Antibacterial evaluation and molecular docking studies of pyrazole–thiosemicarbazones and their pyrazole–thiazolidinone conjugates

Ebenezer, Oluwakemi; Singh‐Pillay, Ashona; Koorbanally, Neil A.; Singh, Pushpinder

doi:10.1007/s11030-020-10046-w

Cited by 22 publications

(12 citation statements)

References 41 publications

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“…The chloro and dichloro Derivatives 137b and 137a were most potent against both Staphylococcus strains with MBC of 0.16 µM and 1.3 µM, respectively. Compound 137c also was high active against MRSA (MBC = 1.3 µM) [140].…”

Section: Antimicrobial Activitymentioning

confidence: 95%

The Bioactivity of Thiazolidin-4-Ones: A Short Review of the Most Recent Studies

Mech

Kurowska

Trotsko

2021

IJMS

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Thiazolidin-4-ones is an important heterocyclic ring system of a pharmacophore and a privileged scaffold in medicinal chemistry. This review is focused on the latest scientific reports regarding biological activities of thiazolidin-4-ones published in 2020 and 2021. The review covers recent information about antioxidant, anticancer, anti-inflammatory, analgesic, anticonvulsant, antidiabetic, antiparasitic, antimicrobial, antitubercular and antiviral properties of thiazolidin-4-ones. Additionally, the influence of different substituents in molecules on their biological activity was discussed in this paper. Thus, this study may help to optimize the structure of thiazolidin-4-one derivatives as more efficient drug agents. Presented information may be used as a practical hint for rational design of new small molecules with biological activity, especially among thiazolidin-4-ones.

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Section: Antimicrobial Activitymentioning

confidence: 95%

The Bioactivity of Thiazolidin-4-Ones: A Short Review of the Most Recent Studies

Mech

Kurowska

Trotsko

2021

IJMS

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“…Pyrazoles are diazoles with a five-membered ring, useful in organic synthesis, the most studied compounds among the family of azoles. In particular, the heterocyclic cycle has a diverse range of chemical and biological properties [ 57 , 58 , 59 ] that can be traced back to several well-established therapeutic agents in different classes. Because of the interesting pharmacological properties of pyrazole hybrids, they garnered much attention.…”

Section: Pyrazole Hybridsmentioning

confidence: 99%

A Review of the Recent Developments of Molecular Hybrids Targeting Tubulin Polymerization

Ebenezer

Shapi

Tuszyński

2022

IJMS

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Microtubules are cylindrical protein polymers formed from αβ-tubulin heterodimers in the cytoplasm of eukaryotic cells. Microtubule disturbance may cause cell cycle arrest in the G2/M phase, and anomalous mitotic spindles will form. Microtubules are an important target for cancer drug action because of their critical role in mitosis. Several microtubule-targeting agents with vast therapeutic advantages have been developed, but they often lead to multidrug resistance and adverse side effects. Thus, single-target therapy has drawbacks in the effective control of tubulin polymerization. Molecular hybridization, based on the amalgamation of two or more pharmacophores of bioactive conjugates to engender a single molecular structure with enhanced pharmacokinetics and biological activity, compared to their parent molecules, has recently become a promising approach in drug development. The practical application of combined active scaffolds targeting tubulin polymerization inhibitors has been corroborated in the past few years. Meanwhile, different designs and syntheses of novel anti-tubulin hybrids have been broadly studied, illustrated, and detailed in the literature. This review describes various molecular hybrids with their reported structural–activity relationships (SARs) where it is possible in an effort to generate efficacious tubulin polymerization inhibitors. The aim is to create a platform on which new active scaffolds can be modeled for improved tubulin polymerization inhibitory potency and hence, the development of new therapeutic agents against cancer.

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“…It is quite obvious that, in the above examples, the molecular hybridization theory (MH) is confirmed in practice (see Refs. [ 33 , 34 , 35 , 36 , 37 , 38 , 39 ] and literature cited therein).…”

Section: Silatranyl Physiologically Active Compoundsmentioning

confidence: 99%

“…A principle of MH, “two heads are better than one”, has been successfully used for the synthesis of, for example, new hybrid compounds with enhanced anticancer, anti-inflammatory, and anti-microbial properties (see Refs. [ 33 , 34 , 35 , 36 , 37 , 38 , 39 ] and literature cited therein).…”

Section: Introductionmentioning

confidence: 99%

3-Aminopropylsilatrane and Its Derivatives: A Variety of Applications

et al. 2022

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Silatranes arouse much research interest owing to their unique structure, unusual physical–chemical properties, and diverse biological activity. The application of some silatranes and their analogues has been discussed in several works. Meanwhile, a comprehensive review of the wide practical usage of silatranes is still absent in the literature. The ability of silatranes to mildly control hydrolysis allows them to form extremely stable and smooth siloxane monolayers almost on any surface. The high physiological activity of silatranes makes them prospective drug candidates. In the present review, based on the results of numerous previous studies, using the commercially available 3-aminopropylsilatrane and its hybrid derivatives, we have demonstrated the high potential of 1-organylsilatranes in various fields, including chemistry, biology, pharmaceuticals, medicine, agriculture, and industry. For example, these compounds can be employed as plant growth biostimulants, drugs, optical, catalytic, sorption, and special polymeric materials, as well as modern high-tech devices.

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Antibacterial evaluation and molecular docking studies of pyrazole–thiosemicarbazones and their pyrazole–thiazolidinone conjugates

Cited by 22 publications

References 41 publications

The Bioactivity of Thiazolidin-4-Ones: A Short Review of the Most Recent Studies

The Bioactivity of Thiazolidin-4-Ones: A Short Review of the Most Recent Studies

A Review of the Recent Developments of Molecular Hybrids Targeting Tubulin Polymerization

3-Aminopropylsilatrane and Its Derivatives: A Variety of Applications

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