370,323 results match your criteria protein derivatives

A broadly cross-reactive monoclonal antibody against hepatitis E virus capsid antigen.

Appl Microbiol Biotechnol 2021 Jun 15. Epub 2021 Jun 15.

Institute of Novel and Emerging Infectious Diseases, Friedrich-Loeffler-Institut, Federal Research Institute for Animal Health, 17493, Greifswald-Insel Riems, Germany.

To generate a hepatitis E virus (HEV) genotype 3 (HEV-3)-specific monoclonal antibody (mAb), the Escherichia coli-expressed carboxy-terminal part of its capsid protein was used to immunise BALB/c mice. The immunisation resulted in the induction of HEV-specific antibodies of high titre. The mAb G117-AA4 of IgG1 isotype was obtained showing a strong reactivity with the homologous E. Read More

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Novel Benzyloxyphenyl Pyrimidine-5-Carbonitrile Derivatives as Potential Apoptotic Antiproliferative Agents.

Anticancer Agents Med Chem 2021 Jun 11. Epub 2021 Jun 11.

Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, 44519. Egypt.

Background: Pyrimidine-5-carbonitrile had a broad spectrum of biological activities such as antiviral, antioxidant and anticancer activity. Among similar compounds, monastrol being the most prominent due to cell-permeant inhibitor of mitosis therefore, we investigated the new Pyrimidine-5-carbonitrile as a cytotoxic agent for p53 pathway.

Objective: Several new benzyloxyphenyl pyrimidine-5-carbonitrile derivatives were designed, synthesized, characterized, and their cytotoxicity was evaluated. Read More

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Synthesis of novel 5-(2,5-bis(2,2,2-trifluoroethoxy)phenyl)-1,3,4-oxadiazole-2-thiol derivatives as potential glucosidase inhibitors.

Bioorg Chem 2021 May 31;114:105046. Epub 2021 May 31.

Neurogenetics Lab, Department of Applied Zoology, Mangalore University, Mangalagangothri 574199, India.

Background: A hybrid molecule of different biologically active substances can improve affinity and efficiency compared to a standard drug. Hence based on this fact, we predict that a combination of fluorine, oxadiazole, sulfur, etc., may enhance α-glucosidase inhibition activity compared to a standard drug. Read More

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Pathways of iron and sulfur acquisition, cofactor assembly, destination, and storage in diverse archaeal methanogens, methanotrophs, and alkanotrophs.

J Bacteriol 2021 Jun 14:JB0011721. Epub 2021 Jun 14.

Department of Microbiology and Immunology, Montana State University, Bozeman, Montana 59717.

Archaeal methanogens, methanotrophs, and alkanotrophs have a high demand for iron (Fe) and sulfur (S); however, little is known of how they acquire, traffic, deploy, and store these elements. Here, we examined the distribution of homologs of proteins mediating key steps in Fe/S metabolism in model microorganisms, including iron(II) sensing/uptake (FeoAB), sulfide extraction from cysteine (SufS), the biosynthesis of iron-sulfur [Fe-S] clusters (SufBCDE), siroheme (Pch2-dehydrogenase), protoheme (AhbABCD), and cytochrome (CcmCF), and iron-storage/detoxification (Bfr, FtrA, IssA), among 326 publicly available, complete or metagenome-assembled genomes of archaeal methanogens/methanotrophs/alkanotrophs. Results indicate several prevalent but non-universal features including FeoB, SufBC, and the biosynthetic apparatus for the basic tetrapyrrole scaffold as well as its siroheme (and F) derivatives. Read More

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Natural Phytochemicals as Novel Therapeutic Strategies to Prevent and Treat Parkinson's Disease: Current Knowledge and Future Perspectives.

Oxid Med Cell Longev 2021 25;2021:6680935. Epub 2021 May 25.

Department of Applied Life Science, Graduate School, BK21 Program, Konkuk University, Chungju 27478, Republic of Korea.

Parkinson's disease (PD) is the second-most common neurodegenerative chronic disease affecting both cognitive performance and motor functions in aged people. Yet despite the prevalence of this disease, the current therapeutic options for the management of PD can only alleviate motor symptoms. Research has explored novel substances for naturally derived antioxidant phytochemicals with potential therapeutic benefits for PD patients through their neuroprotective mechanism, targeting oxidative stress, neuroinflammation, abnormal protein accumulation, mitochondrial dysfunction, endoplasmic reticulum stress, neurotrophic factor deficit, and apoptosis. Read More

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Top-Down Proteomics of Human Saliva Highlights Anti-inflammatory, Antioxidant, and Antimicrobial Defense Responses in Alzheimer Disease.

Front Neurosci 2021 26;15:668852. Epub 2021 May 26.

