Jacobus P. Petzer
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View article: Development of Halogenated Indole-Based Chalcones as New Class of MAO-Inhibitors
Development of Halogenated Indole-Based Chalcones as New Class of MAO-Inhibitors Open
The design and synthesis of chalcones based on halogenated indole are the main topics of this investigation. Ten derivatives were synthesized by introducing halogen substitutions (F, Cl, Br) at the aromatic B ring's ortho, meta, and para p…
View article: In vitro inhibition of snake venom toxins by varespladib, marimastat, nafamostat and dimercaprol
In vitro inhibition of snake venom toxins by varespladib, marimastat, nafamostat and dimercaprol Open
Snakebite envenoming causes more than 130,000 deaths and more than 400,000 disabilities per year and has been classified as a priority Neglected Tropical Disease by the World Health Organization (WHO). While antivenom therapy remains the m…
View article: Phytochemical profiling and in silico prediction of interactions between Artemisia afra Jacq. ex-Wild, Catharanthus roseus (L.) G. Don and CYP2B6 enzyme
Phytochemical profiling and in silico prediction of interactions between Artemisia afra Jacq. ex-Wild, Catharanthus roseus (L.) G. Don and CYP2B6 enzyme Open
Understanding herb-drug interactions is important due to the increasing use of herbal medicines alongside conventional drugs. These interactions can alter the pharmacokinetic properties of drugs, potentially causing subtherapeutic effects …
View article: Assembling of phenyl substituted halogens in the C3-position of substituted isatins by mono wave assisted synthesis: development of a new class of monoamine oxidase inhibitors
Assembling of phenyl substituted halogens in the C3-position of substituted isatins by mono wave assisted synthesis: development of a new class of monoamine oxidase inhibitors Open
View article: Design, synthesis, and evaluation of benzoxathiolone derivatives as monoamine oxidase inhibitors and antibacterial agents
Design, synthesis, and evaluation of benzoxathiolone derivatives as monoamine oxidase inhibitors and antibacterial agents Open
Benzoxathiolone derivatives have in vitro activity against monoamine oxidase A (MAO-A) and MAO-B, making them potential lead compounds for the treatment of neuropsychiatric and neurodegenerative disorders. They also have antibacterial acti…
View article: Interaction of cholinesterase inhibitors with snake venom acetylcholinesterase from snake species of Southern Africa
Interaction of cholinesterase inhibitors with snake venom acetylcholinesterase from snake species of Southern Africa Open
Acetylcholinesterase (AChE) is present in the venom of Elapid snakes, except the Mambas. Although the physiological role of AChE in snake venom is uncertain, it may contribute to acute neuromuscular paralysis following envenomation. With t…
View article: The inhibition of monoamine oxidase by 2-methylbenzo[d]oxazole derivatives
The inhibition of monoamine oxidase by 2-methylbenzo[d]oxazole derivatives Open
The monoamine oxidase (MAO) enzymes metabolise neurotransmitter amines and are drug targets for the treatment of neuropsychiatric and neurodegenerative disorders. Over the past several decades, MAO inhibitors have been used as antidepressa…
View article: Naphthoquinones and tricyclic derivatives: in vitro evaluation as xanthine oxidase inhibitors
Naphthoquinones and tricyclic derivatives: in vitro evaluation as xanthine oxidase inhibitors Open
The enzyme, xanthine oxidase (XO), is a complex flavoprotein that catalyzes the sequential oxidation of hypoxanthine and xanthine to ultimately yield uric acid as the final steps in the catabolism of adenine nucleotides. In this process mo…
View article: An investigation of the monoamine oxidase inhibition properties of benzothiazole derivatives
An investigation of the monoamine oxidase inhibition properties of benzothiazole derivatives Open
Literature reports that alkyloxy substituted coumarin derivatives inhibit the monoamine oxidase (MAO) enzymes, specifically the MAO-B isoform. To further investigate this finding, the present study synthesised and evaluated a series of alk…
View article: Synthesis of 1,2,4-Oxadiazin-5(6H)-One Derivatives and Their Biological Investigation as Monoamine Oxidase Inhibitors
