Synthesis and in vitro antileishmanial efficacy of novel benzothiadiazine‐1,1‐dioxide derivatives

Mangwegape, Daisy K.; Zuma, Nonkululeko H.; Aucamp, Janine; N’Da, David D.

doi:10.1002/ardp.202000280

Cited by 13 publications

(14 citation statements)

References 32 publications

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“…Antipromastigote assay : The antipromastigote activity of synthesized compounds was evaluated as described previously by Mangwegape et al [47] . using L. donovani 9515 (MHOM/IN/95/9515) and L. major IR‐173 (MHOM/IR/‐173).…”

Section: In Vitro Biological Assaysmentioning

confidence: 99%

“…Cytotoxicity assay : Human embryonal kidney (HEK‐293) cells (ATCC CRL 1573) were used for basal cytotoxicity of the synthesized compounds possessing antileishmanial activity by adopting the resazurin assay, as previously described [47] …”

Section: In Vitro Biological Assaysmentioning

confidence: 99%

“…Antipromastigote assay: The antipromastigote activity of synthesized compounds was evaluated as described previously by Mangwegape et al [47] using L. donovani 9515 (MHOM/IN/95/ 9515) and L. major IR-173 (MHOM/IR/-173). All compounds were first screened for > 70 % growth inhibition at 10 μM [40] and qualifying compounds were further used for IC 50 determina-tions.…”

Section: In Vitro Biological Assaysmentioning

confidence: 99%

“…Cytotoxicity assay: Human embryonal kidney (HEK-293) cells (ATCC CRL 1573) were used for basal cytotoxicity of the synthesized compounds possessing antileishmanial activity by adopting the resazurin assay, as previously described. [47] Macrophage toxicity: Toxicity of the compounds on the differentiated host THP-1 cells were also evaluated. As mentioned, duplicate plates of differentiated THP-1 cells were prepared during the anti-amastigote assay.…”

Section: In Vitro Biological Assaysmentioning

confidence: 99%

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Synthesis, in vitro Antileishmanial Efficacy and Hit/Lead Identification of Nitrofurantoin‐Triazole Hybrids

et al. 2022

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Leishmaniasis is a vector-borne neglected parasitic infection affecting thousands of individuals, mostly among populations in low-to moderate-income developing countries. In the absence of protective vaccines, the management of the disease banks solely on chemotherapy. However, the clinical usefulness of current antileishmanial drugs is threatened by their toxicity and the emergence of multidrug-resistant strains of the causative pathogens. This emphasizes the imperative for the development of new and effective antileishmanial agents. In this regard, we synthesized and evaluated in vitro the antileishmanial activity and cytotoxicity profile of a series of nitrofurantoin-triazole hybrids. The nitrofurantoin derivative 1 featuring propargyl moiety was distinctively the most active of all, was nontoxic to human cells and possessed submicromolar cellular activity selectively directed towards the pathogens of the life threatening visceral leishmaniasis. Hence it was identified as potential antileishmanial lead for further investigation into its prospective to act as alternative to therapies.

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Section: In Vitro Biological Assaysmentioning

confidence: 99%

Section: In Vitro Biological Assaysmentioning

confidence: 99%

Section: In Vitro Biological Assaysmentioning

confidence: 99%

Section: In Vitro Biological Assaysmentioning

confidence: 99%

See 2 more Smart Citations

Synthesis, in vitro Antileishmanial Efficacy and Hit/Lead Identification of Nitrofurantoin‐Triazole Hybrids

et al. 2022

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“…The antipromastigote activity of synthesized compounds was evaluated as described previously by Mangwegape et al (2021) using three strains of L. donovani (1S (MHOM/SD/62/1S) and 9515 (MHOM/IN/95/9515)) and L. major (IR-173 [MHOM/IR/−173]). The assay method is available in the Supinfo S1.…”

Section: Antipromastigote Assaymentioning

confidence: 99%

Exploring novel nitrofuranyl sulfonohydrazides as anti‐Leishmania and anti‐cancer agents: Synthesis, in vitro efficacy and hit identification

2022

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Leishmaniasis and cancer are two deadly diseases that plague the human population. There are a limited number of drugs available for the treatment of these diseases; however, their overuse has resulted in pathogenic resistance. Recent studies have indicated the repurposing of nitro‐containing compounds to be a new avenue into finding new treatments. In this study, new nitrofuranyl sulfonohydrazide derivatives were synthesized and evaluated for their in vitro antileishmanial and anticancer activities. The analogue 2h, featuring biphenyl moiety exhibited selective (SI > 10) submicromolar activity (IC50 0.97 μM) against acute promyelocytic leukemia cells hence was identified anticancer hit. This study revealed no antileishmanial hit. However, several promising analogues were uncovered and are worthy of further structural modifications to improve their toxicity and bioactivity profiles.

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Synthesis, electrochemistry, and in vitro antileishmanial efficacy of novel ferrocenylazines

Moller

Kannigadu

Aucamp

et al. 2023

Applied Organom Chemis

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Synthesis and in vitro antileishmanial efficacy of novel benzothiadiazine‐1,1‐dioxide derivatives

Cited by 13 publications

References 32 publications

Synthesis, in vitro Antileishmanial Efficacy and Hit/Lead Identification of Nitrofurantoin‐Triazole Hybrids

Synthesis, in vitro Antileishmanial Efficacy and Hit/Lead Identification of Nitrofurantoin‐Triazole Hybrids

Exploring novel nitrofuranyl sulfonohydrazides as anti‐Leishmania and anti‐cancer agents: Synthesis, in vitro efficacy and hit identification

Synthesis, electrochemistry, and in vitro antileishmanial efficacy of novel ferrocenylazines

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