Advancement in chiral heterocycles for the antidiabetic activity.

For the synthesis and development of pharmaceuticals, chirality is an important structural component. Chiral heterocyclic compounds have annoyed the interest of synthetic chemists who are working to create useful and efficient techniques for these molecules. As indicated by the expanding number of chiral drugs created in the last two decades, the link between chirality and pharmacological activity has become more important in the pharmaceutical and biopharmaceutical industries. Approximately 65% of currently used drugs are chiral, and many of them are promoted as racemates in many circumstances. There are a growing number of new chiral heterocyclic compounds with important biological properties and intriguing uses in medical chemistry and drug discovery. In this study, we review current breakthroughs in chiral heterocycles and their different physiological activities that have been published in the last year (from 2010 to early 2023). This study focuses on the current trends in the use of chiral heterocycles in drug design and the creation of several powerful and competent candidates for diabetic illnesses.

Supramolecular Cocrystals of Gliclazide: Synthesis, Characterization and Evaluation.

PURPOSE: To prepare the supramolecular cocrystals of gliclazide (GL, a BCS class II drug molecule) via mechanochemical route, with the goal of improving physicochemical and biopharmaceutical properties. METHODS: Two cocrystals of GL with GRAS status coformers, sebacic acid (GL-SB; 1:1) and α-hydroxyacetic acid (GL-HA; 1:1) were screened out using liquid assisted grinding. The prepared cocrystals were characterized using thermal and analytical techniques followed by evaluation of antidiabetic activity and pharmacokinetic parameters. RESULTS: The generation of new, single and pure crystal forms was characterized by DSC and PXRD. The crystal structure determination from PXRD revealed the existence of both cocrystals in triclinic (P-1) crystal system. The hydrogen bonded network, determined by material studio was well supported by shifts in FTIR and SSNMR. Both the new solid forms displayed improved solubility, IDR, antidiabetic activity and pharmacokinetic parameters as compared to GL. CONCLUSIONS: The improvement in these physicochemical and biopharmaceutical properties corroborated the fact that the supramolecular cocrystallization may be useful in the development of pharmaceutical crystalline materials with interesting network and properties.

Anticancer Potential of Azole Containing Marine Natural Products: Current and Future Perspectives.

BACKGROUND: Despite significant advancement in oncology research, cancer still poses one of the leading causes of mortality worldwide. The increased incidences of cancer may be attributed to the limited efficacy and disastrous side effects of conventional therapies like chemotherapy, radiotherapy and surgery. Azole containing medicinal agents are known for plethora of medicinal properties, including anticancer potential. OBJECTIVE: In this review, we highlighted azole containing natural products with anticancer potential from marine sources. METHODS: A comprehensive literature search was performed for writing the review. Updated views about various marine sponges, cyanobacteria, tunicates and microalgae producing azole nucleus containing secondary metabolites with anticancer potential have been discussed. RESULTS: The present article describes the structural, chemical, and biological features of azoles containing natural agents from marine sources with promising anti-cancer potential. Additionally, current challenges and future perspectives of azoles in cancer prevention and treatment are also discussed. CONCLUSION: This review might encourage scientific community to explore marine sources for developing novel and potent azole containing anti-cancer agents with better safety profile.

Retrospection on polymorphism and cocrystallization of anti-retrovirals.

Successful pharmaceutical development of a drug molecule depends not only on its potency and selectivity but also on its solid state. Thus the properties of active pharmaceutical ingrdient depend on the identity of its constituents as well as on their arrangement. It is quite common for a drug molecule to exist in more than one crystalline arrangement leading to polymorphism. The various polymorphs differ from each other in dissolution rate, bioavailability, oral absorption, toxicology and clinical trial results. Ultimately both safety and efficacy are impacted by properties that vary among different solid forms. In the recent years screening of polymorphs is increasingly emphasised in the pharmaceutical industry not only because of the valuable knowledge obtained provides necessary guidance for further development but also because of the issue of intellectual property rights. Cocrystallization is an emerging area of research and provides a unique opportunity to enhance marketed products or to pursue compounds that had otherwise been deemed non developable. This review discusses that how common polymorphism among anti- retroviral and its effect on their efficacy. Prevalence of cocrystallization in improving the bioavailability and efficacy of these pharmaceutically important drugs is also incorporated.