Research Topic

Medicinally Privileged Scaffolds: Lactones and Lactams

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Cyclic esters and amides (commonly known as lactones and lactams respectively) are widely distributed in nature and many of them are being used as frontline drugs against an array of diseases. Besides natural sources, a huge number of synthetic lactones and lactams possess excellent pharmacological activities ...

Cyclic esters and amides (commonly known as lactones and lactams respectively) are widely distributed in nature and many of them are being used as frontline drugs against an array of diseases. Besides natural sources, a huge number of synthetic lactones and lactams possess excellent pharmacological activities and available in market as potential drugs. Accordingly, these two scaffolds (lactones and lactones) acquire key interest in modern drug discovery research and are subjected to preclinical and clinical studies around the globe in the battle against several dreadful diseases that include, but are not limited to, drug-resistant bacterial infection, critical fungal and protozoal infection, neuromotor dysfunction and so on. The medicinal significance of lactones and lactams as antibacterial, antifungal, antidiabetic, anti-inflammatory, antiparkinsonian, anti-HIV, antipsychotic, immunomodulators, vasodilators as well as anticancer have also been documented through hundreds of patents and publications.

This Research Topic is particularly dedicated to confer the recent advances that have been made in the chemistry and biology of lactone and lactam (both natural and synthetic). In silico design (through docking studies) and evaluation of ADMET profiles, state-of-the-art synthesis (including metal-ligand frameworks that involve lactones and lactams), biological evaluation (in vitro, ex-vivo, and in vivo), as well as studies on mechanism of action/effect in living systems are proposed to be the topics of discussion. This issue also enumerates the pertinent examples of lactonization and lactamization, both catalyzed and uncatalyzed. In the recent past, a number of catalysts have been reported to succeed lactonization and lactamization which include Lewis acids, organocatalysts, heterogeneous catalysts, phase-transfer catalysts, solid-supported catalysts and inorganic catalysts (bases, acids and salts). The following sub-topics are encouraged:
• Novel syntheses of lactone and lactam derivatives: Depending on ring sizes β-, γ-, δ-, ω-lactones and lactams, capro-lactams/lactones, macro-lactams/lactones including various subcategories like macrolides, ketolides etc. will be considered as subject of interest.
• Since green and sustainable chemistry is an extremely emerging and comparatively new field of research, attempts to stimulate more activities on green medicinal chemistry are provided. Syntheses of lactone and lactam derivatives that accomplish greener aspects (green methodology: green techniques, green solvents, green catalysts, preserves atom economy etc.) will be considered as an additional advantage for publication. Reports detailing microwave-assisted, sonochemical, mechanochemical syntheses of lactones and lactams will receive special attention.
• Synthetic efforts targeted to radiopharmaceuticals, biomarkers, and chemotherapeutic agents that involve lactam/lactone will be counted.
• Isolation, purification and spectral characterization of naturally occurring lactones and lactams and studies on their biological/pharmacological activity.
• In silico design of novel lactone and lactam pharmacophores. Docking studies, drug-protein interactions, binding with enzymes, epigenetic investigations will be prioritized.
• In silico ADMET (absorption, distribution, metabolism, excretion/elimination and toxicity) characteristics of lactone and lactam derivatives.
• Investigation on mechanism of action in cells and/or living systems including enzyme-inhibition studies.
• Extensive biological evaluation that elaborates in vitro, ex-vivo, and in vivo studies.
• Explorative studies on genomics and proteomics involving lactones and lactams.


Keywords: lactone, lactam, synthesis, medicinal activity, pharmacology


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