Lesetja J. Legoabe
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View article: Synthesis of pyrazolyl acrylamide-chalcone conjugates with sub-micromolar antitrypanosomal activities
Synthesis of pyrazolyl acrylamide-chalcone conjugates with sub-micromolar antitrypanosomal activities Open
A series of compounds was synthesized in 3 steps and studied for their activity against Trypanosoma brucei, the causative agent of human African trypanosomiasis. These compounds were also evaluated for their cytotoxicity against the HEK293…
View article: Synthesis and in vitro anti-trypanosomal evaluation of quinolone hydrazide analogues
Synthesis and in vitro anti-trypanosomal evaluation of quinolone hydrazide analogues Open
African trypanosomiasis is a major health threat to humans and animals in 36 countries within sub-Saharan Africa. We previously identified quinolone hydrazides exhibiting sub-micromolar anti-trypanosomal activity. However, the most potent …
View article: Synthesis of Pyrazolyl Acrylamide-Chalcone Conjugates with Sub-Micromolar Antitrypanosomal Activities
Synthesis of Pyrazolyl Acrylamide-Chalcone Conjugates with Sub-Micromolar Antitrypanosomal Activities Open
A series of compounds was synthesized in 4-5 steps and studied for their activity against Trypanosoma brucei, the causative agent of human African trypanosomiasis. These compounds were also evaluated for their cytotoxicity against the HEK2…
View article: Nitroimidazole scaffold: a potential panacea for infectious diseases—a review
Nitroimidazole scaffold: a potential panacea for infectious diseases—a review Open
Nitroimidazoles are five-membered heterocyclic ring systems in which the ‘’nitro’’ group is appended to either carbon 2 (benznidazole), 4 (pretomanid) or 5 (fexinidazole) of the imidazole ring. This compound class has shown broad pharmacol…
View article: 6-Phenoxyl-4-aminoquinoline: synthesis and preliminary antitubercular-structure activity relationship analyses
6-Phenoxyl-4-aminoquinoline: synthesis and preliminary antitubercular-structure activity relationship analyses Open
Diphenyl ether and quinoline based compounds have been reported to show antibacterial activity. Against Mycobacterium tuberculosis , drug targets inhibited by diphenyl ether compounds are reportedly different from those perturbed by quinol…
View article: Pyrazolyl amide-chalcones conjugates: Synthesis and antikinetoplastid activity
Pyrazolyl amide-chalcones conjugates: Synthesis and antikinetoplastid activity Open
A series of novel pyrazolyl amide-chalcones conjugates was synthesized in five steps and evaluated against a range of medically important kinetoplastid parasites including Trypanosoma cruzi , Trypanosoma brucei brucei , Trypanosoma brucei …
View article: Hydrazinated geraniol derivatives as potential broad‐spectrum antiprotozoal agents
Hydrazinated geraniol derivatives as potential broad‐spectrum antiprotozoal agents Open
Geraniol, a primary component of several essential oils, has been associated with broad‐spectrum antiprotozoal activities, although moderate to weak. This study primarily concentrated on the synthesis of hydrazinated geraniol derivatives a…
View article: Synthesis and in vitro biological activity of chalcone derivatives as potential antiparasitic agents
Synthesis and in vitro biological activity of chalcone derivatives as potential antiparasitic agents Open
Kinetoplastids are a group of flagellated protozoans including medically important parasites of the genus Trypanosoma and Leishmania . The corresponding diseases have afflicted humans for centuries. In an effort to combat kinetoplastid inf…
View article: Synthesis and In Vitro Antibacterial Evaluation of Mannich Base Nitrothiazole Derivatives
Synthesis and In Vitro Antibacterial Evaluation of Mannich Base Nitrothiazole Derivatives Open
Nitrothiazole derivatives have been reported to exhibit activity against aerobic, anaerobic, and microaerophilic bacteria. This activity profile makes the nitrothiazole compound class an ideal lead source against Mycobacterium tuberculosis…
View article: Novel quinoline derivatives with broad‐spectrum antiprotozoal activities
