Pharma Research Bulletin

Volume 3, Issue 1, 2024

Number of Articles - 5
Research Article

Design and Synthesis of A Newer Series of Caffeic Acid Analogs as Potential New Delhi Metallo-β-Lactamase-1 (NDM-1) Inhibitors

Meenu Verma, Ajmer Singh Grewal*, Deepti Pandita, Viney Lather.

*Guru Gobind Singh College of Pharmacy, Yamunanagar, Haryana, India.

Abstract

Design and Synthesis of A Newer Series of Caffeic Acid Analogs as Potential New Delhi Metallo-β-Lactamase-1 (NDM-1) Inhibitors

New Delhi metallo-β-lactamase-1 (NDM-1) constructing microorganisms are unaffected by all the β-lactams together with carbapenems and pose an extreme risk to community wellbeing as they can simply spread through horizontal gene transfer. The present work was planned to design, prepare and evaluate the novel caffeic acid analogues as potential NDM-1 inhibitors. Docking studies were accomplished to explore the binding interactions of the designed molecules in the active site of the NDM-1 protein. A newer series of azetidine-substituted caffeic acid derivatives were synthesized using microwave irradiation and characterized using FTIR and 1H NMR spectroscopy. Designed molecules showed appreciable hydrogen bonds with Asn220 and metal interactions with zinc ions in the active site of NDM-1. Compounds 1, 6, 9 and 14 showed powerful in vitro antibacterial activities against Escherichia coli and compounds 4 and 13 showed potent antibacterial activities against Pseudomonas aeruginosa. The preliminary in silico results show an enormous potential for these molecules to act as strong NDM-1 inhibitors.
Review Article

Molecular Approaches and Significant Advances to Target Identification, Drug Discovery and Drug Development

Prabitha Prabhakaran, Sakshi Bhardwaj*, Dhivya Shanmugarajan, Sharath Chandra.

*Department of Life Sciences, Altem Technologies, Bangalore, India.

Abstract

Molecular Approaches and Significant Advances to Target Identification, Drug Discovery and Drug Development

Molecular pharmacology is a multidisciplinary field that explores how drugs interact with molecular targets in biological systems to achieve therapeutic effects. It integrates molecular biology, biochemistry, pharmacology, cheminformatics, and bioinformatics. Advances in biotechnology and molecular biology have driven the discovery of new targets and the development of potent medications. The primary aim is to identify optimal therapies by understanding drug interactions with receptors, enzymes, and transport molecules. Drug design, based on knowledge of biological targets, involves rational approaches where molecules are tailored to bind effectively. Computer-aided drug design (in silico) accelerates this process using methods like molecular docking, dynamics, and pharmacophore modelling. The drug discovery and development process includes early discovery, preclinical studies, clinical trials, FDA approvals, and post-marketing surveillance. Computational techniques such as QSAR, ADMET profiling, and molecular modelling enhance target identification and ligand optimization. High-throughput screening, aided by robotics and automation, enables rapid testing of millions of molecules, leading to the discovery of therapies for cancer and neurological diseases. Biotechnology advancements have enabled the development of monoclonal antibodies and gene therapies, with technologies like CRISPR-Cas9 offering precise gene editing. Genomics and proteomics accelerate target discovery by identifying disease-related genes and proteins, fostering personalized medicine approaches. Molecular pharmacology continues to revolutionize drug design and discovery, providing new opportunities for treating complex diseases and advancing precision medicine.
Review Article

Plants Use in Human Zinc Deficiency: A Review

Nisha Grewal*, Ankit, Smita Narwal, Gurvirender Singh.

*Global Research Institute of Pharmacy, Radaur-135133, Yamunanagar, Haryana, India.

