This book has been designed by authors mainly based on the synthesis of hydrazone derivatives and including the recent development in the field of chemistry. We have conferred about the mechanism and pathogenesis of the disease. New to the book Tuberculosis. Drug Design. QSAR. Biological Evaluation. This book useful for those who are student of chemistry, Pharmaceutical Sciences, Cheminformatics and Life Sciences.
The present book with title ‘Synthesis and biological screening of thiazoline 2(3H) thione’ includes very informative note on design, synthesis and screening of novel thiazoline 2(3H) thione as potential antitubercular agents which is very important for M.pharm, Ph.D. and academic researcher who are angage with antitubecular drug discovery process. This book also included the review of novel target for tuberculosis and some heterocycles as antitubercular agents.
Quinazolinone is a versatile lead molecule for designing potential bioactive agents. Quinazolinone and its derivatives are gaining prominence through their varied biological and pharmacological properties. This book provides comprehensive synthetic methods, characterisation and biological evaluation of Quinazolinone and its derivatives. The topics covered include the review of Quinazolinones, schemes of synthesis, physical and spectral characteristics and biological evaluation. This book will be useful for the students and researchers who are involved in the synthesis of this type of heterocyclic compounds.
The work mainly concerns about computational molecular modeling techniques, which can be used for the study of complexes between ligands and biomacromolecules (proteins). Characterizations of such interactions lead to the understanding of biological function of biomacromolecules and therapeutic effect of drugs, therefore interest of many laboratories is focused on such study. In this work I present application of molecular modeling techniques for the interactions of antitubercular compounds with modeled type II NADH: Menaquinone oxidoreductase protein, which is responsible for the micro-organism to grow in absence of oxygen. Our results contribute to the better understanding of the mechanism of biological activity antitubercular drug. The extent of this research requires complex approach involving several experimental and computational techniques, but also about their combination with experimental techniques in the field of the study ligand/biomacromolecules interactions.
Mannich bases are important compounds due to their wide range of biological and industrial applications. Schiff’s and Mannich bases of isatin possess versatile activities like antimicrobial,antiviral,anticancer, antitubercular activities etc. References show heterocyclic compounds containing coumarin to exhibit activities such as antimicrobial, antiviral, antitubercular, antipyretic, antiinflammatory and antioxidant activities and isonoazid to be an excellent antitubercular agent. In the light of these interesting biological activities the present work was carried out with view of synthesizing some isatin based Mannich bases from coumarin and isoniazid. Nowadays microwave mediated synthesis has gained importance in organic synthesis. In this current study, microwave assisted parallel synthesis along with the conventional method was opted for synthesizing Schiff’s and Mannich bases of isatin and their efficacies based on the percentage yield and consumption of time for synthesis by each method were compared. The structure of the compounds synthesised has been confirmed by IR, 1H NMR and mass spectral data.All the compounds were screened for antimicrobial and antioxidant activity.
Work documented here is about the synthesis and biological activities evaluation of Quinazolin-4(3H)-one based heterocyclic compounds. Chapter 1 provides detail introduction of Quinazolin-4(3H)-one alkaloids. Chapter 2 & 3 describe synthetic approaches for the synthesis and functionalization of Quinazolin-4(3H)-ones, while chapter 4 explains the biological activities evaluation of Quinazolin-4(3H)-ones and their analogs.
This book helps to new researchers to synthesize new quinoxaline compound which shows various biological activities. Also it helps for QSAR study of quinoxaline compounds. In this book detailed methods of synthesis has been given also this book comprises spectral analysis of compounds like IR, NMR and Mass analysis of synthesized compounds. Also we have given XRD analysis and single crystal study of some quinoxaline compounds
This book describes about the QSAR studies of very prominent cancer target that is histone deacetylase inhibitors. Histone deacetylase is a protein which plays a crucial role in cancer cells proliferation and differentiation. In this books some favorable situations has been describes for the possible targets for anti cancer agents. For this purpose 2D and 3D QSAR studies have been performed and described.