Novel quinoline derivatives with broad‐spectrum antiprotozoal activities Open
Several quinoline derivatives incorporating arylnitro and aminochalcone moieties were synthesized and evaluated in vitro against a broad panel of trypanosomatid protozoan parasites responsible for sleeping sickness ( Trypanosoma brucei rho…
View article: Tractable Quinolone Hydrazides Exhibiting Sub‐Micromolar and Broad Spectrum Antitrypanosomal Activities
Tractable Quinolone Hydrazides Exhibiting Sub‐Micromolar and Broad Spectrum Antitrypanosomal Activities Open
Nagana and Human African Trypanosomiasis (HAT), caused by (sub)species of Trypanosoma , are diseases that impede human and animal health, and economic growth in Africa. The few drugs available have drawbacks including suboptimal efficacy, …
View article: A scoping review on efficacy and safety of medicinal plants used for the treatment of diarrhea in sub-Saharan Africa
A scoping review on efficacy and safety of medicinal plants used for the treatment of diarrhea in sub-Saharan Africa Open
View article: Design and synthesis of imidazo[1,2‐<i>a</i>]pyridine‐chalcone conjugates as antikinetoplastid agents
Design and synthesis of imidazo[1,2‐<i>a</i>]pyridine‐chalcone conjugates as antikinetoplastid agents Open
A library of imidazo[1,2‐a]pyridine‐appended chalcones were synthesized and characterized using 1 H NMR, 13 C NMR and HRMS. The synthesized analogues were screened for their antikinetoplastid activity against Trypanosoma cruzi , Trypanosom…
View article: 2‐Aroyl quinazolinone: Synthesis and in vitro anti‐parasitic activity
2‐Aroyl quinazolinone: Synthesis and in vitro anti‐parasitic activity Open
Trypanosomes and Leishmania are parasitic protozoans that affect millions of people globally. Herein we report the synthesis of 2‐aroyl quinazolinones and their antiprotozoal efficacy against Trypanosoma brucei , Trypanosoma brucei rhodesi…
View article: Steroid-triazole conjugates: A brief overview of synthesis and their application as anticancer agents
Steroid-triazole conjugates: A brief overview of synthesis and their application as anticancer agents Open
Steroids are biomolecules that play pivotal roles in various physiological and drug discovery processes. Abundant research has been fuelled towards steroid-heterocycles conjugates over the last few decades as potential therapeutic agents a…
View article: Quinolone analogues of benzothiazinone: Synthesis, antitubercular structure-activity relationship and ADME profiling
Quinolone analogues of benzothiazinone: Synthesis, antitubercular structure-activity relationship and ADME profiling Open
Mycobacterium tuberculosis (Mtb) has an impermeable cell wall which gives it an inherent ability to resist many antibiotics. DprE1, an essential enzyme in Mtb cell wall synthesis, has been validated as a target for several TB drug candidat…
View article: Striatal adenosine A2A receptor involvement in normal and large nest building deer mice: Perspectives on compulsivity and anxiety
Striatal adenosine A2A receptor involvement in normal and large nest building deer mice: Perspectives on compulsivity and anxiety Open
Obsessive-compulsive disorder (OCD) is characterized by recurring obsessive thoughts and repetitive behaviors that are often associated with anxiety and perturbations in cortico-striatal signaling. Given the suboptimal response of OCD to c…
View article: Quinolone-3-amidoalkanol: A New Class of Potent and Broad-Spectrum Antimicrobial Agent
Quinolone-3-amidoalkanol: A New Class of Potent and Broad-Spectrum Antimicrobial Agent Open
Herein, we describe 39 novel quinolone compounds bearing a hydrophilic amine chain and varied substituted benzyloxy units. These compounds demonstrate broad-spectrum activities against acid-fast bacterium, Gram-positive and -negative bacte…
View article: Striatal Adenosine A2A Receptor Involvement in Normal and Large Nest Building Deer Mice: Perspectives on Compulsivity and Anxiety
Striatal Adenosine A2A Receptor Involvement in Normal and Large Nest Building Deer Mice: Perspectives on Compulsivity and Anxiety Open
View article: Quinolone: a versatile therapeutic compound class
