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Abstract: Due to their diverse applications in industrial and synthetic organic chemistry, quinoline and 1,3,4-oxadiazole have become important heterocyclic compounds. Quinoline and 1,3,4- oxadiazole compounds have been developed for various medical conditions such as anti-cancer, anti-bacterial, anti-fungal, antimalarial, antioxidants, anti-HIV, anticonvulsant, antiviral, etc. The current review includes synthetic protocols for biologically active 1,3,4-oxadiazole incorporating quinoline hybrids with their structure-activity relationship to explore work (Mainly from 2010 to 2021) based on 1,3,4-oxadiazole-quinoline hybrids to the medicinal chemist for further research in the development of the molecule.

Abstract: Quinoline has recently become an important heterocyclic molecule due to its numerous industrial and synthetic organic chemistry applications. Quinoline derivatives have been used in clinical trials for a variety of medical conditions that causes cancer. The present literature study is composed of recent progress (mainly from 2010 to the present) in the production of novel quinoline derivatives as potential anti-cancer agents, as well as their structure-activity relationship, which will provide insight into the development of more active quinoline hybrids in the future. : The present review comprises the synthetic protocols of biologically active Quinoline analogs with their structure-activity relationship studies as anti-cancer agents, which provide depth view of work done on quinoline derivatives to the medicinal chemist for future research.

Abstract: Herbal medicines are being used by humans since the oldest civilizations and have been an integral part of traditional and alternative medicines. In recent times, pharmaceutical and biomedical scientists are taking interest in developing nutraceutical-based medicines to overcome the side effects and adverse drug reactions caused by allopathic medicines. Nutraceuticals have started occupying the global market. Nutraceuticals have gained widespread acceptance due to their efficacy in treating difficult to treat diseases, low toxicity, low cost, easy accessibility, etc. Safety and efficacy are other important factors in the commercialization process of nutraceuticals. Different novel advanced drug delivery systems have been constantly studied to improve the efficacy and bioavailability of medicines obtained from herbal sources. The transdermal drug delivery system provides a potent alternative to the conventional method of using nutraceuticals. The development of transdermal system-based nutraceuticals could provide the advantage of enhanced bioavailability, improved solubility, bypass of the first-pass metabolism, and targeted delivery of drugs in brain-related disorders. It additionally provides the advantage of being non-invasive. This article reviews the potential effects of various nutraceuticals in brain-related disorders as well as trends in transdermal nano-systems to deliver such nutraceuticals. We have also focused on advantages, applications as well as recent United States-based patents which emphasize emerging interest towards transdermal nutraceuticals in brain disorders.

Abstract: Heterocyclic compounds are fundamental building blocks for developing novel bioactive compounds. Due to their extensive uses in both industrial and synthetic organic chemistry, quinoline and benzimidazole have recently become important heterocycles. Clinical trials have investigated quinoline and benzimidazole analogues to treat a variety of illnesses, including cancer, bacterial and fungal infection, DNA damage, etc. Medicinal chemists are paying attention to nitrogen-containing hybrid heterocyclic compounds that have a wide range of therapeutical potential with lesser adverse effects. Many efforts have been made to find new and more efficient ways to synthesize these molecules. However, microbial resistance is becoming a major threat to the scientific community; hence, the necessity for the discovery and development of novel antimicrobial drugs with novel modes of action is becoming highly significant. One strategy to overcome this problem is to produce hybrid molecules by combining two or more bioactive heterocyclic moieties in a single molecular platform. Based on established research data on quinoline-bearing benzimidazole derivatives, it can be concluded that both moieties are used for the synthesis of promising therapeutically active agents. This present review comprises the synthetic approaches of biologically active quinolines containing benzimidazole derivatives with their structure-activity relationship studies to provide an overview of the work done on quinoline derivatives to the medicinal chemist for future research.

Currently, black pepper commands the leading position among all the spices as a spice of great commercial importance in all the world trade and finds its way into the dietary habits of millions of people worldwide. Black pepper is biologically known as Piper nigrum and contains piperine as the main active chemical constituent. This paper highlights various general methods for extracting piperine from the crude drug such as maceration extraction, hydrotropic extraction, accelerated solvent extraction, thin-layer chromatography, and extraction with ethanol & dichloromethane Ionic fluid-based ultrasonic-assisted extraction, etc. In this review, piperine and its analogs exhibit numerous pharmacological activities and synthetic schemes of insecticidal activity, anti-cancer activity, anti-inflammatory activity, anti-diabetic activity, anti-hyperlipidemic activity, antifungal activity, narcotic activity, etc. and its structure-activity relationship. The biochemistry of piperine has also been summarized in the presented article. This very exhaustive review details the complete information about piperine, its derivatives, and further processing. Furthermore, the current study summarises recent research that has linked piperine to its use as a treatment for a variety of ailments.

