Synthesis and Evaluation of Antioxidant, Anti-inflammatory and Antiulcer Activity of Conjugates of Amino Acids with Nifedipine

Subudhi, Bharat Bhusan; Sahoo, Sudarsan

doi:10.1248/cpb.59.1153

Cited by 9 publications

(3 citation statements)

References 11 publications

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“…This study suggested that adding amino acids to nifedipine boosted its antioxidant activity and also enhanced its antisecretory properties and anti-inflammatory and anti-ulcer activities. Phe and Met conjugates of nifedipine showed the greatest activity in the series [ 121 ].…”

Section: Conjugated or Hybrid Moleculesmentioning

confidence: 99%

Conjugation as a Tool in Therapeutics: Role of Amino Acids/Peptides-Bioactive (Including Heterocycles) Hybrid Molecules in Treating Infectious Diseases

et al. 2023

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Peptide-based drugs are gaining significant momentum in the modern drug discovery, which is witnessed by the approval of new drugs by the FDA in recent years. On the other hand, small molecules-based drugs are an integral part of drug development since the past several decades. Peptide-containing drugs are placed between small molecules and the biologics. Both the peptides as well as the small molecules (mainly heterocycles) pose several drawbacks as therapeutics despite their success in curing many diseases. This gap may be bridged by utilising the so called ‘conjugation chemistry’, in which both the partners are linked to one another through a stable chemical bond, and the resulting conjugates are found to possess attracting benefits, thus eliminating the stigma associated with the individual partners. Over the past decades, the field of molecular hybridisation has emerged to afford us new and efficient molecular architectures that have shown high promise in medicinal chemistry. Taking advantage of this and also considering our experience in this field, we present herein a review concerning the molecules obtained by the conjugation of peptides (amino acids) to small molecules (heterocycles as well as bioactive compounds). More than 125 examples of the conjugates citing nearly 100 references published during the period 2000 to 2022 having therapeutic applications in curing infectious diseases have been covered.

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Section: Conjugated or Hybrid Moleculesmentioning

confidence: 99%

Conjugation as a Tool in Therapeutics: Role of Amino Acids/Peptides-Bioactive (Including Heterocycles) Hybrid Molecules in Treating Infectious Diseases

et al. 2023

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“…[373][374][375] The most common synthetic procedure to obtain pyridines is using the Hantzsch reaction. [376][377][378][379][380][381][382][383] The preparation of 1,4-dihydropyridines requires two equivalents of β-keto ester, an aldehyde and nitrogen donor. Sudalai and co-workers utilized dimethylmalonate 35 as the β-keto ester, 2-nitro-benzaldehyde 36 for the aldehyde and ammonium acetate as the nitrogen donor (Scheme 9).…”

Section: Nifedipinementioning

confidence: 99%

Therapeutic Potential of Heterocyclic Compounds Targeting Mitochondrial Calcium Homeostasis and Signaling in Alzheimer’s Disease and Parkinson’s Disease

Tapias¹,

González-Andrés²,

Peña³

et al. 2023

Preprint

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The brain is a complex organ that controls body functions and homeostasis through the action of neuronal and glial cells. Neuronal activity is highly energy-dependent and requires large numbers of functional mitochondria to provide substantial amount of energy via mitochondrial oxidative phosphorylation (OXPHOS), the most efficient metabolic process to generate adenosine triphosphate (ATP). Under stress conditions, neurons are particularly vulnerable to mitochondrial dysfunction, leading to decreased ATP synthesis, excessive generation of reactive oxygen species (ROS) and reactive nitrogen species (RNS), and intracellular Ca2+ dyshomeostasis, although not necessarily in this order. Alzheimer's disease (AD) and Parkinson’s disease (PD) are the two most common neurodegenerative diseases in elderly and are characterized by the presence of abnormal protein aggregates and the progressive and irreversible loss of neurons in specific brain regions. The exact mechanisms underlying the etiopathogenesis of AD or PD remain unknown, but there is extensive evidence indicating that compromised mitochondrial energy metabolism along with a depleted antioxidant system play a vital role in the pathophysiology of these neurological disorders. Toxic accumulation of proteins such as amyloid β peptides (Aβ) or amyloid precursor protein (APP) in AD and α-synuclein (α-syn) or leucine-rich repeat kinase 2 (LRRK2) in PD cause mitochondrial deficits through direct inhibition of electron transport chain (ETC) assembly and function, thereby resulting in further generation of ROS/RNS and disturbance of Ca2+ influx. Due to the improvement in life expectancy, the incidence of age-related neurodegenerative diseases has significantly increased. There is no effective protective treatment or therapy available but rather only very limited palliative treatment. There is an urgent need for the development of preventive strategies and disease-modifying therapies (both neuroprotective and neurorestorative interventions) to treat AD/PD. Here, we review the capability of some heterocyclic compounds to modulate Ca2+ homeostasis and signaling with a potential role in regulating mitochondrial function and associated free radical production during the development and onset of AD or PD. Moreover, we have included the chemical synthesis of a series of heterocycles and their derivatives.

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“…For example, Siddaiah et al published a modified Hantzsch PEG-mediated, catalyst-free synthesis under solvent-free conditions [43] (Scheme 9). The interest of researchers in dihydropyridine derivatives (including those containing nitro) has not weakened to date due to new types of activities revealed: anticonvulsant [40], antioxidant, anti-inflammatory, and antiulcer [41]. Nifedipine is a calcium-channel blocker of the dihydropyridine type that has been used since the last century [42] as a medicine for the treatment of diseases such as angina, high blood pressure (including during pregnancy), Raynaud's phenomenon, and premature labor.…”

mentioning

confidence: 99%

Recent Progress in the Synthesis of Drugs and Bioactive Molecules Incorporating Nitro(het)arene Core

Bastrakov¹,

Старосотников²

2022

Pharmaceuticals

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Aromatic nitro compounds play a unique role in the synthesis of drugs and pharmaceutically oriented molecules. This field of organic chemistry continues to be in demand and relevant. A significant number of papers are published annually on new general methods for the synthesis of nitrodrugs and related biomolecules. This review is an analysis of the literature on methods for the synthesis of both new and already-known aromatic and heteroaromatic nitrodrugs covering the period from 2010 to the present.

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Synthesis and Evaluation of Antioxidant, Anti-inflammatory and Antiulcer Activity of Conjugates of Amino Acids with Nifedipine

Cited by 9 publications

References 11 publications

Conjugation as a Tool in Therapeutics: Role of Amino Acids/Peptides-Bioactive (Including Heterocycles) Hybrid Molecules in Treating Infectious Diseases

Conjugation as a Tool in Therapeutics: Role of Amino Acids/Peptides-Bioactive (Including Heterocycles) Hybrid Molecules in Treating Infectious Diseases

Therapeutic Potential of Heterocyclic Compounds Targeting Mitochondrial Calcium Homeostasis and Signaling in Alzheimer’s Disease and Parkinson’s Disease

Recent Progress in the Synthesis of Drugs and Bioactive Molecules Incorporating Nitro(het)arene Core

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