: The incidence of cancer is increasing worldwide, affecting a vast majority of the human population. As new different anticancer agents are being developed now, the requirement is to deal somehow with them and evaluate their safety. Among them, pyridine based drugs are contributing a lot, as it is one of the imperative pharmacophores occurring synthetically as well as naturally in heterocyclic compounds, and having a wide range of therapeutic applications in the area of drug discovery, thereby offering many chances for further improvement in antitumor agents via acting onto numerous receptors of extreme prominence. Many pyridine derivatives have been reported to inhibit enzymes, receptors and many other targets for controlling and curing the global health issue of cancer. Nowadays, in combination with other moieties, researchers are focusing on the development of pyridine-based new derivatives for cancer treatment. Therefore, this review sheds light on the recent therapeutic expansions of pyridine together with its molecular docking, structure-activity-relationship, availability in the market, and a summary of recently patented and published research works that shall jointly help the scientists to produce effective drugs with the desired pharmacological activity.
The objective of this review was to study the novel methods to the omeprazole synthesis and pharmaceutical impurities of proton pump inhibitors that provide an insight to researchers about the development of proton pump inhibitors. However, this paper emphasized on the study of various pharmaceutical impurities of anti-ulcer drug. The drug used for the study was omeprazole which is chemically known as (5-methoxy-2-[[(4-metboxy-3,5dimethylpyridinyl) methyl] sulfinyl]-l-benzimidazole) that inhibits gastric ATPase enzyme by oxidizingits sulfhydryl groups.The process involved during synthesis. The novel process come into existence due to incomplete oxidation of pyrmetazole and overoxidation to sulfone that leads to the formation of sulfone N-oxide. The procedure involved 5-methoxy thiobenzimidazole to the formation of an ester followed by coupling of the ester with the Grignard reagent of 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine. The novel synthesis process for pharmaceutical impurities achieve the expected yield and process observed to be short, simple. The synthesized impurity of proton pump inhibitors can be used as standard impurity, that can be utilized for further studied in various aspects. This review article will describe about the various novel impurities of omeprazole that available as marketed formulation.
Terpenoids are naturally occurring secondary metabolites that consist of isoprene units (i.e., 2-methyl-1,3-butadiene). Terpenoids became recognized because of their diverse pharmacological benefits, such as anti-cancer, anti-inflammatory, antioxidant, analgesic, antibacterial, antifungal, hepatoprotective, antiviral, and antiparasitic activities. But most of these compounds have limited lipophilicity, dissolution rate, aqueous solubility, and drug permeability, so they are not used effectively. The low bioavailability significantly interferes with the performance of terpenoids to cure diseases, and the absorption process of terpenoids also becomes disrupted; therefore, their bioavailability in the blood becomes insufficient to achieve optimal treatment activity. Thus, to overcome this limitation, some strategies are used, such as nanotechnology (nanoparticles, carrier complexation), cocrystal, and glycosylation. Thus, this review summarizes the chemistry of terpenoids, factors that limit the bioavailability of terpenoids, and strategies employed to date with their design principles and outcomes possibly increasing their bioactivity.
Background: Flavonoids are a class of polyphenolic bioactive compounds obtained from plants, which have a wide range of chemical structures and properties. More than 9000 distinct flavonoid molecules have been identified, and have been found to regulate numerous developmental processes and play key biological roles in living organism. Objective: This review aims to highlight the hepatoprotective potentiality of flavonoids and co-relate their pharmacological activity with their chemical structure. Methods: With advancement in the field of research related to phytochemicals, it is evident that flavonoids have versatile health benefits, viz., antioxidant property, free radical scavenging capacity, anticancer activity. The basic structures are C6—C3—C6 rings with various substitution patterns, resulting in a succession of subclass compounds, and the relationships between chemical structures and bioactivity have previously been investigated. Results: The hepatoprotective effects of bioactive flavonoids derived from plants have been widely linked to their antioxidant activity, antiinflammatory activity, effects on sterol regulatory element-binding proteins (SREBP), peroxisome proliferator-activated receptor gamma (PPARγ) receptors, and inflammatory mediator cytokines according to numerous studies. The C2-C3 double bond at the A ring, as well as the hydroxyl groups of C3′or C4′, and the carbonyl group at position C4,have been shown to augment their hepatoprotective activities; however, hydroxymethylation at C3′ and C4′ has been found to diminish the hepatoprotective activity. Conclusion: The impact of flavonoid moieties and the structure-activity relationship of flavonoids related to combating various hepatic disorders have been vividly discussed in this review paper.
Background: Trapa natans L., is annual aquatic plant generally kwon as Water caltrp, Water chest nut belonging to the Trapaceae or Lytraceae family. Trapa natans L is use for the treatment of wide no of diseases without proper standardization. Objective: To give the right pharmacognostical and photochemical information of the Trapanatan L leaves. In this study pharmacognostical investigation of the fresh leaves and powder drug were done to determine the macroscopical, microscopical, quantitative physicochemical and phytochemical property of the drugs. Method: Macroscopical, quantitative and qualitative microscopy, physicochemical evaluation, extractive value, florescence analysis and phytochemical analysis were done according to the WHO guideline. Result: Macroscopical analysis showed that, leaves are greenish to purplish color, rhomboidal shape; alternate, acute, margin is dentate, pinnate venation. Microscopic evaluation showed that leaf is dorsi ventral in nature, upper layer epidermis cells were covered with cuticle layer. Single layer of barrel shape cell were present bellow the upper epidermis layer. Trichomes are generally multicellular. Anomocytic stomata were observed in upper epidermis. From the experiment it was found that methanolic extract give the highest extractive value. Phytochemical analysis gives the evidence for the presence of carbohydrate, alkaloids, glycoside, steroids, flavonoids, tannin, and triterpenoids. Qualitative phytochemical analysis give the evidence for presence of high amount total phenolic content. Conclusion: Different pharmacognostical parameters assessed in this examination help to detection and standardization of Trapa natans L., leaves.
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