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Background: Benzimidazole (Benz-fused bicyclic ring system) is the most versatile class of heterocyclic compounds due to their numerous applications in industrial and synthetic organic chemistry because of its many biological actions. Benzimidazole analogs have been utilized to discover a variety of medical problems, such as cancer, bacterial infections, fungal infections, etc. Nitrogen-containing hybrid heterocyclic compounds are being studied by researchers because it provides a broad range of therapeutic potential and has minimal side effects. Objective: The current review of the literature emphasizes recent developments in the design of new benzimidazole derivatives as possible anticancer agents with their relationship between structure and activity, which will give insight into the future design of more active benzimidazole molecules. Result and Conclusion: The present review consists of synthetic protocols for the synthesis of benzimidazole derivatives along with their pharmacological potentials and structure-activity relationship in correlation with synthetic molecules to provide a depth view of the work done on benzimidazole. It would be significant for further research in the development of better drug molecules representing a potent derivative of medicinal agents.

The skin cancer has become a leading concern worldwide as a result of high mortality rate. The treatment modality involves radiation therapy, chemotherapy or surgery. More often combination therapy of chemotherapeutic agents gives better solution over single chemotherapeutic agent. The Globocon report suggested that high incidence and mortality rate in skin cancer is growing day-to-day. This type of cancer is more prevalent in that area where a person is highly exposed to sunlight. The nanotechnology-based therapy is nowadays drawing attention and becoming a more important issue to be discussed. The nanotherapy of skin cancer is dealt with various approaches and strategies. The strategic based approaches imply nanoparticles targeting carcinoma cells, functionalized nanoparticles for specific targeting to cancer cells, receptor-mediated active targeting as nanoshells, nanostrutured lipid carriers, liposome, ethosome, bilosome, polymeric nanoparticle, nanosphere, dendrimers, carbon nanotubes, quantum dots, solid lipid nanoparticles and fullerenes which are highly efficient in specific killing of cancer cells. The passive targeting of chemotherapeutic agents is also helpful in dealing with carcinoma due to enhanced permeability and retention effect (EPR).:The article outlines nano-based therapy currently focused globally, and the outcomes of the therapy as well.

Background: Oxadiazole emerged as an important class of heterocyclic compound with diverse biological activities like anticancer, antitubercular, anticonvulsant, anti-tubulin, antimicrobial, anti-inflammatory, antioxidant etc. Objective: The objective of this study is to synthesis series of twelve substituted N-[(1,3,4-oxadiazol-2- yl)methyl]benzamines (6a-l) and their evaluation as antiproliferative and antioxidant agents. Methods: The substituted N-[(1,3,4-oxadiazol-2-yl)methyl]benzamines (6a-l) analogues were synthesized as per the reported procedure. The antiproliferative activity was tested against nine different panels cancer cell lines (leukemia, colon, renal, non-small cell lung, breast, CNS, melanoma, prostate, and ovarian cancer) at 10 µM drug concentrations as per the NCI US Protocol. Results: 2-(5-((3-Chloro-4-fluorophenylamino)methyl)-1,3,4-oxadiazol-2-yl)phenol (6e) revealed the significant antiproliferative activity among the series of title compounds (6a-l). The compound, 6e showed maximum sensitivity towards CCRF-CEM, MCF-7, MOLT-4, T-47D, and SR cell lines with percent growth inhibitions (%GIs) of 79.92, 56.67, 39.62, 34.71 and 33.35, respectively. Furthermore, the compounds, 6e and 6c showed promising antioxidant activity with an IC50 value of 15.09 and 19.02 µM, respectively in DPPH free radicals (FR) scavenging activity.R Conclusion: The present study may support a significant value in cancer drug discovery programme.

Background: Pyrazoline is a heterocyclic compound of five rings, three carbon atoms, and two nitrogen atoms in a circle with just one endocyclic bond. Pyrazoline is one form of electron-rich nitrogen carrier, gaining popularity because it combines exciting electronic properties with the potential for dynamic applications. Many methods have been used in this research to synthesize pyrazoline derivatives to show a highly biological effect. Objective: The research of pyrazoline derivatives' biological activity has been a fascinating area of pharmaceutical chemistry. Pyrazolines are used in multifunctional applications. The current review of pyrazoline derivatives patent literature (2000-2021) describing the introduction, general method, and synthetic scheme on Anticancer activity has been discussed. Conclusion: Pyrazolines is a known heterocyclic compound. Pyrazoline is a five-membered ring containing three carbon and two nitrogen atoms nearby. Many approaches can be used to figure out their Synthesis. Numerous pyrazoline derivatives have been discovered to have an essential biological effect on anticancer activity, which has encouraged research in this area. The use of pyrazoline against cancer is a brilliant moiety and has an enormous scope of interest for the researchers to search more about this moiety.

Heterocyclic compounds are well known for their different biological activity. The heterocyclic analogs are the building blocks for synthesis of the pharmaceutical active compounds in the organic chemistry. These derivatives show various type of biological activity like anticancer, antiinflammatory, anti-microbial, anti-convulsant, anti-malarial, anti-hypertensive, etc. From the last decade research showed that the quinoline analogs plays a vital role in the development of newer medicinal active compounds for treating various type of disease. Quinoline reported for their antiviral, anticancer, anti-microbial and anti-inflammatory activity. This review will summarize the various synthetic approaches for synthesis of quinoline derivatives and to check their biological activity. Derivatives of quinoline moiety plays very important role in the development of various types of newer drugs and it can be used as lead compounds for future investigation in the field of drug discovery process.

