Synthetic ligustrazine based cyclohexanone and oxime analogs as Anti-Trypanosoma and Anti-Leishmanial agentes

Alkhaldi, Abdulsalam A. M.; Koning, Harry P. de; Bukhari, Syed Nasir Abbas

doi:10.1590/s2175-97902020000418997

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2023

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Cited by 2 publications

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“…We have also extensively reported on ligustrazine-based compounds in recent years due to their diverse biological properties. 20–22 In the second step, novel chalcones were used as starting materials for the synthesis of oximes, and all newly synthesized compounds were evaluated against various types of cancer cells. The most active compounds were then subjected to anticancer mechanistic studies, and some compounds were also sculpted for binding modes.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and evaluation of new chalcones and oximes as anticancer agents

Bukhari

2022

RSC Adv.

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Section: Introductionmentioning

confidence: 99%

Synthesis and evaluation of new chalcones and oximes as anticancer agents

Bukhari

2022

RSC Adv.

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Effects of Synthetic Ligustrazine-Based Chalcone Derivatives on Trypanosoma brucei brucei and Leishmania spp. Promastigotes

Alkhaldi

2023

Molecules

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Current medication therapy for leishmaniasis and trypanosomiasis remains a major challenge due to its limited efficacy, significant adverse effects, and inaccessibility. Consequently, locating affordable and effective medications is a pressing concern. Because of their easy-to-understand structure and high functionalization potential, chalcones are promising candidates for use as bioactive agents. Thirteen synthetic ligustrazine-containing chalcones were evaluated for their ability to inhibit the growth of leishmaniasis and trypanosomiasis in etiologic agents. The tetramethylpyrazine (TMP) analogue ligustrazine was chosen as the central moiety for the synthesis of these chalcone compounds. The most effective compound (EC50 = 2.59 µM) was the chalcone derivative 2c, which featured a pyrazin-2-yl amino on the ketone ring and a methyl substitution. Multiple actions were observed for certain derivatives, including 1c, 2a–c, 4b, and 5b, against all strains tested. Eflornithine served as a positive control, and three ligustrazine-based chalcone derivatives, including 1c, 2c, and 4b, had a higher relative potency. Compounds 1c and 2c are particularly efficacious; even more potent than the positive control, they are therefore promising candidates for the treatment of trypanosomiasis and leishmaniasis.

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Synthetic ligustrazine based cyclohexanone and oxime analogs as Anti-Trypanosoma and Anti-Leishmanial agentes

Cited by 2 publications

References 23 publications

Synthesis and evaluation of new chalcones and oximes as anticancer agents

Synthesis and evaluation of new chalcones and oximes as anticancer agents

Effects of Synthetic Ligustrazine-Based Chalcone Derivatives on Trypanosoma brucei brucei and Leishmania spp. Promastigotes

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