11 research outputs found
Substituted Thiazole Linked Murrayanine-Schiff�s Base Derivatives as Potential Anti-Breast Cancer Candidates: Future EGFR Kinase Inhibitors
No full textCancer is the second leading causes of mortality across the planet which has had affected millions. In spite of massive efforts in producing new molecules and chemotherapeutic approaches for managing cancer, it continued to be the global threat. Small hybrid molecules have gained popularity in chemotherapy due to their potential and smart characteristics in modulating biological targets. The present research attempts in developing few novel hybridized derivatives of murrayanine (an active carbazole derivative) by the semi-synthetic approach to form substituted thiazole linked murrayanine-Schiffs base derivatives. The protocol involved murrayanine 1 as the template material for constructing a hybridized Schiffs base intermediate 3, which further by Hantzchs cyclization was subsequently converted to various hybridized thiazoles analogs 5a-5f. The purity of the synthesized compounds was ascertained by sophisticated analytical techniques. The anti-cancer potential was screened against breast cancer cell lines; MCF-7 and MDA-MB-231 by Sulforhodamine B (SRB) assay. The compound 5b displayed most potent anti-proliferative activity with IC50 values of 23.41?M against MCF-7 cell line and 32.15?M against MDA-MB-231 cell line. It has been observed that analogs having electron withdrawing substituents exhibited pronounced anticancer activity. The docking study was performed by Autodock Vina where the results were found to be in full agreement with the cytotoxic study, depicting that the probable cytotoxic outcome by EGFR inhibitory mechanism. The study revealed the potential of novel hybridized derivatives as active anti-breast cancer candidates. The research will encourage (medicinal) chemists in rationally designing of semi-synthetic analogs of a heterocyclic prototype having pronounced anti-cancer activity.</jats:p
An electrode comprising of graphene nanopowder inserted in an enclosed structure in anodic aluminium oxide coated with PANI by using low temperature hydrothermal process
No full text
Anti-microbial Perspective of a Chalcone, (E)-1-(1-methoxy-9H-carbazol-3-yl)-3-(4-(methylsulfonyl) phenyl)prop-2-en-1-one: Fabrication of a Hybrid by Unification of a Natural Product with a Synthetic Component
No full textMurraya koenigii L. has been explored exhaustively and is known to possess more than 20 different carbazole-based alkaloids having multifarious therapeutic perception of this class of alkaloids, murrayanine is the highest explored alkaloid and is known to have (ethno)-pharmacological perspectives of purgative, astringent, febrifuge, anti-helminthic, anti-oxidant, anti-ulcerogenic, immunomodulation, etc. As murrayanine possess multiple sites for substituting wide-range of electron-donating / -withdrawing groups by semi-synthetic approach, in the present research, a chalcone; (E)-1-(1-methoxy-9H-carbazol-3-yl)-3-(4-(methylsulfonyl)phenyl)prop-2-en-1-one was fabricated rationally by incorporating a natural portion (murrayanine) in the A-ring and a synthetic component (4-methylsulfonyl group) in the B-ring and screened against two bacterial species (Escherichia coli and Staphylococcus aureus) and two fungal species (Candida albicans and Aspergillus niger). The rationally designed chalcone demonstrated noteworthy anti-microbial activity. The fabricated chalcone was observed to be a better anti-bacterial agent as compared to its anti-fungal potentials. As compared to the standard drugs, the experimental molecule does hold well against pathogenic challenges. The present research therefore opened new avenues of judiciously developing a natural scaffold having an active methylsulfonyl group, which will inspire life science researchers across the globe in developing inhibitors with pronounced biological activity as compared with the parent compounds
Anti-microbial Perspective of a Chalcone, (E)-1-(1-methoxy-9H-carbazol-3-yl)-3-(4-(methylsulfonyl)phenyl)prop-2-en-1-one: Fabrication of a Hybrid by Unification of a Natural Product with a Synthetic Component
No full textMurraya koenigii L. has been explored exhaustively and is known to possess more than 20 different carbazole-based alkaloids having multifarious therapeutic perception. Of this class of alkaloids, murrayanine is the highest explored alkaloid and is known to have (ethno)-pharmacological perspectives of purgative, astringent, febrifuge, anti-helminthic, anti-oxidant, anti-ulcerogenic, immunomodulation, etc. As murrayanine possess multiple sites for substituting wide-range of electron-donating / -withdrawing groups by semi-synthetic approach, in the present research, a chalcone; (E)-1-(1-methoxy-9H-carbazol-3-yl)-3-(4-(methylsulfonyl)phenyl)prop-2-en-1-one was fabricated rationally by incorporating a natural portion (murrayanine) in the A-ring and a synthetic component (4-methylsulfonyl group) in the B-ring and screened against two bacterial species (Escherichia coli and Staphylococcus aureus) and two fungal species (Candida albicans and Aspergillus niger). The rationally designed chalcone demonstrated noteworthy anti-microbial activity. The fabricated chalcone was observed to be a better anti-bacterial agent as compared to its anti-fungal potentials. As compared to the standard drugs, the experimental molecule does hold well against pathogenic challenges. The present research therefore opened new avenues of judiciously developing a natural scaffold having an active methylsulfonyl group, which will inspire life science researchers across the globe in developing inhibitors with pronounced biological activity as compared with the parent compounds
On the Cognitive Process of Abstraction
No full textAbstractConcepts are the basic elements of propositions. Concepts can be best understood as constituted by its subset of objects (Extent) and subset of attributes (Intent). Psychological capacities of human mind for example, learning, thinking, memorizing can be performed by concepts and their association. In this paper, we will explain how human will be able to generalize concrete concepts of Formal Concept Analysis into abstract concepts. In particular, we model the functionalities of concept algebra by making use of Formal Concept Analysis; we illustrate the proposed model with experiments on sample context. This model simulates the thinking process of human mind
Anti-inflammatory potentials of some novel Murrayanine containing 1, 3, 4-Oxadiazole derivatives
No full textMurrayanine-Chalcone Transformed into Novel Pyrimidine Compounds Demonstrated promising Anti-Inflammatory Activity
No full textAnxiolytic activity of some 2, 3-dihydrobenzo[b] [1, 4] oxazepine derivatives synthesized from Murrayanine-Chalcone
No full textDevelopment of mosquito repellant gel formulations from various natural volatile oils: comparative study with the marketed formulation odomos®
No full textDEET based mosquito repellents were found to be comparatively harmful to the person suffering from urea cycle disorders such as ornithine transcarbamylase (OTD) deficiency and, are therefore, contraindicated in individuals. These situations lead to the budding necessity of natural mosquito repellents which will have inexpensive, effectual, non-toxic, environment-friendly, and biodegradable attributes. Inspired from the upcoming global need, a carbopol 940 based mosquito repellant gel formulation was prepared from the essential oils of Cymbopogon nardus, Murraya Koenigii, Cymbopogon citratus, Tridax procumbens, Eucalyptus globules, and Azadirachta indica, and further evaluating them for their appearance, pH, viscosity, spreadability, extrudability, swelling index, and accelerated studies. The mosquito repellent potential was evaluated and simultaneously compared with the positive control (Odomos®). In several developing nations, where the majority of the people do not have access to mosquito net, high-cost mosquito repellant creams, and miscellaneous physical methods, this gel formulation may be an effective, inexpensive, and easily accessible way to prevent mosquito-borne diseases, like malaria, dengue, etc. in the lower sections of the society.
Keywords: Mosquito, Repellent, Malaria, Gel, Formulation, DEET
