scholarly journals Novel 1,2,4-Oxadiazole Derivatives in Drug Discovery

2020 ◽  
Vol 13 (6) ◽  
pp. 111
Author(s):  
Karol Biernacki ◽  
Mateusz Daśko ◽  
Olga Ciupak ◽  
Konrad Kubiński ◽  
Janusz Rachon ◽  
...  
Keyword(s):  
Biological Activities ◽  
Wide Spectrum ◽  
Heterocyclic Ring ◽  
The Novel ◽  
Biological Applications ◽  
Biological Application ◽  
Comprehensive Overview ◽  
Oxadiazole Derivatives ◽  
Novel Drug ◽  
Further Development

Five-membered 1,2,4-oxadiazole heterocyclic ring has received considerable attention because of its unique bioisosteric properties and an unusually wide spectrum of biological activities. Thus, it is a perfect framework for the novel drug development. After a century since the 1,2,4-oxadiazole have been discovered, the uncommon potential attracted medicinal chemists’ attention, leading to the discovery of a few presently accessible drugs containing 1,2,4-oxadiazole unit. It is worth noting that the interest in a 1,2,4-oxadiazoles’ biological application has been doubled in the last fifteen years. Herein, after a concise historical introduction, we present a comprehensive overview of the recent achievements in the synthesis of 1,2,4-oxadiazole-based compounds and the major advances in their biological applications in the period of the last five years as well as brief remarks on prospects for further development.

An Overview on Chemistry and Biological Importance of Pyrrolidinone

2018 ◽  
Vol 15 (2) ◽  
pp. 166-178 ◽  
Author(s):  
Zahra Hosseinzadeh ◽  
Ali Ramazani ◽  
Kamaleddin Hosseinzadeh ◽  
Nima Razzaghi-Asl ◽  
Farideh Gouranlou
Keyword(s):  
Biological Activities ◽  
Wide Spectrum ◽  
Heterocyclic Ring ◽  
Review Article ◽  
Pharmacological Activities ◽  
Future Studies ◽  
Comprehensive Information ◽  
Novel Drugs ◽  
Bioactive Agents ◽  
Great Scope

Background: Pyrrolidinone is a five membered heterocyclic ring that is a versatile lead compound for designing powerful bioactive agents. Pyrrolidinone nucleus is one of the most important heterocyclic compound indicating notable pharmaceutical effects. Many procedures for the preparation of pyrrolidinone and also their various reactions offer great scope in the field of medicinal chemistry. This fascinating group of compounds has diverse pharmacological activities such as antibacterial, antifungal, anticancer and anticonvulsant. Objective: The review article proposes to classify comprehensive information on chemistry and pharmaceutical effects of pyrrolidinone in order to open new viewpoint for future studies. Conclusion: It is clear from the review of the topic that a wide spectrum of pyrrolidinone analogues have been synthesized and the majority of these derivatives have indicated different significant biological activities. Thus, these analogues can be used for future progression of novel drugs against many more poor agents.

A Mini Review on Synthesis of Pyrazinoindole: Recent Progress and Perspectives

2020 ◽  
Vol 17 ◽  
Author(s):  
Aarushi Singh ◽  
Samarpita Mahapatra ◽  
Shubham Sewariya ◽  
Nidhi Singh ◽  
Snigdha Singh ◽  
...  
Keyword(s):  
Biological Activities ◽  
Heterocyclic Ring ◽  
Ring Structure ◽  
Biologically Active ◽  
Comprehensive Overview ◽  
Protein Kinase C Inhibitors ◽  
Therapeutic Uses ◽  
Recent Developments ◽  
Pharmacologically Active ◽  
Synthetic Approaches

: The diverse library of biologically active organic compounds is composed majorly of heterocyclic compounds. Nature provides us with a variety of pharmacologically active compounds consisting of N-heterocycle motif such as Noscapine (anti-cancer), Morphine (analgesic), Chelerythrine (antibacterial), etc. which are the elementary structural units of marketed drugs in the present era. One of such “N-heterocyclic” promising building block which has gained attention of chemists is Pyrazinoindoles and the inflating interest in this moiety is a result of the three-fused heterocyclic ring structure subsuming an indolic nucleus in it. Fused-polycyclic structural core is necessary to synthesize for potential multi-functional drugs which is evident from indole (an example of fused five and six-membered ring structure) being an exemplary, established privileged template in medicinal chemistry. In the literature, Pyrazino-fused indoles have been found documented regarding their biological activities and therapeutic uses particularly as antifungal, antibacterial, serotonergic receptor inhibitor, central nervous system depressants, anticonvulsants, antihistaminic, protein kinase C inhibitors, antidepressants and so on. Although various synthesis strategies are available in the literature yet the medical relevance of the Pyrazinoindoles demands the development of versatile and simple novel methodologies. This review features comprehensive overview of the recent developments in synthetic approaches and therapeutic applications of Pyrazinoindoles based scaffolds.