The present book on "Introduction and review of Anti tubercular agents" is very informative for the M. Pharm. Ph.D. and academic/Industry researcher who can exhaustively engage with drug discovery of anti-tubercular agents.This book includes Introduction of tuberculosis with some novel targets for tuberculosis drug therapy and review of some novel heterocycles which exhibited excellent anti tubercular activity.
We carried out a QSAR study on benzotriazine derivatives & studied 28 potent GABAA receptor ligands; derivatives of benzotriazines, using a combination of various physicochemical, steric, electronic and thermodynamic descriptors to determine the quantitative correlation between binding affinity and structural features with potent anticonvulsant activity. Correlation between these properties and anticonvulsant activity was used to synthesize compounds possessing potent anticonvulsant activity. Most of the compounds showed an ability to inhibit the maximum electroshock (MES) and pentylenetetrazole (PTZ)-induced convulsions. Compound 1A, i.e. 2-(4-Chloro-phenyl)-5-nitro-1H-benzimidazole exhibited maximum activity.
Diabetes is the most common form of diabetes, accounting for over 90% of cases. Current treatment approaches for diabetes include diet, exercise, and a variety of pharmacologic agents, including insulin. The work is an attempt to generate predictive QSAR models based on QSAR method and to find the structural features of dipeptidyl peptidase IV inhibitors to guide the rational synthesis of activity. The developed models provide insight into the influence of various interactive fields on the activity and, thus, can help in designing and forecasting the dipeptidyl peptidase IV inhibitors. In each series, significant correlations are found between the inhibition potencies of specific dipeptidyl peptidase IV inhibitors and some physicochemical and lipophilicity, hydrophobic parameter of the compounds explained by different regression equations. Our results contribute to the better understanding of the mechanism of biological activity antidiabetic drug.
Arun Joshi is one of the most prolific writers in Indian writing in English who used his art as a wepon to resolve the society.This book gives clear picture of Arun Joshi's vision of life. The Author attempts to record Joshi's "exploration of mysterious under world which the human soul". The book offers a comprehensive critical analysis of Arun Joshi's novels. The central focus of Arun Joshi's fiction is in the 'self' irretrivably lost in the labyrinth of industrialized and dehumanized society. the protagonist of Arun Joshi feels helpless, isolated and dispossessed. In all five chapters of the book, the major concerns of Arun Joshi viz., existential predicament, alienation, dispossession, rootlessness have been discussed.
The development of new therapies to treat hypertension effectively is currently an intensive area of research. To achieve this objective quantitative structure activity relationship (QSAR) study was carried out on a reported series of phthalazine derivatives as alpha-1d antagonist, as it provides the rationale for the changes in the pharmacophore to have more potent and less toxic analogue. In this article, we report 2D and 3D QSAR studies for the set of 20, alpha-1d antagonist. A simple and convenient procedure has been developed for the synthesis of Novel 1 phthalazinone and 1, 4phthalazinedione derivatives using Schotten–Baumann reaction and Gabriel Michael reaction respectively. All compounds have been characterized by IR, NMR,and MASS spectroscopy.
The book is an attempt to study the synthesis of heterocycles with novel chromophores as potential antimicrobial agents. The phthalazine based scaffolds having different heterocyclic chromophores includes diversity with five groups, phthalazine-methoxyacrylates, phthalazine-oxadiazoles, phthalazine-isoxazoles, phthalazine-methoxyacrylate-isoxazoles and phthalazine-triazolothiadiazole and triazolothiadiazines. Further, 114 compounds were tested for antimicrobial activity against Esherichia coli, Salmonella typhi, Bacillus subtilis and Staphylococcus aureus. The thiazole and pyridine substituted derivatives shows better activity. All the compounds were thoroughly characterized with all possible physic-chemical techniques.
The objective of drug discovery phase is to synthesize lead compounds, new analogs with improved potency, reduced off target activities and physio-chemical/metabolic properties suggestive of reasonable in-vivo pharmacokinetics. The goal of present work is to design drug with minimum side effect and maximum potency. 2D QSAR is planned using Multiple Linear Regression Analysis, for achieving the goal, which can help in recognizing the important descriptor that can help in increasing the potency of anticancer drug.