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Piperidine nucleus as a promising scaffold for Alzheimer's disease: Current Landscape and Future Perspective
Curr Top Med Chem. 2023 Apr 6. doi: 10.2174/1568026623666230406084315. Online ahead of print.ABSTRACTHeterocycles and their derivatives hold an important place in medicinal chemistry due to their vast therapeutic and pharmacological significance and wider implications in drug design and development. Piperidine is a nitrogen-containing heterocyclic moiety that exhibits an array of pharmacological properties. This review discusses the potential of piperidine derivatives against the neurodegenerative disease Alzheimer's. The incidences of Alzheimer's disease are increasing nowadays, and constant efforts are being made to deve...
Source: Current Topics in Medicinal Chemistry - April 11, 2023 Category: Chemistry Authors: Parul Grover Suman Rohilla Monika Bhardwaj Lovekesh Mehta Anjleena Malhotra Source Type: research

QSAR into the New Millennium: Structural, Topological, Quantum, Shape, Electronic and Bio Descriptors for Machine Learning & amp; AI - Honoring Prof. Satya Prakash Gupta
Curr Top Med Chem. 2023 Apr 6. doi: 10.2174/1568026623666230406102636. Online ahead of print.NO ABSTRACTPMID:37038679 | DOI:10.2174/1568026623666230406102636 (Source: Current Topics in Medicinal Chemistry)
Source: Current Topics in Medicinal Chemistry - April 11, 2023 Category: Chemistry Authors: Krishnan Balasubramanian Vaishali Patil Source Type: research

Hydrazides as potential HDAC inhibitors: Structure-activity relationships and biological implications
Curr Top Med Chem. 2023 Apr 5. doi: 10.2174/1568026623666230405124207. Online ahead of print.ABSTRACTEpigenetic modulations by HDACs are associated with multiple disease conditions. In this context, HDACs play vital roles in the progression of diseases including several cancers, neurodegenerative diseases, inflammatory diseases, and metabolic disorders. Though several HDAC inhibitors have been established as drug candidates, their usage has been restricted because of broad-spectrum inhibition, highly toxic character, and off-target adverse effects. Therefore, specific HDAC selectivity is essential to get rid of such advers...
Source: Current Topics in Medicinal Chemistry - April 11, 2023 Category: Chemistry Authors: Suvankar Banerjee Sandip Kumar Badya Nilanjan Adhikari Tarun Jha Balaram Ghosh Source Type: research

Multicomponent Reactions Applied to Total Synthesis of Biologically Active Molecules: A Short Review
Curr Top Med Chem. 2023 Apr 3. doi: 10.2174/1568026623666230403102437. Online ahead of print.ABSTRACTMulticomponent reactions (MCRs) are processes in which three or more starting materials are combined in the same reaction vessel, forming an adduct that contains all or most of the atoms of the starting materials. MCRs are one-pot processes that provide attractive advantages for the total synthesis of target molecules. These reactions allow rapid access to structurally complex adducts from particularly simple starting materials. Moreover, MCRs are generally intrinsically associated with principles of green syntheses, such a...
Source: Current Topics in Medicinal Chemistry - April 5, 2023 Category: Chemistry Authors: Juliana A Dos Santos Pedro P de Castro Kleber T de Oliveira Timothy J Brocksom Giovanni W Amarante Source Type: research

Epigenetics mechanism and therapeutic potential of approved epi-drugs in pulmonary hypertension disease
Curr Top Med Chem. 2023 Apr 3. doi: 10.2174/1568026623666230403090650. Online ahead of print.ABSTRACTEpigenetics is defined as a heritable change occurring in gene expression and phenotype without altering the underlying primary DNA sequence itself. Epigenetic variation consists of DNA methylation repatterning, posttranslational modification of histone proteins, and non-coding RNAs (ncRNAs). Epigenetic modifications are deeply involved in tumorigenesis and tumor development. Epigenetic abnormalities can be therapeutically reversed, and three families of epigenetic marks, including "readers", "writers" and "erasers", could ...
Source: Current Topics in Medicinal Chemistry - April 4, 2023 Category: Chemistry Authors: Li Zhanqiang Huang Huoqiang Lu Dianxiang Source Type: research

Plants of the genus Mahonia as a Potential Traditional Chinese Medicine for the Prevention and Treatment of Alzheimer's Disease
Curr Top Med Chem. 2023 Mar 30. doi: 10.2174/1568026623666230330105251. Online ahead of print.ABSTRACTAlzheimer's disease (AD), a prevalent multiple neurodegenerative disease, has gained attention, particularly in the aging population. However, presently available therapies merely focus on alleviating the symptoms of AD and fail to slow disease progression significantly. Traditional Chinese medicine (TCM) has been used to ameliorate symptoms or interfere with the pathogenesis of aging-associated diseases for many years based on disease-modifying in multiple pathological roles with multi-targets, multi-systems and multi-asp...
Source: Current Topics in Medicinal Chemistry - April 3, 2023 Category: Chemistry Authors: Shuo Yang Huikai Shao Xiyu Chen Qiwen Liu Shengfeng Huang Yang Huang Source Type: research

Recent Advances in the Multistep Continuous Preparation of Apis and Fine Chemicals
Curr Top Med Chem. 2023 Mar 31. doi: 10.2174/1568026623666230331083734. Online ahead of print.ABSTRACTOver the last two decades, with the advent of continuous flow technologies, continuous processes have emerged as a major area in organic synthesis. In this context, continuous flow processes have been increasing in the preparation of Active Pharmaceutical Ingredients (APIs) and fine chemicals, such as complex synthetic intermediates, agrochemicals, and fragrances. Thus, the development of multi-step protocols has attracted special interest from the academic and industrial chemistry communities. In addition to the beneficia...
Source: Current Topics in Medicinal Chemistry - April 3, 2023 Category: Chemistry Authors: Pedro P ôssa de Castro Gabriel Martins Ferreira Batista Giovanni Wilson Amarante Timothy John Brocksom Kleber Thiago de Oliveira Source Type: research

Coumarin as a Privileged and Medicinally important Scaffold in the Treatment of Tuberculosis
Curr Top Med Chem. 2023 Mar 30. doi: 10.2174/1568026623666230330084058. Online ahead of print.ABSTRACTCoumarin and its derivatives, which are abundant in nature, have a significant role in medicinal chemistry due to their ability to bind with different targets or receptors. In addition, these possess a wide range of biological activity. Thus coumarin-based scaffold has inspired even further research into coumarin and its substituted derivatives, allowing for the creation of a huge variety of structurally different substituted products. In recent, these were reported to have potent antitubercular activity. Tuberculosis (TB)...
Source: Current Topics in Medicinal Chemistry - April 3, 2023 Category: Chemistry Authors: Vaibhav Gupta Ramesh Ambatwar Neeru Bhanwala Gopal L Khatik Source Type: research