A Review on Fast Dissolving Tablet

2017 ◽  
Vol 8 (03) ◽  
Author(s):  
Sagar T. Malsane ◽  
Smita S. Aher ◽  
R. B. Saudagar
Keyword(s):  
Drug Delivery ◽  
Patient Compliance ◽  
Research Area ◽  
Oral Route ◽  
Dosage Forms ◽  
The Novel ◽  
The Past ◽  
Orally Disintegrating Tablets ◽  
Novel Drug ◽  
Experience Difficulty

Oral route is presently the gold standard in the pharmaceutical industry where it is regarded as the safest, most economical and most convenient method of drug delivery resulting in highest patient compliance. Over the past three decades, orally disintegrating tablets (FDTs) have gained considerable attention due to patient compliance. Usually, elderly people experience difficulty in swallowing the conventional dosage forms like tablets, capsules, solutions and suspensions because of tremors of extremities and dysphagia. In some cases such as motion sickness, sudden episodes of allergic attack or coughing, and an unavailability of water, swallowing conventional tablets may be difficult. One such problem can be solved in the novel drug delivery system by formulating “Fast dissolving tablets” (FDTs) which disintegrates or dissolves rapidly without water within few seconds in the mouth due to the action of superdisintegrant or maximizing pore structure in the formulation. The review describes the various formulation aspects, superdisintegrants employed and technologies developed for FDTs, along with various excipients, evaluation tests, marketed formulation and drugs used in this research area.

Primordial science and pioneering approaches of guggul for chronic ailments – A modernized review

2020 ◽  
Vol 7 (2) ◽  
pp. 14-20
Author(s):  
Jamal Basha D ◽  
Kumar P R ◽  
Ranganayakulu D
Keyword(s):  
Water Solubility ◽  
Therapeutic Potential ◽  
Chemical Constituents ◽  
Signs And Symptoms ◽  
Dosage Forms ◽  
The Novel ◽  
Lipids Metabolism ◽  
Clinical Conditions ◽  
Novel Drug ◽  
Conventional Dosage

An oleo gum resin guggulu is a product which obtained as a result of gummosis from the bark of Commiphora wightii (Arnott) Bhandari [syn. Commiphoramukul (Hook. Ex Stocks) Family, Burseraceae]. It has been known for its immense applicability in the Ayurveda since time immemorial for the treatment of variety of disorders such as inflammation, gout, rheumatism, impotence, leprosy, obesity, and disorders of lipids metabolism. It is a mixture of phytoconstituents like terpenoids, steroids, flavonoids, guggultetrols, lignans, sugars, and amino acids. This review is an effort to compile all the information available on all of its chemical constituents which are responsible for its therapeutic potential, limitation of guggul extracts and the necessity of novel principles for gum guggul. Nowadays, Guggul is available as the marketed formulation for curing numerous clinical conditions and is accessible in combination with various other ingredients. Though conventional dosage form shows the dominance as patient compliance and easy availability, yet it has found to pose the problems like dose fluctuation, peak-valley effect, non-adjustment of the administered drug, invasiveness etc. Guggul lacks its desired effect due to its low bioavailability and water solubility. This makes it a partial or a deficient therapy for remedy of many signs and symptoms. Novel drug delivery system (NDDS), a new approach and has excluded many of drawbacks exhibited by conventional dosage forms. Some of the novel dosage forms of guggul has been formed like nanoparticles, nanovesicles, gugglusomes and proniosomal gel. But still, the novel formulations for guggul has its less outspread in the market. Guggul can be executed as a profitable drug using NDDS. There is a need to highlight the unidentified and unexplained facts about guggul so as to make it more efficacious and effective in terms of bioavailability and aqueous insolubility.

