A5105181052- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Synthetic Organic Chemistry Methods
- Chemical Synthesis and Analysis
- Asymmetric Synthesis and Catalysis
- Synthesis and Catalytic Reactions
- Synthesis and Characterization of Pyrroles
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and biological activity
- Tuberculosis Research and Epidemiology
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Quinazolinone synthesis and applications
- Crystal structures of chemical compounds
- Synthesis and Reactivity of Heterocycles
- Chemical synthesis and pharmacological studies
- Cyclopropane Reaction Mechanisms
- Synthesis and Reactions of Organic Compounds
- Carbohydrate Chemistry and Synthesis
- Advanced Synthetic Organic Chemistry
- Inorganic and Organometallic Chemistry
- Cancer therapeutics and mechanisms
- Radiopharmaceutical Chemistry and Applications
- Trypanosoma species research and implications
- Malaria Research and Control
- Multicomponent Synthesis of Heterocycles
University of the Witwatersrand
2006-2024
iThemba Laboratory
2012-2016
Paragon (Greece)
2015
Visceral leishmaniasis is a severe parasitic disease that one of the most neglected tropical diseases. Treatment options are limited, and there an urgent need for new therapeutic agents. Following HTS campaign hit optimization, novel series amino-pyrazole ureas has been identified with potent in vitro antileishmanial activity. Furthermore, compound 26 shows high levels vivo efficacy (>90%) against Leishmania infantum, thus demonstrating proof concept this series.
Abstract Several N ‐ethoxycarbonylmethyl enaminones, prepared by Eschenmoser sulfide contraction between ‐(ethoxycarbonylmethyl)pyrrolidine‐2‐thione and various ortho ‐oxygenated phenacyl halides, underwent cyclisation to give ethyl 6‐aryl‐2,3‐dihydro‐1 H ‐pyrrolizine‐5‐carboxylates upon microwave heating with silica gel in xylene. With enaminones made from ‐hydroxyphenacyl not only did dihydropyrrolizine formation take place, but spontaneous lactonisation also occurred...
An enantiopure β-lactam with a suitably disposed electron withdrawing group on nitrogen, participated in π-allylpalladium mediated reaction 2,6-dichloropurine tetrabutylammonium salt to afford an advanced cis-1,4-substituted cyclopentenoid both high regio- and stereoselectivity. This intermediate was successfully manipulated the total synthesis of (-)-Abacavir.
Triage of a set antimalaria hit compounds, identified through high throughput screening against the Chloroquine sensitive (3D7) and resistant (Dd2) parasite Plasmodium falciparum strains several novel chemotypes suitable for hit-to-lead chemistry investigation. The was further refined investigation their in vitro ADME properties, which templates with good potential to be developed as antimalarial agents. One example profiled an vivo murine berghei model malaria infection.
Three intermediates along the reaction path by which 3‐[2‐(2‐oxo‐2‐phenylethyl)‐1‐pyrrolidinyl]propanenitrile is converted into rel ‐(7 R ,8a )‐ and (7 S )‐diastereoisomers of 7‐phenyl‐1,2,3,7,8,8a‐hexahydroindolizine‐6‐carbonitrile upon treatment with potassium tert ‐butoxide were isolated characterized. They include ‐(6 ,7 (6 7‐hydroxy‐7‐phenyloctahydroindolizine‐6‐carbonitrile (the former obtained as a monohydrate), 7‐phenyl‐1,2,3,5,8,8a‐hexahydroindolizine‐6‐carbonitrile. The alcohol...
A wide range of N -(ethoxycarbonylmethyl)enaminones, prepared by the Eschenmoser sulfide contraction between -(ethoxycarbonylmethyl)pyrrolidine-2-thione and various bromomethyl aryl heteroaryl ketones, underwent cyclization in presence silica gel to give ethyl 6-(hetero)aryl-2,3-dihydro-1 H -pyrrolizine-5-carboxylates within minutes upon microwave heating xylene at 150 °C. Instead functioning as a nucleophile, enaminone acted an electrophile its carbonyl group during cyclization. Yields...
Abstract This paper describes a five‐step synthesis of carbon‐14‐labelled pyrazole compound (11). A total 2.96 MBq 11 was obtained with the specific activity 2242.4 MBq/mmol. The radiochemical purity >99%, and overall yield 60% based on [ 14 C 6 ] 4‐bromoaniline starting material. Biodistribution results showed that radiotracer (administrated orally) has high accumulation in small intestine, large intestine liver both non‐infected tuberculosis (TB)‐infected mice. Therefore, this suggests...
Abstract For see ChemInform in Full Text.
The title compound, C20H19NO5S2, crystallizes as an almost 2:1 mixture of two molecular orientations (described Orient-A and Orient-B). consequences these is the formation three types N—H⋯O hydrogen-bonded dimers in which (Orient-A + Orient-A) are likely to be most stable, while mixed Orient-B) more frequent. Extra interactions form C—H⋯O C—H⋯π act further stabilize probably allow less energetically favourable (Orient-B exist by preventing their conversion Orient-A)-only during...
The crystal structure of the title compound, C23H28Br4O6, confirms that it consists two hexasubstituted aromatic units linked by a central methylene group. molecule lies on crystallographic twofold axis passes through bridging atom. Examination extended reveals presence ribbons molecules held together C—H⋯O and C—H⋯Br interactions.
Abstract Metathesis of (X) and (XI) proceeds only under the microwave‐assisted conditions.