Medicinal chemistry of bioactive natural products free download


















Karmaine Millington and Anthony O. Okorodudu Department of Pathology, University of Texas Medical Branch, Galveston, TX This book would serve as an in-depth resource reference for anyone concerned about natural products and their application in medicine. The products addressed range from ginkgolides and natural antibiotics to products used to treat cancer, malaria, HIV, and Alzheimer disease.

Each chapter includes a comprehensive review of the literature concerning the biochemistry of these compounds and pertinent historical data. The efficacy of these compounds in therapeutic use is compared with that of medicines both synthetic and natural cleared by the FDA. Relevant information is also given regarding the political, social, and financial issues related to the use and availability of these natural products. The book is well illustrated, presenting structures for the drugs of interest, chemical reactions in the derivation of these products, and other interesting items such as photographs of the natural source.

Overall, this book offers much detailed information on the biochemistry of these natural products, and it should be a. Continue with Facebook. Sign up with Google. Log in with Microsoft. Bookmark this article. Loss of the acetic acid with the help of the hydroxyl group can lead to the quinone methide inter- Scheme 3.

The proposed biosynthesis of compound Apparently, the compound ation of lupinifolin, epoxylupinifolin and dereticulatin was formed during PTLC purification when methanol triacetate. They inhibited the P cell line at 0. All compounds were inactive against the KB cell line.

Other flavonoid compounds including the calycopterones, a new class of biflavonoids, which ex- hibited novel cytotoxicity in a diverse panel of human tumor cell lines Wall et al. It is a , p. O-methyltylophorinidine 43 , a phenanthroin- tol 46 from the plant from Thailand called Plao-Noi, dolizidine alkaloid, has been reisolated from Ficus Croton sublyratus Kurz.

Euphorbiaceae by Japanese hispida collected in Chiang Rai in the northern part scientists at the Sankyo company. Interestingly, a The structure of compound 46 was proved to be the related phenanthroindolizidine 44 was isolated from diterpene as shown by spectroscopic methods and syn- the Danaid butterfly, Ideopsis similis.

The compound thesis Ogiso et al. The compound was found to have a potent cytotoxic property against was proved to be a potent antiulcer drug.

Prostaglandins are known to inhibit acid secretion and stimulate the secretion of mucus, and of bicarbonate. This compound is now commercially available under the trade name of Kelnec.

The antiulcerative effect of Thai bananas of different varieties have also been recently investigated Pannangpetch et al. It is now generally accepted that Helicobacter pylori infection is the major cause of chronic active gastritis and peptic ulcer disease.

It was found that rotenoids from the roots of Derris malaccensis ex- hibited selective activity against Helicobacter pylori. Tephrosin 47 and toxicarol 48 gave the best res- Antiulcer agents ult with minimum inhibitory concentrations MIC of 0. It is thus their lives, and the treatment of this condition has long likely that the selective anti-H. The plant is used for pest control and as a fish poison. Plants are also a good source of antiulcer drugs.

The modern treatment of peptic ulcers started in the s with the use of a drug called carbenoxolone 45 which is a sodium salt of a triterpenic acid. Miroes- trol 55 was previously isolated and found to exhibit potent estrogenic activity. It was regarded as the com- pound with the highest estrogenic potency among the known phytoestrogens. Recent investigation resulted in the isolation of deoxymiroestrol 56 and it was found that deoxymiroestrol was 10 times more po- tent than the previously isolated miroestrol in terms of their growth-promoting effects on MCF-7 human breast cancer cells in the presence of an estrogen antagonist, toremifene.

Due to the facile aerial oxid- ation of deoxymiroestrol to miroestrol, it is likely that miroestrol was an artifact Chansakaow et al. Some Thai medicinal plants have recently been invest- igated for anti-inflammatory activity. Both compounds showed significant topical anti-inflammatory activity in the TPA-induced ear edema assay in rats Tuchinda et al.

