wiley, 2015)Based on a previous report that α-tetralone (3,4-dihydro-2H-naphthalen-1-one) is a promising scaffold for the design of highly potent inhibitors of the enzyme, monoamine oxidase, the present study investigates the monoamine ... -
Synthesis and evaluation of chromone derivatives as inhibitors of monoamine oxidase
(Springer, 2019)Based on reports that chromone compounds are good potency inhibitors of monoamine oxidase (MAO), the present study evaluates the effect of substitution with flexible side chains on the 3 position on MAO inhibition potency. ... -
Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents
(Elsevier, 2011)A series of fluorescent heterocyclic adamantane amines were synthesised with the goal to develop novel fluorescent ligands for neurological assay development. These derivatives demonstrated multifunctional neuroprotective ... -
Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy
(Elsevier, 2012)Malaria and HIV are among the most important global health problems of our time and together are responsible for approximately 3 million deaths annually. These two diseases overlap in many regions of the world including ... -
Synthesis and evaluation of methoxy substituted 2-benzoyl-1-benzofuran derivatives as lead compounds for the development adenosine A1 and/or A2A receptor antagonists
(Elsevier, 2020)A series of fourteen methoxy substituted 2-benzoyl-1-benzofuran derivatives were synthesised and their affinities determined for adenosine A1 and A2A receptors via radioligand binding assays to establish the structure ... -
The synthesis and evaluation of sesamol and benzodioxane derivatives as inhibitors of monoamine oxidase
(Elsevier, 2015)In the present study, series of eight sesamol (1,3-benzodioxol-5-ol) and eight benzodioxane (2,3-dihydro-1,4-benzodioxine) derivatives were synthesised and evaluated as inhibitors of recombinant human monoamine oxidase ... -
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 ...