Synthesis, characterization and biological activities of 1,3,4-oxadiazole derivatives of nalidixic acid and their copper complexes

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Nalidixic Acid ◽  
Copper Complexes ◽  
Biological Activities ◽  
Bidentate Coordination ◽  
Antibacterial And Antifungal Activities ◽  
Elemental Analyses ◽  
Oxadiazole Derivatives ◽  
Antibacterial And Antifungal ◽  
Derivatives Of ◽  
Substituted 1

A series of novel 1, 3, 4-oxadiazole analogues was synthesized from cyclization of hydrazones of substituted 1-ethyl-1,4-dihydro-7-methyl-4-oxo-1,8-naphthyridine-3-carbohydrazides were prepared from nalidixic acid. The structures of synthesized oxadiazole derivatives and their copper complexes were elucidated on the basis of FTIR, elemental analyses, 1H-NMR and atomic absorption spectral analysis. It was observed from spectral data that metal ligand ratio was 1:1 in all copper complexes and they were bidentate, coordination was found to be done through oxygen of 4-oxo group and nitrogen of oxadiazole ring. The synthesized compounds were further evaluated with biological activities and compared with parent hydrazones. Copper complexes possess antibacterial and antifungal activities better than the oxadiazoles while they have better antioxidant activity then copper complexes. Parent hydrazones were better in all biological activities than synthesized oxadiazoles.

Diverse chemical and biological potentials of various pyridazine and pyridazinone derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Industrial Chemical ◽  
Anti Inflammatory ◽  
Pyridazinone Derivatives

A series of heterocyclic compounds incorporating pyridazine moiety were for diverse biological activities. Pyridazines and pyridazinones derivatives showed wide spectrum of biological activities such as vasodialator, cardiotonic, anticonvulsant, antihypertensive, antimicrobial, anti-inflammatory, analgesic, anti-feedant, herbicidal, and various other biological, agrochemical and industrial chemical activities. The results illustrated that the synthesized pyridazine/pyridazine compounds have diverse and significant biological activities. Mechanistic insights into the biological properties of pyridazinone derivatives and various synthetic techniques used for their synthesis are also described.

Anthocyanins As Modulators of Cell Redox-Dependent Pathways in Non-Communicable Diseases

2020 ◽  
Vol 27 (12) ◽  
pp. 1955-1996 ◽  
Author(s):  
Antonio Speciale ◽  
Antonella Saija ◽  
Romina Bashllari ◽  
Maria Sofia Molonia ◽  
Claudia Muscarà ◽  
...  
Keyword(s):  
Human Health ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Antioxidant Defenses ◽  
Noncommunicable Diseases ◽  
Protective Effects ◽  
Pathological Conditions ◽  
Chronic Pulmonary Diseases ◽  
Underlying Mechanisms

: Chronic Noncommunicable Diseases (NCDs), mostly represented by cardiovascular diseases, diabetes, chronic pulmonary diseases, cancers, and several chronic pathologies, are one of the main causes of morbidity and mortality, and are mainly related to the occurrence of metabolic risk factors. Anthocyanins (ACNs) possess a wide spectrum of biological activities, such as anti-inflammatory, antioxidant, cardioprotective and chemopreventive properties, which are able to promote human health. Although ACNs present an apparent low bioavailability, their metabolites may play an important role in the in vivo protective effects observed. : This article directly addresses the scientific evidences supporting that ACNs could be useful to protect human population against several NCDs not only acting as antioxidant but through their capability to modulate cell redox-dependent signaling. In particular, ACNs interact with the NF-κB and AP-1 signal transduction pathways, which respond to oxidative signals and mediate a proinflammatory effect, and the Nrf2/ARE pathway and its regulated cytoprotective proteins (GST, NQO, HO-1, etc.), involved in both cellular antioxidant defenses and elimination/inactivation of toxic compounds, so countering the alterations caused by conditions of chemical/oxidative stress. In addition, supposed crosstalks could contribute to explain the protective effects of ACNs in different pathological conditions characterized by an altered balance among these pathways. Thus, this review underlines the importance of specific nutritional molecules for human health and focuses on the molecular targets and the underlying mechanisms of ACNs against various diseases.

Tamarix articulata (T. articulata) - An Important Halophytic Medicinal Plant with Potential Pharmacological Properties

2019 ◽  
Vol 20 (4) ◽  
pp. 285-292 ◽  
Author(s):  
Abdullah M. Alnuqaydan ◽  
Bilal Rah
Keyword(s):  
Medicinal Plant ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
In Vivo Model ◽  
Drug Candidate ◽  
Phytochemical Analysis ◽  
Pharmacological Properties