Iridoids 53 and 54 were isolated from the polar fractions of the butanol ex- 8-Isopentenylnaringenin, a prenylflavonoid, isol- tract of Vitex peduncularis Wall. Verbenaceae and ated from a methanol extract of the heartwood were tested for inhibition of cyclooxygenase COX, of Anaxagorea luzonensis, has been found to ex- prostaglandin H synthase -1 and COX-2 regulated hibit estrogen agonist activity Kitaoka et al. Similar agonist activity has also been repor- ine cell lines. Similarly, iridoid 54 had a of chronically debilitating or life-threatening diseases COX-2 IC50 value of 0.

With new diseases et al. The research on nat- ural products will be essential for the discovery of lead compounds in the future because of the incredible diversity of chemical structures that are produced by living organisms. We also acknowledge the Epothilons A and B: Antifungal and cytotoxic compounds from facilities in the Department of Chemistry, Mahidol Sorangium cellulosum myxobacteria. Production, physico- chemical and biological properties.

Phytochemistry — Characterization of Flavonoid Glycosides by acidic and enzymic hydrolyses. Phyto- References chemistry 4: — Tetrahedron — Science — Chimia 10— Cancer Research — Planta Med.

Arotocarpus integer. Plant Med. Clark AM Natural products as a resource for new drugs. Potentiating the resources of the rain forest. Isolation of 8-isopentenylnaringenin and an initial study on Cordell GA Biodiversity and drug discovery-a symbiotic its structure-activity relationship. Current Topics in Medicinal Chemistry. Medicinal Chemistry. Current Drug Research Reviews.

Anti-Cancer Agents in Medicinal Chemistry. Anti-Infective Agents. View More. Advances in Anticancer Agents in Medicinal Chemistry. Frontiers in Medicinal Chemistry. Natural products present in the plant and animal kingdom offer a huge diversity of chemical structures which are the result of biosynthetic processes that have been modulated over the millennia through genetic effects. With the rapid developments in spectroscopic techniques and accompanying advances in high-throughput screening techniques, it has become possible to isolate, and then determine the structures and biological activity of natural products rapidly, thus opening up exciting new opportunities in the field of new drug development to the pharmaceutical industry.

The series also covers the synthesis or testing and recording of the medicinal properties of natural products. The diagrams are clear and the writing excellent. In summary, this is another excellent volume in a very valuable series on natural products for which Professor Atta-ur-Rahman is to be congratulated Current discoveries and research into bioactive naturalproducts Medicinal Chemistry of Bioactive Natural Products provides amuch-needed survey of bioactive natural products and theirapplications in medicinal chemistry.

This comprehensive referencefeatures articles by some of the world's leading scientists in thefield on discovery, structure elucidation, and elegant syntheticstrategies--developed for natural products--with an emphasis on thestructure activity relationship of bioactive natural products. Thetopics have been carefully chosen on the basis of relevance tocurrent research and to importance as clinicially usefulagents.

Rather than attempting to be a comprehensive encyclopedia ofbioactive natural products, Medicinal Chemistry of BioactiveNatural Products guides the reader to the key developments in thefield. By providing not only practical detail but a historicalperspective on the chemistry and biology of the compounds underconsideration, the book serves as a handy resource for researchersin their own work developing pharmaceuticals, and as an inspiringintroduction for young scientists to the dynamic field of bioactivenatural products research.

Natural Product Chemistry continues to expand to exciting new frontiers of great importance in medicine. Written by international authorities in various fields of natural product chemistry, this latest volume in the well-established series Studies in Natural Products Chemistry contains 23 chapters, covering topics ranging from immunosuppressant and antimalarial compounds to bioactive substances useful in cancer and neural diseases.

This present volume, will again be of great interest to research scientists and scholars working in the exciting field of new drug discovery. With the rapid developments in spectroscopic techniques and accompanying advances in high-throughput screening techniques, it has become possible to isolate, determine the structures and biological activity of natural products rapidly, thus opening up exciting new opportunities in the field of new drug development to the pharmaceutical industry.

The present volume contains 22 articles written by leading experts in natural product chemistry on biologically active natural products. It includes research on a variety of different classes of natural products including sesquiterpenes, quassinoids, diterpenoids, lignans, oligostilbenes, phenylethanoids, phenylpropanoid glycosides, curcumin analogues, glycosphingolipids etc.



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