Publications by authors named "Goitsemodimo H Rakodi"
Corrigendum to " antiplasmodium and antitrypanosomal activities, β-haematin formation inhibition, molecular docking and DFT computational studies of quinoline-urea-benzothiazole hybrids" [Heliyon Volume 10, Issue 19, October 2024, Article e38434].
Oluwatoba E Oyeneyin Rashmika Moodley Chakes Mashaba Larnelle F Garnie Damilola A Omoboyowa Goitsemodimo H Rakodi
Heliyon
December 2024
[This corrects the article DOI: 10.1016/j.heliyon.
View Article and Find Full Text PDFantiplasmodium and antitrypanosomal activities, β-haematin formation inhibition, molecular docking and DFT computational studies of quinoline-urea-benzothiazole hybrids.
Oluwatoba E Oyeneyin Rashmika Moodley Chakes Mashaba Larnelle F Garnie Damilola A Omoboyowa Goitsemodimo H Rakodi
Heliyon
October 2024
Article Synopsis
- Quinoline-urea-benzothiazole hybrid compounds showed promising anti-parasitic activities against the 3D7 chloroquine-sensitive strain with effective concentrations ranging from 0.33 to 0.97 μM.
- Many hybrids performed comparably to chloroquine in inhibiting β-haematin formation, with two compounds showing slightly better efficacy than chloroquine.
- Molecular docking studies indicated that some compounds had higher binding energies than known drugs like chloroquine and pentamidine, and stability was confirmed through 100 ns simulations, indicating potential for effective enzyme targeting.
Article Synopsis
- - Stigmasterol, an unsaturated phytosterol found in Rhoicissus tridentata, exhibits a range of health benefits including anti-inflammatory, anti-cancer, and neuroprotective properties, making it a valuable compound for pharmacological applications
- - Researchers synthesized eight bio-active derivatives of stigmasterol through various chemical reactions, utilizing spectroscopic methods to confirm their structures and assess their cytotoxicity against specific breast cancer cell lines
- - The synthesized derivatives demonstrated enhanced cytotoxic activity compared to the original stigmasterol, with one derivative (5,6-Epoxystigmast-22-en-3β-ol) particularly showing promising results against the tested cancer cells
A series of 25 new benzothiazole−urea−quinoline hybrid compounds were synthesized successfully via a three-step synthetic sequence involving an amidation coupling reaction as a critical step. The structures of the synthesized compounds were confirmed by routine spectroscopic tools (1H and 13C NMR and IR) and by mass spectrometry (HRMS). In vitro evaluation of these hybrid compounds for their antitubercular inhibitory activity against the Mycobacterium tuberculosis H37Rv pMSp12::GPF bioreporter strain was undertaken.
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