scholarly journals Development of Phenothiazine Hybrids with Potential Medicinal Interest: A Review

Molecules ◽  
2022 ◽  
Vol 27 (1) ◽  
pp. 276
Author(s):  
Marina C. Posso ◽  
Fernanda C. Domingues ◽  
Susana Ferreira ◽  
Samuel Silvestre
Keyword(s):  
Drug Resistance ◽  
Biological Activity ◽  
Biological Activities ◽  
New Drugs ◽  
Present Review ◽  
Multi Drug Resistance ◽  
Phenothiazine Derivatives ◽  
Bioactive Scaffolds ◽  
Drug Candidates ◽  
Resistance Reversal

The molecular hybridization approach has been used to develop compounds with improved efficacy by combining two or more pharmacophores of bioactive scaffolds. In this context, hybridization of various relevant pharmacophores with phenothiazine derivatives has resulted in pertinent compounds with diverse biological activities, interacting with specific or multiple targets. In fact, the development of new drugs or drug candidates based on phenothiazine system has been a promising approach due to the diverse activities associated with this tricyclic system, traditionally present in compounds with antipsychotic, antihistaminic and antimuscarinic effects. Actually, the pharmacological actions of phenothiazine hybrids include promising antibacterial, antifungal, anticancer, anti-inflammatory, antimalarial, analgesic and multi-drug resistance reversal properties. The present review summarizes the progress in the development of phenothiazine hybrids and their biological activity.

Synthesis and Biological Activity of Hydrazones and Derivatives: A Review

2020 ◽  
Vol 20 (5) ◽  
pp. 342-368 ◽  
Author(s):  
Juliana de Oliveira Carneiro Brum ◽  
Tanos Celmar Costa França ◽  
Steven R. LaPlante ◽  
José Daniel Figueroa Villar
Keyword(s):  
Biological Activity ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
New Drugs ◽  
New Drug ◽  
Cancer Inflammation

Hydrazones and their derivatives are very important compounds in medicinal chemistry due to their reported biological activity for the treatment of several diseases, like Alzheimer’s, cancer, inflammation, and leishmaniasis. However, most of the investigations on hydrazones available in literature today are directed to the synthesis of these molecules with little discussion available on their biological activities. With the purpose of bringing lights into this issue, we performed a revision of the literature and wrote this review based on some of the most current research reports of hydrazones and derivatives, making it clear that the synthesis of these molecules can lead to new drug prototypes. Our goal is to encourage more studies focused on the synthesis and evaluation of new hydrazones, as a contribution to the development of potential new drugs for the treatment of various diseases.

Quantitative structure-activity relationship model, molecular docking simulation and computational design of some novel compounds against DNA gyrase receptor.

2020 ◽  
Vol 16 ◽  
Author(s):  
Shola Elijah Adeniji
Keyword(s):  
Biological Activity ◽  
Molecular Docking ◽  
Binding Energy ◽  
Biological Activities ◽  
Docking Simulation ◽  
Dna Gyrase ◽  
Computational Design ◽  
Multi Drug Resistance ◽  
Drug Candidate ◽  
Standard Drug

Introduction: Mycobacterium tuberculosis has instigated a serious challenge toward the effective treatment of tuberculosis. The reoccurrence of the resistant strains of the disease to accessible drugs/medications has mandate for the development of more effective anti-tubercular agents with efficient activities. Time expended and costs in discovering and synthesizing new hypothetical drugs with improved biological activity have been a major challenge toward the treatment of multi-drug resistance strain M. tuberculosis (TB). Meanwhile, to solve the problem stated, a new approach i.e. QSAR which establish connection between novel drugs with a better biological against M. tuberculosis is adopted. Methods: The anti-tubercular model established in this study to forecast the biological activities of some anti-tubercular compounds selected and to design new hypothetical drugs is subjective to the molecular descriptors; MATS7s, SM1_DzZ, SpMin4_Bhv, TDB3v and RDF70v. Ligand-receptor interactions between quinoline derivatives and the receptor (DNA gyrase) was carried out using molecular docking technique by employing the PyRx virtual screening software and discovery studio visualizer software. Furthermore, docking study indicates that compounds 20 of the derivatives with promising biological activity have the utmost binding energy of -17.79 kcal/mol. Results: Meanwhile, the interaction of the standard drug; isoniazid with the target enzyme was observed with the binding energy -14.6 kcal/mol which was significantly lesser than the binding energy of the ligand (compound 20).Therefore, compound 20 served as a template structure to designed compounds with more efficient activities. Among the compounds designed; compounds 20p was observed with better anti-tubercular activities with more prominent binding affinities of -24.3kcal/mol. Conclusion: The presumption of this research aid the medicinal chemists and pharmacist to design and synthesis a novel drug candidate against the tuberculosis. Moreover, in-vitro and in-vivo test could be carried out to validate the computational results.