Synthesis of 1,2,4-Oxadiazin-5(6H)-One Derivatives and Their Biological Investigation as Monoamine Oxidase Inhibitors Open
Monoamine oxidase (MAO) plays a key role in the pathogenesis of central nervous system disorders, and MAO inhibitors have been used in the treatment of depression and Parkinson’s disease. In the search for new classes of MAO inhibitors, th…
View article: Synthesis and evaluation of 2-methylbenzothiazole derivatives as monoamine oxidase inhibitors
Synthesis and evaluation of 2-methylbenzothiazole derivatives as monoamine oxidase inhibitors Open
Neurodegenerative disorders are caused by the progressive death of neuronal cells in specific regions of the brain and spinal cord. The most common neurodegenerative disorders are Alzheimer’s disease and Parkinson’s disease. The inhibition…
View article: Synthesis and evaluation of 3-hydroxyquinolin-2(1H)-one derivatives as inhibitors of tyrosinase
Synthesis and evaluation of 3-hydroxyquinolin-2(1H)-one derivatives as inhibitors of tyrosinase Open
View article: Synthesis and Monoamine Oxidase Inhibition Properties of 4-(2-Methyloxazol-4-yl)benzenesulfonamide
Synthesis and Monoamine Oxidase Inhibition Properties of 4-(2-Methyloxazol-4-yl)benzenesulfonamide Open
4-(2-Methyloxazol-4-yl)benzenesulfonamide was synthesized by the reaction of 4-(2-bromoacetyl)benzenesulfonamide with an excess of acetamide. The compound was evaluated as a potential inhibitor of human monoamine oxidase (MAO) A and B and …
View article: Interactions of small molecule inhibitors with secreted phospholipase <scp>A<sub>2</sub></scp>: A review of the structural data
Interactions of small molecule inhibitors with secreted phospholipase <span>A<sub>2</sub></span>: A review of the structural data Open
The secreted phospholipase A 2 (sPLA 2 ) family of enzymes hydrolyzes glycerophospholipid substrates at the sn ‐2 position of the acyl ester bond. Besides their roles in the degradation of phospholipids, these enzymes also play an importan…
View article: Efficacies and ADME properties of redox active methylene blue and phenoxazine analogues for use in new antimalarial triple drug combinations with amino-artemisinins
Efficacies and ADME properties of redox active methylene blue and phenoxazine analogues for use in new antimalarial triple drug combinations with amino-artemisinins Open
Efforts to develop new artemisinin triple combination therapies effective against artemisinin-tolerant strains of Plasmodium falciparum based on rational combinations comprising artemisone or other amino-artemisinins, a redox active drug a…
View article: Indazole derivatives as novel inhibitors of monoamine oxidase and D-amino acid oxidase
Indazole derivatives as novel inhibitors of monoamine oxidase and D-amino acid oxidase Open
The monoamine oxidase (MAO) enzymes metabolize neurotransmitter amines in the peripheral and central tissues, and inhibitors of these enzymes find application in the treatment of neuropsychiatric and neurodegenerative disorders. Based on r…
View article: 4-(2-Methyloxazol-4-Yl)benzenesulfonamide
4-(2-Methyloxazol-4-Yl)benzenesulfonamide Open
4-(2-Methyloxazol-4-yl)benzenesulfonamide was synthesized by the reaction of 4-(2-bromoacetyl)benzenesulfonamide with an excess of acetamide. The obtained compound was evaluated as a potential inhibitor of human monoamine oxidase (MAO) A a…
View article: A Multitarget Approach against Neuroinflammation: Alkyl Substituted Coumarins as Inhibitors of Enzymes Involved in Neurodegeneration
A Multitarget Approach against Neuroinflammation: Alkyl Substituted Coumarins as Inhibitors of Enzymes Involved in Neurodegeneration Open
Neurodegenerative disorders (NDs) include a large range of diseases characterized by neural dysfunction with a multifactorial etiology. The most common NDs are Alzheimer’s disease and Parkinson’s disease, in which cholinergic and dopaminer…
View article: Investigation of Novel Thiazole Derivatives Bearing the Benzenesulfonamide Moiety as MAO Inhibitors with a Promising Activity Profiles
Investigation of Novel Thiazole Derivatives Bearing the Benzenesulfonamide Moiety as MAO Inhibitors with a Promising Activity Profiles Open
We have recently reported that a series of 1,3,4-oxadiazol-2-ylbenzenesulfonamides acts as potent and specific monoamine oxidase B (MAO-B) inhibitors with some compounds possessing potencies in the nanomolar range. While sulfonamide compou…
