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.
Life threatening infections caused by pathogenic fungi are becoming increasingly common, especially in individuals with suppressed immune systems. However, there are only a limited number of antifungal drugs available for such infections, which leads to a strong need to develop new classes of compounds having antifungal activity. From the literature survey; it was found that there has been a lot of research going in the field of novel antifungal drug development. It was found that many antifungal agents contain benzimidazole moiety in their structure. Therefore benzimidazole was selected for the development of new chemical entities as potential antifungal agents. Fifteen derivatives of benzimidazole were synthesized using different substituted phenol as a side chain. Synthesized compounds were characterized by chromatographic methods, Infrared spectroscopy and Nuclear Magnetic Resonance spectroscopy for their structural confirmation. These compounds were tested for antifungal activity. Furthermore, these benzimidazole derivatives were subjected to QSAR study. These compounds provide a preliminary insights into newer antifungal agents and which can help further modification.
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.
A series of newer 3-(4'-methoxyphenyl)-5-substituted phenylisoxazoles derivatives have been synthesized by reacting hydroxylamine hydrochloride with chalcone. The chalcones were formed by reacting different aromatic aldehydes with 4-methoxyacetophenone in presence of aqueos KOH. The acute toxicity study was carried on all the synthesized compounds and they were screened for their anti-inflammatory activity by carrageenan induced paw edema method. Anti-inflammatory studies showed statistically significant activity when compared to control indomethacin. The two most potent compounds giving good anti-inflammatory activity were further evaluated for their anti-ulcer activity. The compounds were subjected to docking and quantitative structure activity relationships (QSAR) studies.
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.
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.
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 book describes the synthesis of schiff bases possessing pyrazole derivatives. The synthesized entities were characterized for their formation using spectral techniques viz. IR and NMR. The derivatives were tested for their antimicrobial results and were compared with 5 different standard drugs available in the market. The compounds, thus synthesized were found to be good antimicrobial agents. The derivatives synthesized can be further optimized to generate lead for the better future of the society.
A newly synthesized compounds bis dihydroxy diones having varied pharmacological activities such as various biological activities such as antioxidant , antitumors, antibacterial,anti-inflammatory and also shown to display anti-tumor activities. Based on the importance of these ring system, our attention attracted towards synthesis of new molecules constituted with ?-Diketones as well as pymiridine rings and study their biological activity.
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.
Research in the field of heterocyclic and carbohydrate chemistry has experienced a remarkable surge in recent years due to their variety in structure, chemical reactivity and their pervasive presence in nature. Number of chemotherapeutic agents has been emerging from these classes of compounds against various diseases including tuberculosis and lymphatic filariasis. These two diseases are posing a major public health problem mostly in developing countries. This book describes the design and synthesis of novel bioactive heterocyclic and carbohydrate derivatives and different techniques which are being employed for investigating antitubercular and antifilarial activities. This book also provides the structural elucidation of many heterocyclic and carbohydrate based molecules in detail using IR, NMR and mass spectroscopy. This book would be beneficial for advanced undergraduates and graduates, who are at the beginning of their research careers. It will also be very useful as a reference book for research scholars and medicinal chemist.
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.
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.
The present investigation is concerned with synthesis of new 2 and 6 - substituted 4H-chromen-4-One derivatives with the objectives of discovering novel and potent anti-inflammatory agents and anti-oxidants. The results of anti-inflammatory activity were revealed that the compound has indole 2 substitution with 4-nitrophenyl amino methyl (at 6th position) on 4H- chromen–4–one having more anti-inflammatory activity as compared to other substituent’s. While, indole 2 substituted 4-methoxy phenyl amino methyl (at 6th position) 4H–chromen–4–one showed outperformed anti-oxidant activity in different anti-oxidant model as compared to other substituent’s. The all newly synthesized compounds displayed moderate to potent anti-inflammatory and anti-oxidant activity and has therapeutic potential in combating this devastating inflammatory and oxidative condition of the body, might be deserve promising substances for further in vivo evaluation as anti-inflammatory and anti-oxidant properties. However the anti-inflammatory activity is not related to antioxidant potential.
This work was done by Arpita Patel under the guidance of Assoc. prof. of Dr. Badmanaban R. and Prof. Dr. Dhrubojyoti Sen and with the help of Dr.Chhaganbhai N. Patel Head of Pharmaceutical Chemistry department & principal of institute Shri Sarvajanik Pharmacy College. This work was started with the thought of the treatment of many infectious diseases are challenging due to resistance to antimicrobial agents. It is necessary to continue the search for new antibacterial agents. Multi drug treatment of inflammatory conditions associated with microbial infections posses a unique problem especially for patients with impaired liver or kidney functions. Hence, mono therapy with a drug having both anti-inflammatory and antimicrobial activities is highly desirable. Encouraged by these observations and in continuation of the research on the synthesis of five membered heterocyclic compounds such as pyrazole will give a good impact.