Development of novel isatin–nicotinohydrazide hybrids with potent activity against susceptible/resistant<i>Mycobacterium tuberculosis</i>and bronchitis causing–bacteria

Elsayed, Zainab M.; Eldehna, Wagdy M.; Abdel‐Aziz, Marwa M.; Hassab, Mahmoud A. El; Al‐Warhi, Tarfah; Abdel‐Aziz, Hatem A.; Abou‐Seri, Sahar M.; Mohammed, Eman R.

doi:10.1080/14756366.2020.1868450

Cited by 44 publications

(21 citation statements)

References 42 publications

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“…The electron-withdrawing -F group improves the potency while electron-donating methyl decrease the potential. Recently, Elsayed et al [ 65 ] screened the anti-TB and antibacterial potency of novel isatin-nicotinohydrazide hybrids ( 42a – m and 43a – c , Figure 4 c). The anti-TB activities were evaluated against the drug-susceptible MTB strain (ATCC 27294) and INH/Streptomycin-resistant MTB (ATCC 35823).…”

Section: Development Of Isatin Derivatives As Promising Therapeutic A...mentioning

confidence: 99%

“…The active analogues were further subjected to docking simulation to determine the hydrogen bonding interaction within the cavity of decaprenylphosphoryl-b-D-Ribose 20-Epimerase (DprE1). It was proposed that compounds 42g and 42h show the best energy scores, at 10.1 and 9.7 kcal/mole, and the H-bond between carbonyl C=O with amino acid residues His-132 and Tyr-415 and hydrazide NH as well as the N-atom of pyridine displayed H-bond interactions with His-132 and Asn-385, respectively [ 65 ].…”

Section: Development Of Isatin Derivatives As Promising Therapeutic A...mentioning

confidence: 99%

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Therapeutic Outcomes of Isatin and Its Derivatives against Multiple Diseases: Recent Developments in Drug Discovery

Cheke¹,

Patil²,

Firke

et al. 2022

Pharmaceuticals

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Isatin (1H indole 2, 3-dione) is a heterocyclic, endogenous lead molecule recognized in humans and different plants. The isatin nucleus and its derivatives are owed the attention of researchers due to their diverse pharmacological activities such as anticancer, anti-TB, antifungal, antimicrobial, antioxidant, anti-inflammatory, anticonvulsant, anti-HIV, and so on. Many research chemists take advantage of the gentle structure of isatins, such as NH at position 1 and carbonyl functions at positions 2 and 3, for designing biologically active analogues via different approaches. Literature surveys based on reported preclinical, clinical, and patented details confirm the multitarget profile of isatin analogues and thus their importance in the field of medicinal chemistry as a potent chemotherapeutic agent. This review represents the recent development of isatin analogues possessing potential pharmacological action in the years 2016–2020. The structure–activity relationship is also discussed to provide a pharmacophoric pattern that may contribute in the future to the design and synthesis of potent and less toxic therapeutics.

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Section: Development Of Isatin Derivatives As Promising Therapeutic A...mentioning

confidence: 99%

Section: Development Of Isatin Derivatives As Promising Therapeutic A...mentioning

confidence: 99%

Therapeutic Outcomes of Isatin and Its Derivatives against Multiple Diseases: Recent Developments in Drug Discovery

Cheke¹,

Patil²,

Firke

et al. 2022

Pharmaceuticals

View full text Add to dashboard Cite

show abstract

“…The applied docking approach was firstly validated by re-docking each co-crystalized ligand into the active site of its corresponding enzyme. This step was followed by RMSD calculation between the co-crystalized and the docked poses for each enzyme [ 81 ]. Finally, the four major compounds were docked in the binding site of each enzyme using the validated docking protocol.…”

Section: Methodsmentioning

confidence: 99%

GC/MS Profiling, Anti-Collagenase, Anti-Elastase, Anti-Tyrosinase and Anti-Hyaluronidase Activities of a Stenocarpus sinuatus Leaves Extract

