Microwave irradiated one pot, three component synthesis of a new series of hybrid coumarin based thiazoles: Antibacterial evaluation and molecular docking studies

Mamidala, Srikanth; Peddi, Sudhir Reddy; Aravilli, R Kowshik; Jilloju, Parameshwara Chary; Manga, Vijjulatha; Vedula, Rajeswar Rao

doi:10.1016/j.molstruc.2020.129114

Cited by 43 publications

(17 citation statements)

References 51 publications

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“…Zhang et al [81] presented the design, synthesis of benzimidazolallylidenehydrazinylmethylthiazole derivatives (57a-o, Figure 22), and their screening as well as their precursors for in vitro antimycobacterial activity against the selectable M. tuberculosis strain H37Ra [82,83]. All tested compounds (30) showed in vitro antimycobacterial activity against M. tuberculosis with MICs in range of 2-100 µg/mL. Most of the compounds exhibited moderate activity (MIC ≤ 10 µg/mL).…”

Section: Antituberculosismentioning

confidence: 99%

Thiazole Ring—A Biologically Active Scaffold

2021

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Background: Thiazole is a good pharmacophore nucleus due to its various pharmaceutical applications. Its derivatives have a wide range of biological activities such as antioxidant, analgesic, and antimicrobial including antibacterial, antifungal, antimalarial, anticancer, antiallergic, antihypertensive, anti-inflammatory, and antipsychotic. Indeed, the thiazole scaffold is contained in more than 18 FDA-approved drugs as well as in numerous experimental drugs. Objective: To summarize recent literature on the biological activities of thiazole ring-containing compounds Methods: A literature survey regarding the topics from the year 2015 up to now was carried out. Older publications were not included, since they were previously analyzed in available peer reviews. Results: Nearly 124 research articles were found, critically analyzed, and arranged regarding the synthesis and biological activities of thiazoles derivatives in the last 5 years.

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Section: Antituberculosismentioning

confidence: 99%

Thiazole Ring—A Biologically Active Scaffold

2021

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“…Mamidala et al [ 44 ] reported the synthesis of new coumarin-based thiazole derivatives, starting from thiocarbohydrazide, aldehydes, and α-halocarbonyl coumarins in a molar ratio of 1:2:1, under microwave heating ( Scheme 13 ). Various solvents like methanol, ethanol, dimethyl sulfoxide (DMSO), and acetonitrile and different catalysts such as acetic acid, sulfuric acid, and hydrochloric acid were investigated in order to optimize the reaction regarding time and yield.…”

Section: Synthesis Of Thiazole Derivativesmentioning

confidence: 99%

An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives

et al. 2021

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Thiazole, a five-membered heteroaromatic ring, is an important scaffold of a large number of synthetic compounds. Its diverse pharmacological activity is reflected in many clinically approved thiazole-containing molecules, with an extensive range of biological activities, such as antibacterial, antifungal, antiviral, antihelmintic, antitumor, and anti-inflammatory effects. Due to its significance in the field of medicinal chemistry, numerous biologically active thiazole and bisthiazole derivatives have been reported in the scientific literature. The current review provides an overview of different methods for the synthesis of thiazole and bisthiazole derivatives and describes various compounds bearing a thiazole and bisthiazole moiety possessing antibacterial, antifungal, antiprotozoal, and antitumor activity, encouraging further research on the discovery of thiazole-containing drugs.

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“…Coumarin has been classified as an oxygenated heterocycle rather than a benzoic acid derivative. Many coumarin hybrids have been reported to be used for medical disorders, namely as anti-allergic [ 103 ], antiviral [ 104 ], vasodilatory [ 105 ], antibacterial [ 106 , 107 ], exhibiting cyclooxygenase inhibition [ 108 ], lipoxygenase [ 109 ], antithrombotic [ 110 ], and anticancer activity [ 111 ]. The molecular hybridization of the coumarin nucleus to a biodynamic system that is a biologically active pharmacophore has enhanced biological activities.…”

Section: Coumarin 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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Microwave irradiated one pot, three component synthesis of a new series of hybrid coumarin based thiazoles: Antibacterial evaluation and molecular docking studies

Cited by 43 publications

References 51 publications

Thiazole Ring—A Biologically Active Scaffold

Thiazole Ring—A Biologically Active Scaffold

An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives

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

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