Recent developments in anti-Trichomonas research: An update review

Bala, Veenu; Chhonker, Yashpal S.

doi:10.1016/j.ejmech.2017.11.029

Cited by 35 publications

(36 citation statements)

References 81 publications

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“…In fact, metronidazole and its analogue, tinidazole, are the only drugs accepted by the Food and Drug Administration (FDA) to treat this infection. Both are generally effective, but alternatives should be sought to treat those patients who are hypersensitive and the infections caused by nitroimidazoles‐resistant isolates . In this regard, the trichomonicidal activity of various 5‐nitroindazole derivatives such as 3‐alkoxy‐1‐ and 2‐alkylindazoles, 3‐alkoxyindazoles, 1‐substituted indazol‐3‐ols, and 2‐substituted and fused indazolin‐3‐ones has recently been described.…”

Section: Introductionmentioning

confidence: 99%

“…Both are generally effective, but alternatives should be sought to treat those patients who are hypersensitivea nd the infections caused by nitroimidazoles-resistant isolates. [22][23][24][25]27] In this regard,t he trichomonicidal activity of various5 -nitroindazole derivatives such as 3-alkoxy-1- [12,28] and 2-alkylindazoles, [11,28] 3-alkoxyindazoles, 1-substituted indazol-3ols, and 2-substituted and fused indazolin-3-ones [29,30] has recently been described.…”

Section: Introductionmentioning

confidence: 99%

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Antichagasic, Leishmanicidal, and Trichomonacidal Activity of 2‐Benzyl‐5‐nitroindazole‐Derived Amines

et al. 2018

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Three different series of new 5-nitroindazole derivatives-1-(ω-aminoalkyl)-2-benzylindazolin-3-ones (series A; ten compounds), 3-(ω-aminoalkoxy)-2-benzylindazoles (series B; four compounds) and 3-alkylamino-2-benzylindazoles (series C; five compounds)-have been synthesized and evaluated against the protozoan parasites Trypanosoma cruzi, Leishmania amazonensis, and Trichomonas vaginalis: etiological agents of Chagas disease, cutaneous leishmaniasis, and trichomoniasis, respectively. Many indazoles of series A, B, and C were efficient against T. cruzi. Some compounds in series A, after successfully passing the preliminary screening for epimastigotes, exhibited activity values against amastigotes of several T. cruzi strains that were better than or similar to those shown by the reference drug benznidazole and displayed low nonspecific toxicity against mammalian cells. On the other hand, preliminary studies against promastigotes of L. amazonensis showed high leishmanicidal activity for some derivatives of series A and C. With regard to activity against T. vaginalis, some indazoles of series B and C were rather efficient against trophozoites of a metronidazole-sensitive isolate and showed low nonspecific toxicities toward Vero cell cultures. Additionally, some of these compounds displayed similar activity against metronidazole-sensitive and resistant isolates, showing the absence of cross-resistance between these derivatives and the reference drug.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Antichagasic, Leishmanicidal, and Trichomonacidal Activity of 2‐Benzyl‐5‐nitroindazole‐Derived Amines

et al. 2018

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“…Human trichomoniasis, caused by Trichomonas vaginalis ( T. vaginalis ), is the most common chronic nonviral infection and responsible for more than 200 million cases each year. [ 89,90 ] Isatin derivatives were reported to possess potential activity against T. vaginalis , [ 91,92 ] so dimerization of isatin may provide valuable therapeutic intervention for the treatment of human trichomoniasis.…”

Section: Antiprotozoal and Antiviral Activitymentioning

confidence: 99%

Isatin dimers and their biological activities

Zhang

Liu

et al. 2020

Archiv der Pharmazie

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Dimerization is a promising strategy to develop novel drug candidates that could extend the biological spectrum, enhance the activity, overcome drug resistance, as well as improve pharmacological, pharmacokinetic, and physicochemical profiles. Isatin dimers possess a broad spectrum of biological properties and the isatin dimer indirubin has already been used in the clinic, revealing the potential of isatin dimers as putative drugs. This review covers the recent advances of isatin dimers as pharmacologically significant scaffolds and the structure–activity relationship to set up the direction for the design and development of isatin dimers with higher efficiency and lower toxicity.

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“…Gegenstand aktueller Forschung ist die Überwindung der bestehenden Metronidazol-Resistenzen. Synthetische chemische Substanzen und Pflanzen werden aktuell erforscht, um neue Medikamente gegen Trichomonaden herzustellen [22].…”

Section: Cave Die Partnerbehandlung Ist Obligat!unclassified