Younis

Ayoub

Mostafa

et al. 2022

Plants

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Today, skin care products and cosmetic preparations containing natural ingredients are widely preferred by consumers. Therefore, many cosmetic brands are encouraged to offer more natural products to the market, such as plant extracts that can be used for their antiaging, antiwrinkle, and depigmentation properties and other cosmetic purposes. In the current study, the volatile constituents of the hexane-soluble fraction of a Stenocarpus sinuatus (family Proteaceae) leaf methanol extract (SSHF) were analyzed using GC/MS analysis. Moreover, the antiaging activity of SSHF was evaluated through in vitro studies of anti-collagenase, anti-elastase, anti-tyrosinase, and anti-hyaluronidase activities. In addition, an in silico docking study was carried out to identify the interaction mechanisms of the major compounds in SSHF with the active sites of the target enzymes. Furthermore, an in silico toxicity study of the identified compounds in SSHF was performed. It was revealed that vitamin E (α-tocopherol) was the major constituent of SSHF, representing 52.59% of the extract, followed by γ-sitosterol (8.65%), neophytadiene (8.19%), β-tocopherol (6.07%), and others. The in vitro studies showed a significant inhibition by SSHF of collagenase, elastase, tyrosinase, and hyaluronidase, with IC50 values of 60.03, 177.5, 67.5, and 38.8 µg/mL, respectively, comparable to those of the positive controls epigallocatechin gallate (ECGC, for collagenase, elastase, hyaluronidase) and kojic acid (for tyrosinase). Additionally, the molecular docking study revealed good acceptable binding scores of the four major compounds, comparable to those of ECGC and kojic acid. Besides, the SSHF identified phytoconstituents showed no predicted potential toxicity nor skin toxicity, as determined in silico. In conclusion, the antiaging potential of SSHF may be attributed to its high content of vitamin E in addition to the synergetic effect of other volatile constituents. Thus, SSHF could be incorporated in pharmaceutical skin care products and cosmetics after further studies.

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“…5 A typical interaction between the susceptible and resistant strains. Source: Elsayed et al ( 2021 ); Karkman et al ( 2018 ) …”

Section: Natural Disasters and Climate Change’s Socio-economic Conseq...mentioning

confidence: 99%

A review of the global climate change impacts, adaptation, and sustainable mitigation measures

Abbass

Qasim

Song

et al. 2022

Environ Sci Pollut Res

866

185

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Climate change is a long-lasting change in the weather arrays across tropics to polls. It is a global threat that has embarked on to put stress on various sectors. This study is aimed to conceptually engineer how climate variability is deteriorating the sustainability of diverse sectors worldwide. Specifically, the agricultural sector’s vulnerability is a globally concerning scenario, as sufficient production and food supplies are threatened due to irreversible weather fluctuations. In turn, it is challenging the global feeding patterns, particularly in countries with agriculture as an integral part of their economy and total productivity. Climate change has also put the integrity and survival of many species at stake due to shifts in optimum temperature ranges, thereby accelerating biodiversity loss by progressively changing the ecosystem structures. Climate variations increase the likelihood of particular food and waterborne and vector-borne diseases, and a recent example is a coronavirus pandemic. Climate change also accelerates the enigma of antimicrobial resistance, another threat to human health due to the increasing incidence of resistant pathogenic infections. Besides, the global tourism industry is devastated as climate change impacts unfavorable tourism spots. The methodology investigates hypothetical scenarios of climate variability and attempts to describe the quality of evidence to facilitate readers’ careful, critical engagement. Secondary data is used to identify sustainability issues such as environmental, social, and economic viability. To better understand the problem, gathered the information in this report from various media outlets, research agencies, policy papers, newspapers, and other sources. This review is a sectorial assessment of climate change mitigation and adaptation approaches worldwide in the aforementioned sectors and the associated economic costs. According to the findings, government involvement is necessary for the country’s long-term development through strict accountability of resources and regulations implemented in the past to generate cutting-edge climate policy. Therefore, mitigating the impacts of climate change must be of the utmost importance, and hence, this global threat requires global commitment to address its dreadful implications to ensure global sustenance.

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Development of novel isatin–nicotinohydrazide hybrids with potent activity against susceptible/resistantMycobacterium tuberculosisand bronchitis causing–bacteria

Cited by 44 publications

References 42 publications

Therapeutic Outcomes of Isatin and Its Derivatives against Multiple Diseases: Recent Developments in Drug Discovery

Therapeutic Outcomes of Isatin and Its Derivatives against Multiple Diseases: Recent Developments in Drug Discovery

GC/MS Profiling, Anti-Collagenase, Anti-Elastase, Anti-Tyrosinase and Anti-Hyaluronidase Activities of a Stenocarpus sinuatus Leaves Extract

A review of the global climate change impacts, adaptation, and sustainable mitigation measures

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