Synthetic Studies in Antimycobacterial Agents Based on Carbohydrates and Heterocycles
IR@CDRI: CSIR-Central Drug Research Institute, Lucknow
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| Creator |
Singh, B K
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| Date |
2014-09-10T06:58:57Z
2014-09-10T06:58:57Z 2008 |
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http://hdl.handle.net/123456789/1399
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| Description |
Guide- Dr. R. P. Tripathi, Phd Thesis Submitted to Dr. Ram Manohar Lohia Avadh University, Faizabad in 2008
Medicinal chemistry, an important branch of science, serving the mankind to overcome conditions unfavorable for their survival has fascinated the scientific community throughout the world. In the present scenario, development of new technologies in all branch of sciences and their amalgamation have outominated in new materials and products both for physical and biochemical use. The most abundant source of organic materials has revolutionalized the drug discovery process from carbohydrates. A great deal of drug molecules has been developed and tremendous works are in progress from carbohydrates. The developments in chemistry and biochemistry of glycoconjugates or glycohybrids as information carrier during various biological processes such as trafficking of different biomolecules, modulation of protein function, energy storage, intercellular adhesion, signal transduction, malignant transformation, viral and bacterial cell surface recognition, as well as involvement in selective binding and several other molecular recognition phenomenon make them superb in pharmaceutical, medicinal and biological sciences. One of the prominent and wide spread disease, tuberculosis (TB) claiming nearly two million death every year throughout the world and recent challenge of MDRTB and HIV/TB synergy has led to declare this disease as global health threat by WHO. Therefore, attempts are being made to develop new antitubercular drugs with a novel and new mode of action. A number of molecules have been developed as preclinical or clinical candidate from time to time. However no new drug has entered into clinics since last 50 years. There fore at CDRI tuberculosis disease area has been identified as the most important target. In our group a number of molecules from carbohydrates and heterocycles have been reported to possess significant antitubercular activity. In continuation of the efforts in our group it was proposed to synthesized few derivatives of ascorbic acid and evaluate their antitubercular activity. The reasoning was based on certain facts associated with the structure of ascorbic acid. It has also been discovered that dihydropyrimidines are novel class of molecules that possess antifilarial activity. The work of the present Ph.D. thesis has been divided into five chapters. Each chapter deals with a specific objective and references. The first chapter deals an exploratory review on applications of L-ascorbic acid in organic synthesis: covering all aspect including details of synthetic applications, discovery and history, biosynthesis and its use as starting material for chiral synthons. Chapter 2 covers a DBU catalyzed one pot synthesis of tetronolactone and tetramic acid derivatives from L-ascorbic acid. The two classes of compounds are key component in a variety of natural product and antibiotics. Chapter 3 illustrates the synthesis of dienyl tetronic acid and their conversion into tetramic acid with extended conjugation. The compounds were designed keeping in mind the structure of thiolactomycin, a thiotetronolactone, an antitubercular lead. The compounds have been screened for their antitubercular activity. Chapter 4 covers the synthesis of a number of sugar triazoles using a click chemistry approach (3+2 cycloaddition) by the reaction of azido sugars with different acetylenes. The compounds were designed based on the earlier observations that triazoles shown significant antitubercular activity. In the last chapter an entirely different approach was undertaken to synthesize 2-sulfanyl-6-methyl-1,4-dihydropyrimidines by the reaction of 1,2,3,4-tetrahydropyrimidine-2-thione with different alkyl bromides. The synthesized compounds have displayed potent antifilarial activity both in vitro and in vivo. |
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3674512 bytes
application/pdf |
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| Language |
en
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CSIR-CDRI Thesis No. S-218
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| Subject |
Antimycobacterial
Carbohydrates Heterocycles |
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| Title |
Synthetic Studies in Antimycobacterial Agents Based on Carbohydrates and Heterocycles
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| Type |
Thesis
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