Design, synthesis, and biological evaluation of isatin‐indole‐3‐carboxaldehyde hybrids as a new class of xanthine oxidase inhibitors

Singh, Atamjit; Heer, Shilpa; Kaur, Komalpreet; Gulati, Harmandeep Kaur; Kumar, Nitish; Sharma, Anchal; Singh, Jatinder; Bhagat, Kavita; Kaur, Gurinder; Kaur, Kirandeep; Singh, Harbinder; Chadha, Renu; Bedi, Preet Mohinder Singh

doi:10.1002/ardp.202200033

Cited by 23 publications

(11 citation statements)

References 44 publications

(60 reference statements)

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“…Our study indicated that microplastics stimulate the GST activity as the exposure period increased. LDPE had a significant effect on GST activity after 7 days of exposure Molecular docking studies is an effective tool to analyze the possible binding sites of a ligand in a particular enzyme and its interactions with the catalytic or non-catalytic sites at a molecular level that are responsible for the modulation of the activity of that enzyme (Chowdhary et al, 2022;Singh et al, 2022;Yuvaraj et al, 2021). Superoxide dismutase (SOD) catalyzes the conversion of superoxide radicals to oxygen and hydrogen peroxide resulting in the protection of cells from oxidative stress.…”

Section: Discussionmentioning

confidence: 99%

Biochemical responses, growth and reproduction of earthworm in low density polyethylene (LDPE)

Angmo

Dutta

Singh

et al. 2023

Environmental Quality Mgmt

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There is an unprecedented production of plastic that is accelerating its disposal while affecting the fitness of the terrestrial as well as the aquatic environment. The term microplastics refers to plastic fragments that are less than 5 mm in size and are widely distributed in the environment. Therefore, the present study intends to explore the biological response of earthworms (Eisenia fetida) toward different concentrations of low‐density polyethylene. E. fetida treated with low‐density polyethylene concentration (Control), 250 mg kg−1, 1000 mg kg−1, 6000 mg kg−1, 12,000 mg kg−1, and 25,000 mg kg−1. The above ratios were thoroughly mixed with 1kg of artificial soil and tested for growth, reproduction (cocoons and hatchling count), and enzymatic activities namely superoxide dismutase, guaiacol peroxidase, glutathione‐S‐transferase, and glutathione reductase and molecular docking studies. No mortality was observed during the exposure period at any concentrations. On the 28th day, when compared to the control the highest decrease in body weight of earthworms was observed in 25,000 mg (28.4%) followed by 12,000 mg (12.2%) and 6000 mg (3.4%). The cocoon and hatchlings significantly declined as the dose of microplastics increases. Enzymatic activity such as SOD and POD showed declined trend as the dose increased, while GST and GR increased with an increase in microplastic concentrations on 28th day. Furthermore, molecular docking showed that LDPE can modulate the activity of all four enzymes significantly.

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Section: Discussionmentioning

confidence: 99%

Biochemical responses, growth and reproduction of earthworm in low density polyethylene (LDPE)

Angmo

Dutta

Singh

et al. 2023

Environmental Quality Mgmt

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“…Keeping in view the pharmacological profile of isatin [70,71] and 1,2,3-triazole nucleus, Dehwal et al designed and synthesised 5-Fluoro-1H-indole-2,3-dione-triazoles and evaluated for antifungal activity against the Candida albicans. Among them, compound 42 was found to be most potent antifungal agent against Candida albicans with MIC value of 0.0075 μmol/mL as compared with standard fluconazole (MIC value of 0.0051 μmol/mL).…”

Section: 23-triazole Derivatives Containing Isatin Moietymentioning

confidence: 99%

“…Keeping in view the pharmacological profile of isatin [70,71] and 1,2,3‐triazole nucleus, Dehwal et al . designed and synthesised 5‐Fluoro‐1H‐indole‐2,3‐dione‐triazoles and evaluated for antifungal activity against the Candida albicans .…”

Section: 23‐triazole Derivatives With Antifungal Activity Against As ...mentioning

confidence: 99%

1,2,3‐Triazole Derivatives as an Emerging Scaffold for Antifungal Drug Development against Candida albicans: A Comprehensive Review

Singh

Sharma

et al. 2023

Chemistry & Biodiversity

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Candida infections are most prominent among fungal infections majorly target immunocompromised and hospitalized patients and cause significant morbidity and mortality. Candida albicans is the notorious and most prevalent among all pathogenic Candida strains. Its emerging resistance toward available antifungal agents making it hard to tackle and emerging as global healthcare emergency. Simultaneously, 1,2,3-triazole nucleus is a privileged scaffold that is gaining importance in antifungal drug development due to being a prominent bioactive linker and isostere of triazole based antifungal class core 1,2,4-triazole. Numerous reports have been updated in scientific literature in last few decades related to utilization of 1,2,3-triazole nucleus in antifungal drug development against Candida albicans. Present review will shed light on various preclinical studies focused on development of 1,2,3-triazole derivatives targeting Candida albicans along with brief highlight on clinical trials and newly approved drugs. Structure-activity relationship has been precisely discussed for each architect along with future perspective that will help medicinal chemists in design and development of potent antifungal agents for tackling infections derived from Candida albicans.

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“…Additionally, the antiproliferative activity was attenuated by lengthening the carbon spacer between morpholine and isatin. [ 99 ] Specifically, hybrids 59a,b (GI 50 : 4.36 and 9.22 µM) were comparable to plumbagin (GI 50 : 3.50 µM) and were more effective compared with tamoxefene (GI 50 : 50 µM). Mechanistically, hybrid 59a may result in G2/M‐phase mitotic arrest.…”

Section: Miscellaneous Indole/isatin Hybridsmentioning

confidence: 99%

The anti‐breast cancer potential of indole/isatin hybrids

Wang,

Huang,

Yuan

et al. 2023

Archiv der Pharmazie

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Breast cancer (BC) is one of the most prevalent malignancies and the major contributor to cancer mortality in women globally, with a high degree of heterogeneity and a dismal prognosis. As drug resistance is responsible for most BC fatalities and advanced BC is currently considered incurable, finding innovative anti‐BC chemotherapeutics is urgently required. Indole and its analog isatin (indole‐1H‐2,3‐dione) are prominent pharmacophores in the development of novel medications, and their derivatives exhibit strong anticancer activities, also against BC. In particular, indole/isatin hybrids exhibit significant potency against BC including multidrug‐resistant forms and excellent selectivity by influencing a variety of biological targets associated with the disease, supplying helpful building blocks for the identification of potential new BC treatment options. This review includes articles from 2020 to the present and provides insights into the in vitro and in vivo anti‐BC potential, molecular mechanisms, and structure–activity relationships (SARs) of indole/isatin hybrids that may be helpful in the development of innovative anti‐BC chemotherapeutics.

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Design, synthesis, and biological evaluation of isatin‐indole‐3‐carboxaldehyde hybrids as a new class of xanthine oxidase inhibitors

Cited by 23 publications

References 44 publications

Biochemical responses, growth and reproduction of earthworm in low density polyethylene (LDPE)

Biochemical responses, growth and reproduction of earthworm in low density polyethylene (LDPE)

1,2,3‐Triazole Derivatives as an Emerging Scaffold for Antifungal Drug Development against Candida albicans: A Comprehensive Review

The anti‐breast cancer potential of indole/isatin hybrids

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