Structural improvement of new thiazolyl-isatin derivatives produces potent and selective trypanocidal and leishmanicidal compounds

Freitas, Luiz Alberto Barros; Santos, Aline Caroline da Silva; Silva, Gedália de Cássia; Albuquerque, Franciely Nayara do Nascimento; Silva, Elis Dionísio da; Simone, C. A. De; Pereira, Valéria Rêgo Alves; Alves, Luíz Carlos; Brayner, Fábio André; Leite, Ana Cristina Lima; Gomes, Paulo André Teixeira de Moraes

doi:10.1016/j.cbi.2021.109561

Cited by 15 publications

(3 citation statements)

References 26 publications

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“…Neglected tropical diseases remain a global threat to health and thus the need for the development of new approaches and therapies to fight against these infections. Freitas et al, in 2021 [36] reported the synthesis and evaluation of the anti-parasitic properties of some isatinthiazolyl 6a-j hybrids. The hybrid 6e,h,i,j were found to be the most potent compounds with anti-Trypanosoma cruzi activity for trypomastigote form having IC50 values of 4.43 μM, 2.05 μM, 4.12 μM and 1.72 μM respectively.…”

Section: Isatin-azole Hybridsmentioning

confidence: 99%

“…There exist several isatin hybrid molecules generated by the combination of isatin moiety with other useful pharmacophores that have outstanding biological activities. Some of these hybrids include; Isatin-Azole hybrids [8][9][10]14,23,[33][34][35][36][37][38], Isatin-furan hybrids [9,18,33,35,39], Isatinthiophene hybrids [8,40], Isatin-indole hybrids [9,41], Isatin-fluoroquinolone hybrids [9,17,42], Isatin-Imine hybrids [9], Isatin-sulfonamide hybrids [2,9,21,43,44], Isatin-pyridine hybrids [45][46][47][48], Isatinchalcone hybrids [49], Isatin-quinazoline hybrids [50,51], Isatin-pthalazine hybrids [50], Isatinhydrazide hybrids [9,33,35,48], Isatin-naphthalene hybrids [14], isatin-thiosemicarbazone hybrid [9,20], Isatin-oxime hybrids [52], Isatin-nitrone hybrids…”

Section: Introductionmentioning

confidence: 99%

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A Survey of Isatin Hybrids and their Biological Properties

Shu,

Eni,

Ntie-Kang

2024

Preprint

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The emergence of diverse infections worldwide, which is a serious global threat to human existence, necessitate the urgent development of novel therapeutic candidates that can combat these diseases with efficacy. Isatin, a secondary metabolite from tryptophan is considered a privileged scaffold and favorable pharmacophore with a unique structural moiety and varied chemical and biological properties resulting in its widespread applications by medicinal chemists. Molecular hybridization is one of the most common and important techniques use in the synthesis of their bioactive hybrids in drug discovery. This review containing published articles from 2005 to 2022 focuses on isatin hybrids which have been synthesized and reported in the literature alongside a discussion on their biological properties. The purpose of this review is to set up the direction for the design and development of isatin-hybrids with tailored biological properties as effective therapeutic candidates inspired by nature.

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Section: Isatin-azole Hybridsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

A Survey of Isatin Hybrids and their Biological Properties

Shu,

Eni,

Ntie-Kang

2024

Preprint

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“…Similarly, prenylated chalcones [144] and prenyloxy chalcones [145] have demonstrated both anti-leishmanial and anti-trypanosomal activity. Additional compound classes that have shown potent anti-kinetoplastid activity include binuclear cyclopalladated compounds [146], 1,3,4,5-tetrasubstituted pyrazoles [147], N,N -dihetaryl substituted diamines [148], N-benzene and N-naphthalenesulfonamide derivatives [149], thiazolyl-isatin derivatives [150], and ruthenium-purine complexes [151]. Natural products have also been an area of interest, with several researchers identifying compounds like sesquiterpene lactones [152,153] and terpenoids [154] with anti-trypanosomatid properties.…”

Section: Drug Discovery Targeting Multiple Eukaryotic and Prokaryotic...mentioning

confidence: 99%

Drug Discovery for Cutaneous Leishmaniasis: A Review of Developments in the Past 15 Years

Corman,

McNamara,

Bakowski

2023

Microorganisms

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Leishmaniasis is a group of vector-borne, parasitic diseases caused by over 20 species of the protozoan Leishmania spp. The three major disease classifications, cutaneous, visceral, and mucocutaneous, have a range of clinical manifestations from self-healing skin lesions to hepatosplenomegaly and mucosal membrane damage to fatality. As a neglected tropical disease, leishmaniasis represents a major international health challenge, with nearly 350 million people living at risk of infection a year. The current chemotherapeutics used to treat leishmaniasis have harsh side effects, prolonged and costly treatment regimens, as well as emerging drug resistance, and are predominantly used for the treatment of visceral leishmaniasis. There is an undeniable need for the identification and development of novel chemotherapeutics targeting cutaneous leishmaniasis (CL), largely ignored by concerted drug development efforts. CL is mostly non-lethal and the most common presentation of this disease, with nearly 1 million new cases reported annually. Recognizing this unaddressed need, substantial yet fragmented progress in early drug discovery efforts for CL has occurred in the past 15 years and was outlined in this review. However, further work needs to be carried out to advance early discovery candidates towards the clinic. Importantly, there is a paucity of investment in the translation and development of therapies for CL, limiting the emergence of viable solutions to deal with this serious and complex international health problem.

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Combining network pharmacology with chromatographic fingerprinting and multicomponent quantitative analysis for the quality evaluation of Astragali Radix

Guo

Sha

et al. 2022

Biomedical Chromatography

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Nowadays, cultivated variants and adulterants of Astragali Radix (AR) have flooded the market, causing the quality assurance of AR to be challenging. To address this issue, we combined network pharmacology with chromatographic fingerprinting and multicomponent quantitative analysis for the quality evaluation of AR. Specifically, through network pharmacology, a complete understanding of the active components and pharmacological activities of AR was established. In addition, establishing fingerprint profiles and multicomponent quantitation by high-performance liquid chromatography (HPLC) is convenient and comprehensive, and can more fully reflect the overall situation of the distribution of various chemical components. To evaluate and differentiate AR from different origins, hierarchical cluster analysis and principal component analysis were performed. The result showed that AR acts synergistically through multiple targets and pathways. The content of chemical components in AR from different origins varied significantly. Combining network pharmacology and multicomponent quantification results, astragaloside II and IV and formononetin can be used as quality markers for the quality control of AR. This study provides a comprehensive and reliable strategy for the quality evaluation of AR and identifies its quality markers to ensure the quality of the herb.

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Structural improvement of new thiazolyl-isatin derivatives produces potent and selective trypanocidal and leishmanicidal compounds

Cited by 15 publications

References 26 publications

A Survey of Isatin Hybrids and their Biological Properties

A Survey of Isatin Hybrids and their Biological Properties

Drug Discovery for Cutaneous Leishmaniasis: A Review of Developments in the Past 15 Years

Combining network pharmacology with chromatographic fingerprinting and multicomponent quantitative analysis for the quality evaluation of Astragali Radix

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