Quinolone: a versatile therapeutic compound class Open
View article: Plants’ bioactive secondary metabolites in the management of sepsis: Recent findings on their mechanism of action
Plants’ bioactive secondary metabolites in the management of sepsis: Recent findings on their mechanism of action Open
Sepsis is a severe inflammatory response to systemic infection and is a threatening cause of death in intensive care units. In recent years, a number of studies have been conducted on the protective effect of natural products against sepsi…
View article: Synthesis and in vitro antiprotozoal evaluation of novel metronidazole–Schiff base hybrids
Synthesis and in vitro antiprotozoal evaluation of novel metronidazole–Schiff base hybrids Open
Herein we report the synthesis of 21 novel small molecules inspired by metronidazole and Schiff base compounds. The compounds were evaluated against Trichomonas vaginalis and cross‐screened against other pathogenic protozoans of clinical r…
View article: Arylnitro monocarbonyl curcumin analogues: Synthesis and in vitro antitubercular evaluation
Arylnitro monocarbonyl curcumin analogues: Synthesis and in vitro antitubercular evaluation Open
Curcumin is a natural product that has been reported to exhibit myriad pharmacological properties, one of which is antitubercular activity. It demonstrates antitubercular activity by directly inhibiting Mycobacterium tuberculosis (M.tb) an…
View article: Nigella sativa L. and Its Active Compound Thymoquinone in the Clinical Management of Diabetes: A Systematic Review
Nigella sativa L. and Its Active Compound Thymoquinone in the Clinical Management of Diabetes: A Systematic Review Open
Despite existing conventional hypoglycemic drugs to manage diabetes, their non-availability and cost in low-income countries coupled with the associated side effects remain a major concern. Consequently, exploring for alternative treatment…
View article: Dual production of solar energy and important plant-derived active pharmaceutical ingredients: Artemisinin, a pilot study
Dual production of solar energy and important plant-derived active pharmaceutical ingredients: Artemisinin, a pilot study Open
Agrophotovoltaics is a relatively new field of research where land is used for the production of both solar energy and various suitable (food) crops. Due to persistent rolling blackouts in South Africa, and a dire need to invest in renewab…
View article: Design, synthesis and evaluation of amino-3,5-dicyanopyridines and thieno[2,3-b]pyridines as ligands of adenosine A1 receptors for the potential treatment of epilepsy
Design, synthesis and evaluation of amino-3,5-dicyanopyridines and thieno[2,3-b]pyridines as ligands of adenosine A1 receptors for the potential treatment of epilepsy Open
Due to the implication of adenosine in seizure suppression, adenosine-based therapies such as adenosine receptor (AR) agonists have been investigated. This study aimed at investigating thieno[2,3-b]pyridine derivatives as non-nucleo…
View article: Exploration of 4-aminopyrrolo[2,3-d]pyrimidine as antitubercular agents
Exploration of 4-aminopyrrolo[2,3-d]pyrimidine as antitubercular agents Open
View article: Design, synthesis and evaluation of amino-3,5-dicyanopyryridines and thieno[2,3-b]pyridines as ligands of adenosine receptors
Design, synthesis and evaluation of amino-3,5-dicyanopyryridines and thieno[2,3-b]pyridines as ligands of adenosine receptors Open
Due to the implication of adenosine in seizure suppression, adenosine-based therapies such as adenosine receptor (AR) agonists have been investigated. This study aimed at investigating thieno[2,3- b ]pyridine derivatives as non-nucleoside …
View article: The evaluation of N-propargylamine-2-aminotetralin as an inhibitor of monoamine oxidase
The evaluation of N-propargylamine-2-aminotetralin as an inhibitor of monoamine oxidase Open
View article: Correction to: Exploration of chalcones and related heterocycle compounds as ligands of adenosine receptors: therapeutics development
Correction to: Exploration of chalcones and related heterocycle compounds as ligands of adenosine receptors: therapeutics development Open