Dipartimento di Scienze della Vita e dell'Ambiente, Università di Cagliari, Cagliari, Italy.

Alzheimer disease (AD) is the most prevalent neurodegenerative disease in the elderly, characterized by accumulation in the brain of misfolded proteins, inflammation, and oxidative damage leading to neuronal cell death. By considering the viewpoint that AD onset and worsening may be influenced by environmental factors causing infection, oxidative stress, and inflammatory reaction, we investigated the changes of the salivary proteome in a population of patients with respect to that in healthy controls (HCs). Indeed, the possible use of saliva as a diagnostic tool has been explored in several oral and systemic diseases. Read More

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Photoperiod-induced alterations in biomarkers of oxidative stress and biochemical pathways in rats of different ages: Focus on individual physiological reactivity.

Chronobiol Int 2021 Jun 14:1-19. Epub 2021 Jun 14.

Department of Ecology and Nature Protection, T.G. Shevchenko National University "Chernihiv Collegium", Chernihiv, Ukraine.

Effects of photoperiodicity caused by both the age and individual physiological reactivity estimated by resistance to hypobaric hypoxia on the levels of lipid peroxidation, protein oxidation (aldehydic and ketonic derivatives), total antioxidant capacity, activities of antioxidant enzymes (superoxide dismutase, catalase, glutathione peroxidase, and glutathione reductase), and biochemical parameters of aerobic and anaerobic pathways in hepatic tissue depending on the blood melatonin level were studied. The study was carried out on 96 6- and 21-month-old male rats divided into hypoxia resistance groups (LR, low resistance, HR, high resistance). The analyses were conducted at four photoperiods: winter (January), spring (March), summer (July), and autumn (October). Read More

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Inhibitory effect of thiourea derivatives on the growth of blue-green algae.

J Environ Manage 2021 Jun 10;294:113008. Epub 2021 Jun 10.

Faculty of Science and Marine Environment (FSSM), Universiti Malaysia Terengganu, 21030, Kuala Nerus, Terengganu, Malaysia.

High nutrient loading in aquatic environment has become the main causative of harmful algae blooms (HABs) in water resources particularly pond, lake and river. HABs are mostly dominated by microalgae derived from the group of blue-green algae which are capable of releasing harmful toxins. Therefore, this study aims to investigate the inhibitory effects of thiourea derivatives on the growth of such blue-green algae. Read More

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Structure-based molecular hybridization design of Keap1-Nrf2 inhibitors as novel protective agents of acute lung injury.

Eur J Med Chem 2021 Jun 5;222:113599. Epub 2021 Jun 5.

School of Pharmacy, Ningxia Medical University, 1160 Shengli Street, Yinchuan, 750004, China; School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai, 200433, China. Electronic address:

Blocking the Kelch-like epichlorohydrin-related protein 1 (Keap1)-nuclear factor-erythroid 2 related factor 2 (Nrf2) pathway represents as a promising strategy to reduce oxidative stress and related-inflammation, including acute lung injury (ALI). NXPZ-2, a naphthalensulfonamide derivative, was previously reported to effectively inhibit the Keap1-Nrf2 protein-protein interaction (PPI) by our group. In the present work, a series of novel isothiocyanate-containing naphthalensulfonamides with the thioether, sulfoxide and sulfone moieties were designed by a structure-based molecular hybridization strategy using NXPZ-2 and the Nrf2 activator sulforaphane. Read More

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Delta class glutathione S-transferase (TuGSTd01) from the two-spotted spider mite Tetranychus urticae is inhibited by abamectin.

Pestic Biochem Physiol 2021 Jul 6;176:104873. Epub 2021 May 6.

Department of Chemistry and Biochemistry, University of South Carolina, Columbia, SC 29208, USA. Electronic address:

GSTs (Glutathione S-transferases) are known to catalyze the nucleophilic attack of the sulfhydryl group of reduced glutathione (GSH) on electrophilic centers of xenobiotic compounds, including insecticides and acaricides. Genome analyses of the polyphagous spider mite herbivore Tetranychus urticae (two-spotted spider mite) revealed the presence of a set of 32 genes that code for secreted proteins belonging to the GST family of enzymes. To better understand the role of these proteins in T. Read More

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Bioinspired polysaccharide hybrid hydrogel promoted recruitment and chondrogenic differentiation of bone marrow mesenchymal stem cells.

Carbohydr Polym 2021 Sep 19;267:118224. Epub 2021 May 19.

National Engineering Research Center for Biomaterials, Sichuan University, 29 Wangjiang Road, Chengdu, Sichuan 610064, PR China; College of Biomedical Engineering, Sichuan University, 29 Wangjiang Road, Chengdu 610064, PR China.