Polyprodrug with Glutathione Depletion and Cascade Drug Activation for Multi-drug Resistance Reversal

Biomaterials ◽  
2021 ◽  
pp. 120649
Author(s):  
Xuan Xiao ◽  
Kewei Wang ◽  
Qingyu Zong ◽  
Yalan Tu ◽  
Yansong Dong ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Glutathione Depletion ◽  
Multi Drug Resistance ◽  
Resistance Reversal ◽  
Drug Activation

Synthesis and Biological Evaluation of C-Aromataxane Derivatives as P-Glycoprotein-Mediated Multi Drug Resistance Reversal Agents

Heterocycles ◽  
2015 ◽  
Vol 90 (1) ◽  
pp. 482
Author(s):  
Takayuki Doi ◽  
Naoko Yamaguchi ◽  
Kosuke Ohsawa ◽  
Kazuoki Nakai ◽  
Masahito Yoshida ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Biological Evaluation ◽  
Multi Drug Resistance ◽  
Reversal Agents ◽  
P Glycoprotein ◽  
Resistance Reversal ◽  
Synthesis And Biological Evaluation

Identification of promising objects for the synthesis of thiosulphonate derivatives of benzoquinone and hydroquinone

2021 ◽  
Vol 4 (2) ◽  
pp. 47-53
Author(s):  
N. Y. Monka ◽  
◽  
N. E. Stadnytska ◽  
I. R. Buchkevych ◽  
K. O. Kaplia ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Experimental Studies ◽  
New Drugs ◽  
Reduced Form ◽  
Free Form ◽  
Wide Range ◽  
On Line ◽  
Living Organisms ◽  
Derivatives Of

Benzoquinone and its reduced form hydroquinone belong to phenolic compounds and are found in living organisms in free form or in glycosides. They are active substances of some medicinal plants and have a pharmacological effect on the human body. Accordingly, their derivatives are important objects for chemical synthesis and development of new drugs. This article presents the findings of the structural design of substances with benzoquinone or hydroquinone fragment and sulfur-containing compound. By use of appropriate on-line programs a predictive screening of the biological activity and cytotoxicity of thiosulfonate derivatives of benzoquinone and hydroquinone has been conducted. It has been found that they have immense methodological potential to be synthesized by substances with a wide range of biological activities and a high value of probable activity, which substantiates the feasibility of conducting experimental studies on their biological activity, particularly anticancer.

A Review: Therapeutic and Biological Activity of Benzothiazole Derivatives

2017 ◽  
Vol 4 (3) ◽  
Author(s):  
Suresh Choudhary ◽  
G Jeyabalan ◽  
Naresh Kalra
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
New Products ◽  
Therapeutic Agents ◽  
Present Review ◽  
Benzothiazole Derivatives ◽  
Anti Inflammatory

The Benzothiazole nucleus is present in compounds involved in research aimed at evaluating new products that possess interesting biological activities, such as antitumor, antimicrobial, anthelmintic, antileishmanial, anticonvulsant and anti-inflammatory. The present review focuses on the benzothiazoles with potential activities that are now in development. The synthesized benzothiazole derivatives could be considered as lead molecule for the development of therapeutic agents.

Extra-Pulmonary TB

2021 ◽  
pp. 91-116
Author(s):  
Sarita Rani ◽  
Ankur Kaul ◽  
Anil Kumar Mishra ◽  
Umesh Gupta
Keyword(s):  
Drug Resistance ◽  
Polymeric Micelles ◽  
New Drugs ◽  
Multi Drug Resistance ◽  
Liposomal Formulations ◽  
Extra Pulmonary ◽  
Stability Issues ◽  
Low Solubility ◽  
Line Drug ◽  
Extensively Drug Resistance

Tuberculosis is considered a fatal respiratory disease commonly seen in developing countries. This chapter includes the global scenario of TB patients and brief description of TB history, its pathogenesis, types, diagnosis tests, emergence of MDR (multi drug resistance) and XDR (extensively drug resistance). The traditional chemotherapy of TB includes first and second line drug therapy. These lines of therapies face many difficulties such as low solubility, low bioavailability, and stability issues. Therefore, some new drugs were introduced in the market that showed effective results to the patients. Nanoparticulate drug delivery gained much focus in recent years due to its advantages and ideal characteristics. Numerous nanoparticles, liposomal formulations, and polymeric micelles were reported by the researchers with significant and considerable results. Inhalable formulations were also prepared by scientists that showed effective and remarkable anti-tuberculosis action on TB patients. Many efforts are awaited to completely eradicate TB from the planet.

Phenothiazines and Related Drugs as Multi Drug Resistance Reversal Agents in Cancer Chemotherapy Mediated by p-glycoprotein

2017 ◽  
Vol 13 (1) ◽  
Author(s):  
Ravinesh Mishra ◽  
Swati Sareen ◽  
Bhartendu Sharma ◽  
Shubham Goyal ◽  
Gurpreet Kaur ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Cancer Chemotherapy ◽  
Multi Drug Resistance ◽  
Reversal Agents ◽  
P Glycoprotein ◽  
Resistance Reversal

Application of nanoparticles to reverse multi-drug resistance in cancer

2016 ◽  
Vol 5 (5) ◽  
Author(s):  
Jie Yang ◽  
Haijun Zhang ◽  
Baoan Chen
Keyword(s):  
Drug Resistance ◽  
Side Effects ◽  
Conventional Method ◽  
Therapeutic Agents ◽  
Present Review ◽  
Multi Drug Resistance ◽  
Long Period

AbstractMulti-drug resistance (MDR) poses a large obstacle to various human malignancies. For a long period, combination of multiple therapeutic agents has been the conventional method used to reverse MDR in cancer. However, it is still not an effective method as rather than cancer its serious side effects causes patient’s death. Nanoparticles (NPs) are emerging as a class of therapeutics for cancer, including overcoming MDR. In the present review, we focus on the application of NPs to reverse MDR in cancer. Several kinds of NPs developed for the reversal of MDR are summarized. In addition, investigations

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