Abstract

Plants Use in Human Zinc Deficiency: A Review

Zinc is vital for human health, playing key roles in essential physiological processes like DNA synthesis, immune function, and cellular activity. Despite its significance, zinc deficiency is a widespread health issue impacting billions worldwide. While zinc supplementation is commonly used, incorporating plant- based foods rich in phytochemicals presents an additional strategy to combat zinc insufficiency. Phytochemicals, abundant in fruits, vegetables, and legumes, interact with zinc in intricate ways, influencing how it is absorbed and utilized by the body. However, the relationship between plant compounds and zinc absorption is complex, with some compounds facilitating absorption while others impede it. Understanding these interactions is critical for optimizing dietary approaches to prevent zinc deficiency. Dietary factors, especially in regions where cereal-based diets dominate and lack diverse plant foods rich in zinc, exacerbate the prevalence of zinc insufficiency. Zinc deficiency can go unnoticed, posing challenges for diagnosis due to its varied physiological effects. Plant-derived compounds like polyphenols, flavonoids, and saponins have emerged as potential allies in addressing zinc deficiency, yet their effects vary depending on the context. While zinc supplementation remains a common method, recent research suggests that plant-based compounds hold promise in enhancing zinc absorption. This review delves into the history of zinc research, its physiological impacts, absorption mechanisms, and therapeutic potentials. Furthermore, it explores the role of plants in human zinc therapy, offering insights into future approaches to tackling zinc deficiency through plant-based interventions. Collaborative efforts spanning various disciplines are essential to effectively address the global burden of zinc deficiency and advance public health outcomes.
Research Article

Targeted Monitoring of Adverse Drug Reactions Following Pregabalin and Nortriptyline Prescription Against Neuropathic Pain

Deepika Sharma*, Vishwadeepak Kimothi, Sameer Gupta.

*Chandigarh College of Pharmacy, Landran, Greater Mohali-140307, Punjab, India.

Abstract

Targeted Monitoring of Adverse Drug Reactions Following Pregabalin and Nortriptyline Prescription Against Neuropathic Pain

Neuropathic pain is associated with lesions or illness affecting the somatosensory nervous system (periphery or centrally). Clinically speaking, neuropathic pain is characterized by a pain that comes on suddenly, lasts for a long time, or shoots, and by pain responses that are amplified in response to noxious or non-noxious stimuli. The present study was designed to monitor various incidences of adverse drug reactions (ADRs) associated with pregabalin (75 mg), and nortriptyline (10 mg) treatment of neuropathic pain either in individual use or in combined form. The study enrolled 75 patients in three groups (each containing 25 patients) suffering from neuropathic pain. The patients in different groups were treated with pregabalin (75 mg), nortriptyline (10 mg) and pregabalin + nortriptyline combination (75 mg + 10 mg) for 120 days and monitored for ADRs. Dryness of mouth, dizziness and sedation were the most common ADRs reported in 75 patients. The other ADRs include tingling sensation, weakness, constipation, skin rashes, irritability dizziness, etc. However, the patients treated with nortriptyline and pregabalin combination reported fewer ADRs as compared to when used individually in the management of neuropathic pain.
Review Article

Phytochemistry and Pharmacological Actions of Ginger: An In-Depth Review

Anmol Kaur, Shivani, Ajmer Singh Grewal*, Kumar Guarve.

*Guru Gobind Singh College of Pharmacy, Yamunanagar, Haryana, India.

Abstract

Phytochemistry and Pharmacological Actions of Ginger: An In- Depth Review

Zingiber officinale (generally known as ginger) is one of the utmost extensively employed herbs and food flavouring agents. Z. officinale belongs to the family Zingiberaceae which has over 1200 species in 53 genera. Z. officinale is widely used in traditional medicinal systems to treat a wide range of illnesses. The research includes its effects on cancer prevention, immune modulation, cardiovascular health, and pain relief. Studies also highlight its potential in managing diabetes and gastrointestinal disorders. In the last few decades, Z. officinale was extensively explored for its medicinal potential by innovative scientific methods and a diversity of bioactive molecules were derived from this plant and investigated pharmacologically. The present study is collective information concerning the phytochemistry and pharmacological activities of the herb Z. officinale.