Background:Tamarix Articulata (T. articulata), commonly known as Tamarisk or Athal in Arabic region, belongs to the Tamaricaece species. It is an important halophytic medicinal plant and a good source of polyphenolic phytochemical(s). In traditional medicines, T. articulata extract is commonly used, either singly or in combination with other plant extracts against different ailments since ancient times.Methods:Electronic database survey via Pubmed, Google Scholar, Researchgate, Scopus and Science Direct were used to review the scientific inputs until October 2018, by searching appropriate keywords. Literature related to pharmacological activities of T. articulata, Tamarix species, phytochemical analysis of T. articulata, biological activities of T. articulata extracts. All of these terms were used to search the scientific literature associated with T. articulata; the dosage of extract, route of administration, extract type, and in-vitro and in-vivo model.Results:Numerous reports revealed that T. articulata contains a wide spectrum of phytochemical(s), which enables it to have a wide window of biological properties. Owing to the presence of high content of phytochemical compounds like polyphenolics and flavonoids, T. articulata is a potential source of antioxidant, anti-inflammatory and antiproliferative properties. In view of these pharmacological properties, T. articulata could be a potential drug candidate to treat various clinical conditions including cancer in the near future.Conclusion:In this review, the spectrum of phytochemical(s) has been summarized for their pharmacological properties and the mechanisms of action, and the possible potential therapeutic applications of this plant against various diseases discussed.

Carbohydrate-Binding Agents: Potential of Repurposing for COVID-19 Therapy

2020 ◽  
Vol 21 (11) ◽  
pp. 1085-1096 ◽  
Author(s):  
Rajesh Kumar Gupta ◽  
Girish R. Apte ◽  
Kiran Bharat Lokhande ◽  
Satyendra Mishra ◽  
Jayanta K. Pal
Keyword(s):  
Vaccine Development ◽  
Host Cells ◽  
Carbohydrate Binding ◽  
Atypical Pneumonia ◽  
The Novel ◽  
High Infection ◽  
Binding Agents ◽  
Current Scenario ◽  
Antiviral Activities ◽  
Novel Drug

: With the emergence of the novel severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), the whole world is suffering from atypical pneumonia, which resulted in more than 559,047 deaths worldwide. In this time of crisis and urgency, the only hope comes from new candidate vaccines and potential antivirals. However, formulating new vaccines and synthesizing new antivirals are a laborious task. Therefore, considering the high infection rate and mortality due to COVID-19, utilization of previous information, and repurposing of existing drugs against valid viral targets have emerged as a novel drug discovery approach in this challenging time. The transmembrane spike (S) glycoprotein of coronaviruses (CoVs), which facilitates the virus’s entry into the host cells, exists in a homotrimeric form and is covered with N-linked glycans. S glycoprotein is known as the main target of antibodies having neutralizing potency and is also considered as an attractive target for therapeutic or vaccine development. Similarly, targeting of N-linked glycans of S glycoprotein envelope of CoV via carbohydrate-binding agents (CBAs) could serve as an attractive therapeutic approach for developing novel antivirals. CBAs from natural sources like lectins from plants, marine algae and prokaryotes and lectin mimics like Pradimicin-A (PRM-A) have shown antiviral activities against CoV and other enveloped viruses. However, the potential use of CBAs specifically lectins was limited due to unfavorable responses like immunogenicity, mitogenicity, hemagglutination, inflammatory activity, cellular toxicity, etc. Here, we reviewed the current scenario of CBAs as antivirals against CoVs, presented strategies to improve the efficacy of CBAs against CoVs; and studied the molecular interactions between CBAs (lectins and PRM-A) with Man9 by molecular docking for potential repurposing against CoVs in general, and SARSCoV- 2, in particular.

Resolving the Mystery of Ring Opening in the Synthesis of Benzo[d][1, 3]oxazin-4-one and Quinazolin-4(3H)-one

2019 ◽  
Vol 16 (11) ◽  
pp. 898-905
Author(s):  
Harun Patel ◽  
Rahul Pawara ◽  
Sanjay Surana
Keyword(s):  
Characteristic Feature ◽  
Ring Opening ◽  
Biological Activities ◽  
Heterocyclic Ring ◽  
Ring System ◽  
Time Saving ◽  
Fusion Strategy ◽  
Good Template ◽  
Lead Generation

Quinazoline is the six-membered heterocyclic ring system reported for its versatile biological activities. This characteristic feature of quinazoline makes it a good template for a lead generation library. Ring opening is one of the major concerns in the synthesis of quinazolin-4(3H)-one that results in diamide formation. Here, alternative fusion strategy is reported, which is a time-saving and costeffective method to overcome the ring opening problem associated with the synthesis of benzo[ d][1,3]oxazin-4-one and quinazolin-4(3H)-one.

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