Background: Cancer caused nearly 8.8 million deaths in 2015. Limited efficacy, selectivity, drug resistance and toxicity are major complications associated with chemotherapy, potentiating the discovery of anticancer agents. Methods: A new series of N-(7-hydroxy-4-methyl-2-oxoquinolin-1(2H)-yl)acetamide/benzamide analogues (5a-j) was prepared from the precursor, 7-hydroxy-4-methyl-2H-chromen-2-one (3), as anticancer agent. The structural assignment of quinolone analogues (5a-j) was based on spectroscopic data analyses. The cytotoxicity was tested on breast cancer cell lines (MCF7 and MDA-MB- 231) by sulforhodamine B (SRB) assay and three dose-related parameters GI50, TGI, and LC50 were calculated. Results: 2-(2-chlorophenoxy)-N-(7-hydroxy-4-methyl-2-oxoquinolin-1(2H)-yl)acetamide (5a) showed the most potent cytotoxicity against the MCF7 and MDA-MB-231 cancer cell lines with GI50 of 18.7 and 48.1 µM respectively. The glide scores of the compounds, 5a-d were found to be related to the cytotoxicity profile and the emodel scores for ligands, 5a-j were found to be related to significant cytotoxicity. Conclusion: Compound 5a exhibited the most potent cytotoxicity and this report may provide some predictions to design more potent novel quinolines as cytotoxic agents.

Convulsion generally occurs as a result of the diminishing concentration of GABA below a threshold level in the brain. This degradation pathway of GABA is catalyzed by the γ-aminobutyric acid amino transferase. The objective of the current study is to propose the binding interaction of 3a, 4-Dihydro-3-H-indeno [1, 2-C] pyrazole-2-Carboxamide/ Carbothioamides anticonvulsant analogs with a three-dimensional structural model of the γ -aminobutyric acid amino transferase. For a flexible type of molecular docking, we proposed that these molecules could successfully bind to the active pocket of the enzyme with good predicted affinities in comparison to standard vigabatrin. In this series, 4b, 4c, 4i, 4f and 4a showed significant binding free energy of -9.64, -9.31, -9.01, -8.99 and -8.29 with predicted inhibitory constant values of 0.086, 0.149, 0.237, 0.257 and 0.831 µM, respectively.

Tuberculosis (TB) remains as one of the most serious public health problems worldwide. It is one of the main causes of death in poor and developing countries, especially in sub-Saharan Africa, where it may be associated with the human immunodeficiency virus (HIV). It has been estimated that one third of the world population is infected by Mycobacterium tuberculosis (Mtb), and there were about 8.7 million new TB cases, and about 1.4 million yearly deaths due to TB in 2011. DOTS is the currently used drug therapy in TB but there is non-compliance which results in emergence of resistance. Bacille Calmette Guérin (BCG), an attenuated vaccine derived from Mycobacterium bovis, is the only licensed TB vaccine, but not recommended in HIV-infected infants. There are 14 vaccine candidates that have entered clinical trials and over 35 candidates in discovery and preclinical development. Mycobacterium indicus pranii [Mw; MIP] and M. vaccae are in phase III clinical trial and the Drug Controller of India licensed MIP for human use in India.

A series of 3-substituted-N-aryl-6,7-dimethoxy-3a,4-dihydro-3H-indeno(1,2-c)pyrazole-2-carboxamide analogues were synthesized and characterized by IR, NMR and elemental analysis. All the compounds were screened for anticancer activity as per National Cancer Institute (NCI US) Protocol on leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate and breast cancers cell lines. The compound 3-(4-fluorophenyl)-N-(2,6-dimethylphenyl)-6,7- dimethoxy-3a,4-dihydro-3H-indeno(1,2-c)pyrazole-2-carboxamide (4h) was found to be the most active compound of the series highly active on Leukemia K-562 and SR cell line (Growth Percent (GP) = 26.95 and 33.45 respectively). The molecular docking mode for compound, 3-(4-Fluorophenyl)-N-(2,6-dimethylphenyl)-6,7-dimethoxy-3a,4-dihydro-3H- indeno(1,2-c)pyrazole-2-carboxamide (4h) showed efficient binding with EGFR tyrosine kinase.

There has been considerable interest in the development of novel compounds with anticonvulsant, antidepressant, analgesic, anti-inflammatory, antiallergic, antipsychotic, antimicrobial, antimycobecterial, antitumour, antiviral and antitubercular activities. 1,3,4-oxadiazoles constitute an important class of compounds for new drug development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their biological activities. These observations led to the development of new 1,3,4-oxadiazole derivatives. This review article describes the various biological activities associated with 1,3,4-oxadiazole ring system and is useful in guiding the researchers across the world working on this moiety and consequently have been instrumental in the advancement of 1,3,4-oxadiazole chemistry.