Drug repurposing is a strategy consisting of finding new indications for already known marketed drugs used in various clinical settings or highly characterized compounds despite they can be failed drugs. Recently, it emerges as an alternative approach for the rapid identification and development of new pharmaceuticals for various rare and complex diseases for which lack the effective drug treatments. The success rate of drugs repurposing approach accounts for approximately 30% of new FDA approved drugs and vaccines in recent years.This review focuses on the status of drugs repurposing approach for various diseases including skin diseases, infective, inflammatory, cancer, and neurodegenerative diseases.Efforts have been made to provide structural features and mode of actions of drugs.Keywords: Cancer, drug repositioning, drug reprofiling, recycling of drugs, drug discovery, inflammation, neurodegenerative diseases, skin diseases. since clinical and pre-clinical studies of the re-purposed candidates are already being documented in the original indication(s). Thus, it reduces the time and cost needed to reach the market and risk intrinsic to any research and development program. Moreover, the risk of clinical failure is also low. As an added advantage, this approach gives a possibility to widen the market and to prolong the application of the patent life of a drug. There are mainly two ways to proceed drug-repositioning approach such as experimental strategies and computational strategies.Experimental repurposing strategies include binding assays and phenotypic screening methods, which can be to find binding interactions of drug molecules to assay components and to identify lead compounds from a vide range of compound libraries, respectively [10].Computational approaches are categorized into target-/mechanism based, knowledge-based, pathway-and network-based approaches. These approaches are proven economic in discovering novel therapeutic ligands. Most notably, computational methods augment the drug discovery process by effectively utilizing cheminformatics, bioinformatics, network biology and systems biology. More specifically, these methods exploit known targets, drugs, disease biomarkers or pathways to establish novel methods and accelerate the planning of crucial clinical trials [11].In this perspective, we focused on the status of drugs repurposing approaches for various diseases including skin diseases, infective, inflammatory, cancer, and neurodegenerative diseases. Efforts have been made to provide structural features, and modes of action of drugs, which are exclusively small molecules, peptidomimetics, and macrocyclic compounds.Antibodies, vaccines, and any other biological drugs are not discussed. Drugs repositioning for skin whitening activity.Melanin is a collection of natural pigments that primarily determine the skin, hair and hair color of the human. Melanocytes, which are found in the basal layer of the epidermis, produce melanin by the process called melanogenesis upon the skin exposure to the ultra...
Dimerization of proteins/receptors plays a critical role in various cellular processes, including cell proliferation and differentiation. Therefore, targeting such dimeric proteins/receptors by dimeric small molecules could be a potential therapeutic approach to treating various diseases, including inflammation‐associated diseases like cancer. A novel series of bis‐imidazoles (13–18) and bis‐imidazo[1,2‐a]pyridines (19–28) were designed and synthesized from Schiff base dimers (1–12) for their anticancer activities. All the synthesized compounds were screened for anticancer activities against three cancer cell lines, including cervical (HeLa), breast (MDA‐MB‐231), and renal cancer (ACHN). From structure–activity relationship studies, imidazo[1,2‐a]pyridines (19–28) showed remarkable cytotoxic activities, with compounds 19 and 24 showing the best inhibitory activities against all three cell lines. Especially, both 19 and 24 were very effective against the breast cancer cell line (19, GI50 = 0.43 µM; 24, GI50 = 0.3 µM), exceeding the activity of the control adriamycin (GI50 = 0.51 µM). The in vivo anticancer activity results of compounds 19 and 24 were comparable with those of the animals treated with the standard drug tamoxifen. Therefore, the dimeric imidazo[1,2‐a]pyridine scaffold could serve as a potential lead for the development of novel anticancer agents.
Anti‐inflammatory, specialized proresolving mediators such as resolvins, protectins, maresins, and lipoxins derived from polyunsaturated acids may play a potential role in lung diseases as they protect different organs in animal disease models. Polyunsaturated fatty acids are an important resource for epoxy fatty acids (EET, EEQ, and EDP) that mediate a broad array of anti‐inflammatory and proresolving mechanisms, such as mitigation of the cytokine storm. However, epoxy fatty acids are rapidly metabolized by soluble epoxide hydrolase (sEH). In animal studies, administration of sEH inhibitors (sEHIs) increases epoxy fatty acid levels, reduces lung inflammation, and improves lung function, making it a viable COVID‐19 treatment approach. Thus, using sEHIs to activate endogenous resolution pathways might be a novel method to minimize organ damage in severe cases and improve outcomes in COVID‐19 patients. This review focuses on the use of sEH inhibitors to activate endogenous resolution mechanisms for the treatment of COVID‐19.
: SARS-CoV-2, a positive single-stranded RNA enveloped coronavirus, currently poses a global health threat. Drugs with quinoline scaffolds have long been studied to repurpose their useful broad-spectrum properties into treating various diseases, including viruses. Preliminary studies on the quinoline medications, Chloroquine and Hydroxy chloroquine, against SARS-CoV2, have shown to be a potential area of interest for drug development, due to their ability to prevent viral entry, act as anti-inflammatory modulators, and inhibit key enzymes allowing reduced viral infectivity. In addition to Chloroquine and Hydroxychloroquine, we discuss analogs of the drugs to understand the quinoline scaffold’s potential antiviral mechanisms. The heterocyclic scaffold of quinoline can be modified in many ways primarily through the modification of its substituents, we cover these different synthetic derivatives to understand properties that could enhance its antiviral specificity thoroughly. Chloroquine and its analogs can act on various stages of the viral life cycle pre and post entry. In this study, we review Chloroquine and its synthetic and natural analogs for their antiviral properties in a variety of different viruses. Furthermore, we review the compound’s potential abilities to attenuate symptoms associated with viral infections. Natural compounds that share scaffolding to Chloroquine can act as antivirals or attenuate symptoms through stimulate the host immune system or reducing oxidative stress. Furthermore, we discuss perspectives of the drug’s repurposing due to its ability to inhibit beta-hematin formation and to be a Zinc Ionophore.
A novel series of Schiff base dimers have been designed and synthesized from phthalaldehydes and various amines including aliphatic, aromatic and heterocycles by grinding at room temperature. This solvent free green protocol approach is superior to the classical approach which uses ethanol as solvent. The advantage of this new method is that wide substrates can be incorporated, very simple to carry out the reaction, easy workup with high product yield. Compounds obtained have been screened for anti-bacterial activity against nine different strains (six Gram-negative and three Gram-positive) which include E.coli, Proteus mirabilis, Klebsiella pneumonia, Proteus vulgaris, Morganella morgana, Salmonella typhi, Staphylococcus aureus, Methicillin-resistant Staphylococcus aureus, Enterococci faecalis. Among them, the heterocyclic groups in the side chain of the Schiff base showed better activity than the aromatic and aliphatic groups. Particularly the thiophene substituted 1,4-isomer of the Schiff base dimer showed good antibacterial activity against seven strains. Interestingly, the 1,3 isomer of the Schiff base dimer with thiophene substituent exhibited a potent antibacterial activity. An effective Structure-Activity Relationship have also been established for the Schiff base dimers to find novel and potent anti-bacterial agents.
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