View article: In vitro and in silico antibacterial evaluation of nitrocatechol chalcone and pyrazoline derivatives
In vitro and in silico antibacterial evaluation of nitrocatechol chalcone and pyrazoline derivatives Open
The aim of this study was to determine the in vitro antibacterial activity of nitrocatechol chalcone and pyrazoline derivatives previously synthesised by our research group against Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacte…
View article: The evaluation of isatin analogues as inhibitors of monoamine oxidase
The evaluation of isatin analogues as inhibitors of monoamine oxidase Open
The small molecule, isatin, is a well‐known reversible inhibitor of the monoamine oxidase (MAO) enzymes with IC 50 values of 12.3 and 4.86 μM for MAO‐A and MAO‐B, respectively. While the interaction of isatin with MAO‐B has been characteri…
View article: Monoamine oxidase inhibition properties of 2,1-benzisoxazole derivatives
Monoamine oxidase inhibition properties of 2,1-benzisoxazole derivatives Open
Monoamine oxidase (MAO) are flavoenzymes that metabolize neurotransmitter, dietary and xenobiotic amines to their corresponding aldehydes with the production of hydrogen peroxide. Two isoforms, MAO-A and MAO-B, are expressed in humans and …
View article: Investigation of the monoamine oxidase inhibition properties of benzoxathiolone derivatives
Investigation of the monoamine oxidase inhibition properties of benzoxathiolone derivatives Open
The treatment of neuropsychiatric and neurodegenerative disorders such as depression and Parkinson’s disease represent significant challenges in healthcare. Enzymes that metabolise neurotransmitter amines are important drug targets for the…
View article: 3-(3,4-Dichlorophenyl)-5-(1H-indol-5-yl)-1,2,4-oxadiazole
3-(3,4-Dichlorophenyl)-5-(1H-indol-5-yl)-1,2,4-oxadiazole Open
3-(3,4-Dichlorophenyl)-5-(1H-indol-5-yl)-1,2,4-oxadiazole was synthesized via the condensation of 3,4-dichlorobenzamidoxime and methyl 1H-indole-5-carboxylate using a superbasic medium (NaOH/DMSO). The compound was tested as a potential in…
View article: The pterin binding site of dihydropteroate synthase (DHPS): In silico screening and in vitro antibacterial activity of existing drugs
The pterin binding site of dihydropteroate synthase (DHPS): In silico screening and in vitro antibacterial activity of existing drugs Open
Antimicrobial resistance has rendered the sulfonamide class of antibiotics obsolete. An additional binding site on the dihydropteroate synthase (DHPS) enzyme, i.e., the pterin binding site, has been shown to be a valid alternative to the w…
View article: 3-(3,4-Dichlorophenyl)-5-(1H-indol-5-yl)-1,2,4-oxadiazole
3-(3,4-Dichlorophenyl)-5-(1H-indol-5-yl)-1,2,4-oxadiazole Open
3-(3,4-Dichlorophenyl)-5-(1H-indol-5-yl)-1,2,4-oxadiazole was synthesized via the condensation of 3,4-dichlorobenzamidoxime and methyl 1H-indole-5-carboxylate using superbasic medium (NaOH/DMSO). The compound was tested as a potential inhi…
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: Coumarin-Based Dual Inhibitors of Human Carbonic Anhydrases and Monoamine Oxidases Featuring Amino Acyl and (Pseudo)-Dipeptidyl Appendages: In Vitro and Computational Studies
Coumarin-Based Dual Inhibitors of Human Carbonic Anhydrases and Monoamine Oxidases Featuring Amino Acyl and (Pseudo)-Dipeptidyl Appendages: In Vitro and Computational Studies Open
The involvement of human carbonic anhydrase (hCA) IX/XII in the pathogenesis and progression of many types of cancer is well acknowledged, and more recently human monoamine oxidases (hMAOs) A and B have been found important contributors to…
View article: Resveratrol Analogues as Dual Inhibitors of Monoamine Oxidase B and Carbonic Anhydrase VII: A New Multi-Target Combination for Neurodegenerative Diseases?
Resveratrol Analogues as Dual Inhibitors of Monoamine Oxidase B and Carbonic Anhydrase VII: A New Multi-Target Combination for Neurodegenerative Diseases? Open
Neurodegenerative diseases (NDs) are described as multifactorial and progressive syndromes with compromised cognitive and behavioral functions. The multi-target-directed ligand (MTDL) strategy is a promising paradigm in drug discovery, pot…
View article: The inhibition of monoamine oxidase by 2H-1,4-benzothiazin-3(4H)-ones
The inhibition of monoamine oxidase by 2H-1,4-benzothiazin-3(4H)-ones Open