Novel coumarin-isatin hybrids as potent antileishmanial agents: Synthesis, in silico and in vitro evaluations

Khatoon, Saira; Aroosh, Aiman; Islam, Arshad; Kalsoom, Saima; Ahmad, Faisal; Hameed, Shahid; Abbasi, Sumra Wajid; Yasinzai, Masoom; Naseer, Muhammad Moazzam

doi:10.1016/j.bioorg.2021.104816

Cited by 28 publications

(14 citation statements)

References 39 publications

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“…These compounds were then tested for antileishmanial activity against Leishmania tropica promastigotes and amastigotes and were found to be active, with IC 50 values ranging from 0.1 to 4.13 μmol/L. Compound 116 was found to be the most effective, with IC 50 values of 0.10 and 0.87 μmol/L against L. tropica promastigote and axenic amastigote forms, respectively ( Figure 19 ) [ 137 ].…”

Section: Antimicrobial Activities Of Isatin-based Scaffoldsmentioning

confidence: 99%

A Mini Review on Isatin, an Anticancer Scaffold with Potential Activities against Neglected Tropical Diseases (NTDs)

et al. 2022

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Isatin, chemically an indole-1H-2,3-dione, is recognised as one of the most attractive therapeutic fragments in drug design and development. The template has turned out to be exceptionally useful for developing new anticancer scaffolds, as evidenced by the increasing number of isatin-based molecules which are either in clinical use or in trials. Apart from its promising antiproliferative properties, isatin has shown potential in treating Neglected Tropical Diseases (NTDs) not only as a parent core, but also by attenuating the activities of various pharmacophores. The objective of this mini-review is to keep readers up to date on the latest developments in the biological potential of isatin-based scaffolds, targeting cancer and NTDs such as tuberculosis, malaria, and microbial infections.

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Section: Antimicrobial Activities Of Isatin-based Scaffoldsmentioning

confidence: 99%

A Mini Review on Isatin, an Anticancer Scaffold with Potential Activities against Neglected Tropical Diseases (NTDs)

et al. 2022

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“…However, virtual screening appears ever more efficient with the development of methodological tools [140,144], but several potential biases were reported [145]. For this reason, although this approach is very interesting, fast, and a cost-efficient alternative to high-throughput screening, the results should be tested and validated experimentally [146][147][148] afterward. Among the most recently published works are those of Khatoon et al [148], which identified original coumarin-isatin hybrids derivatives with antileishmanial activity.…”

Section: Recent Technological Advances Enabling the Development Of New Research Tools In The Drug Development Processmentioning

confidence: 99%

“…For this reason, although this approach is very interesting, fast, and a cost-efficient alternative to high-throughput screening, the results should be tested and validated experimentally [146][147][148] afterward. Among the most recently published works are those of Khatoon et al [148], which identified original coumarin-isatin hybrids derivatives with antileishmanial activity. From 10 synthesized derivatives, molecular docking revealed all 10 compounds could successfully fit into the binding pocket of the target (Leishmanolysin gp63) of L. tropica.…”

Section: Recent Technological Advances Enabling the Development Of New Research Tools In The Drug Development Processmentioning

confidence: 99%

Challenges and Tools for In Vitro Leishmania Exploratory Screening in the Drug Development Process: An Updated Review

Cohen

Azas

2021

Pathogens

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Leishmaniases are a group of vector-borne diseases caused by infection with the protozoan parasites Leishmania spp. Some of them, such as Mediterranean visceral leishmaniasis, are zoonotic diseases transmitted from vertebrate to vertebrate by a hematophagous insect, the sand fly. As there is an endemic in more than 90 countries worldwide, this complex and major health problem has different clinical forms depending on the parasite species involved, with the visceral form being the most worrying since it is fatal when left untreated. Nevertheless, currently available antileishmanial therapies are significantly limited (low efficacy, toxicity, adverse side effects, drug-resistance, length of treatment, and cost), so there is an urgent need to discover new compounds with antileishmanial activity, which are ideally inexpensive and orally administrable with few side effects and a novel mechanism of action. Therefore, various powerful approaches were recently applied in many interesting antileishmanial drug development programs. The objective of this review is to focus on the very first step in developing a potential drug and to identify the exploratory methods currently used to screen in vitro hit compounds and the challenges involved, particularly in terms of harmonizing the results of work carried out by different research teams. This review also aims to identify innovative screening tools and methods for more extensive use in the drug development process.

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“…In this context and as continuation of our research interests in biologically active isatin derivatives, 54–56 and non-covalent interactions, 57–62 herein we report the evaluation of in vitro α-glucosidase inhibitory activity of twelve phenoxy pendant isatins 1–12 (Fig. 1) in addition to solid-state structures of two compounds 4 and 9 .…”

Section: Introductionmentioning

confidence: 97%

Phenoxy pendant isatins as potent α-glucosidase inhibitors: reciprocal carbonyl⋯carbonyl interactions, antiparallel π⋯π stacking driven solid state self-assembly and biological evaluation

et al. 2022

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Novel coumarin-isatin hybrids as potent antileishmanial agents: Synthesis, in silico and in vitro evaluations

Cited by 28 publications

References 39 publications

A Mini Review on Isatin, an Anticancer Scaffold with Potential Activities against Neglected Tropical Diseases (NTDs)

A Mini Review on Isatin, an Anticancer Scaffold with Potential Activities against Neglected Tropical Diseases (NTDs)

Challenges and Tools for In Vitro Leishmania Exploratory Screening in the Drug Development Process: An Updated Review

Phenoxy pendant isatins as potent α-glucosidase inhibitors: reciprocal carbonyl⋯carbonyl interactions, antiparallel π⋯π stacking driven solid state self-assembly and biological evaluation

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