Cartilage regeneration by biomimetic cartilage matrix with synchronously recruited stem cells was one of ideal strategies. Inspired by catechol for proteins adhesion, dopamine modified polysaccharide hybrid hydrogel (HD-C) was prepared by integrating collagen I (Col I) and hyaluronic acid derivatives (HA-DN) with sulfhydryl modified polysaccharide hybrid hydrogel (HS-C) as control. Because of double-crosslinking architecture, HD-C hydrogel was endowed with a more compact pore structure, higher mechanical properties and water retention ability in comparison with those of HS-C hydrogel. Read More

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September 2021

Hyaluronic acid based microneedle array: Recent applications in drug delivery and cosmetology.

Carbohydr Polym 2021 Sep 7;267:118168. Epub 2021 May 7.

Department of Pharmaceutics, ISF College of Pharmacy, Moga, Punjab 142001, India. Electronic address:

Microneedles are micron-sized arrays of needles that facilitate drug delivery for local and systemic effects. Hyaluronic acid (HA) is a glycosaminoglycan and is an indigenous component of the connective tissues and dermis. Owing to its versatility and biocompatibility, it has widely been used against various bone, eye, and skin disorders. Read More

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September 2021

Improved SARS-CoV-2 M inhibitors based on feline antiviral drug GC376: Structural enhancements, increased solubility, and micellar studies.

Eur J Med Chem 2021 May 30;222:113584. Epub 2021 May 30.

Department of Chemistry, University of Alberta, Edmonton AB, T6G 2G2, Canada. Electronic address:

Replication of SARS-CoV-2, the coronavirus causing COVID-19, requires a main protease (M) to cleave viral proteins. Consequently, M is a target for antiviral agents. We and others previously demonstrated that GC376, a bisulfite prodrug with efficacy as an anti-coronaviral agent in animals, is an effective inhibitor of M in SARS-CoV-2. Read More

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Model infant biscuits release the opioid-acting peptides milk β-casomorphins and gluten exorphins after in vitro gastrointestinal digestion.

Food Chem 2021 Jun 1;362:130262. Epub 2021 Jun 1.

Dipartimento di Scienze per gli Alimenti, la Nutrizione e l'Ambiente, Università degli Studi di Milano, Via G. Celoria 2, 20133 Milan, Italy.

Infant biscuits (IBs) are commonly used during the complementary feeding of infants from the 6th month of life. They contain wheat flour and dairy ingredients, which can release the opioid-acting peptides β-casomorphins (BCMs) and gluten exorphins (GEs) after gastrointestinal digestion. In the present study, five model IBs were prepared with or without gluten and different powdered milk derivatives in the formulations. Read More

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Synthesis and Testing of Novel Isomeric Mitochondriotropic Derivatives of Resveratrol and Quercetin.

Methods Mol Biol 2021 ;2275:141-160

Department of Chemical Sciences, University of Padova, Padova, Italy.

Resveratrol and quercetin are among the most studied plant polyphenols, and have many health-promoting actions. Strategies to accumulate them into mitochondria may be of therapeutic relevance, since these compounds are redox active and are well known to impact mitochondria and mitochondrial proteins. We report here the procedures to synthesize mitochondria-targeted resveratrol and quercetin derivatives; the synthetic strategies reported are however expected to be adaptable to other polyphenols with similar reactivity at the phenolic hydroxyls. Read More

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January 2021

Medicinal chemistry of anthranilic acid derivatives: A mini review.

Drug Dev Res 2021 Jun 12. Epub 2021 Jun 12.

Department of Chemistry, UGC Sponsored Centre for Advanced Studies, Guru Nanak Dev University, Amritsar, Punjab, India.

Anthranilic acid and its analogues present a privileged profile as pharmacophores for the rational development of pharmaceuticals deliberated for managing the pathophysiology and pathogenesis of various diseases. The substitution on anthranilic acid scaffold provides large compound libraries, which enable a comprehensive assessment of the structure activity relationship (SAR) analysis for the identification of hits and leads in a typical drug development paradigm. Besides, their widespread applications as anti-inflammatory fenamates, the amide and anilide derivatives of anthranilic acid analogues play a central role in the management of several metabolic disorders. Read More

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Role of chitosan based nanomedicines in the treatment of chronic respiratory diseases.

Int J Biol Macromol 2021 Jun 8. Epub 2021 Jun 8.

Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak 124001, India. Electronic address:

Chitosan-loaded nanomedicines provide a greater opportunity for the treatment of respiratory diseases. Natural biopolymer chitosan and its derivatives have a large number of proven pharmacological actions like antioxidant, wound healing, immuno-stimulant, hypocholesterolemic, antimicrobial, obesity treatment, anti-inflammatory, anticancer, bone tissue engineering, antifungal, regenerative medicine, anti-diabetic and mucosal adjuvant, etc. which attracted its use in the pharmaceutical industry. Read More

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Large Stokes shift fluorescence activation in an RNA aptamer by intermolecular proton transfer to guanine.

Nat Commun 2021 06 10;12(1):3549. Epub 2021 Jun 10.

Julius-Maximilians-Universität Würzburg, Institut für Organische Chemie, Am Hubland, 97074, Würzburg, Germany.

Fluorogenic RNA aptamers are synthetic functional RNAs that specifically bind and activate conditional fluorophores. The Chili RNA aptamer mimics large Stokes shift fluorescent proteins and exhibits high affinity for 3,5-dimethoxy-4-hydroxybenzylidene imidazolone (DMHBI) derivatives to elicit green or red fluorescence emission. Here, we elucidate the structural and mechanistic basis of fluorescence activation by crystallography and time-resolved optical spectroscopy. Read More

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Molecular dynamics simulation for mechanism revelation of the safety and nutrition of lipids and derivatives in food: State of the art.

Food Res Int 2021 Jul 11;145:110399. Epub 2021 May 11.

State Key Laboratory of Food Science and Technology, School of Food Science and Technology, National Engineering Research Center for Functional Food, National Engineering Laboratory for Cereal Fermentation Technology, Collaborative Innovation Center of Food Safety and Quality Control in Jiangsu Province, Jiangnan University, 1800 Lihu Road, Wuxi 214122, Jiangsu, People's Republic of China. Electronic address:

Molecular dynamics (MD) simulation has proved to be a powerful tool in the study of proteins, nucleic acids, lipids, and carbohydrates et al. in fields of health, nutrition, and food science. In particular, MD simulation has been employed in the investigation of various lipid systems such as triglycerides, phospholipid membranes, etc. Read More

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Courier service for phosphatidylinositol: PITPs deliver on demand.

Biochim Biophys Acta Mol Cell Biol Lipids 2021 Jun 7;1866(9):158985. Epub 2021 Jun 7.

Dept. of Neuroscience, Physiology and Pharmacology, Division of Biosciences, University College London, London WC1E 6JJ, UK. Electronic address:

Phosphatidylinositol is the parent lipid for the synthesis of seven phosphorylated inositol lipids and each of them play specific roles in numerous processes including receptor-mediated signalling, actin cytoskeleton dynamics and membrane trafficking. PI synthesis is localised to the endoplasmic reticulum (ER) whilst its phosphorylated derivatives are found in other organelles where the lipid kinases also reside. Phosphorylation of PI to phosphatidylinositol (4,5) bisphosphate (PI(4,5)P) at the plasma membrane and to phosphatidylinositol 4-phosphate (PI4P) at the Golgi are key events in lipid signalling and Golgi function respectively. Read More

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Sterol regulation of developmental and oncogenic Hedgehog signaling.

Biochem Pharmacol 2021 Jun 7:114647. Epub 2021 Jun 7.

Department of Cell Biology, Harvard Medical School, Boston, MA, USA. Electronic address:

The Hedgehog (Hh) family of lipid-modified signaling proteins directs embryonic tissue patterning and postembryonic tissue homeostasis, and dysregulated Hh signaling drives familial and sporadic cancers. Hh ligands bind to and inhibit the tumor suppressor Patched and allow the oncoprotein Smoothened (SMO) to accumulate in cilia, which in turn activates the GLI family of transcription factors. Recent work has demonstrated that endogenous cholesterol and oxidized cholesterol derivatives (oxysterols) bind and modulate SMO activity. Read More

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Degradation of Janus kinases in CRLF2-rearranged acute lymphoblastic leukemia.

Blood 2021 Jun 10. Epub 2021 Jun 10.

St Jude Children's Research Hospital, Memphis, Tennessee, United States.

CRLF2-rearranged (CRLF2r) acute lymphoblastic leukemia (ALL) comprises over half of Philadelphia chromosome-like (Ph-like) ALL, is associated with poor outcome in children and adults. Overexpression of CRLF2 results in activation of JAK-STAT and parallel signaling pathways in experimental models, but existing small molecule inhibitors of Janus kinases show variable and limited efficacy. Here we evaluated the efficacy of proteolysis-targeting chimeras (PROTACs) directed against Janus kinases. Read More

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Synthesis, Molecular Docking, and Biological Evaluation of Some Novel 2-(5-Substituted 1,3,4-oxadiazole-2-yl)-1,3-benzothiazole Derivatives as Anticonvulsant Agents.

Cent Nerv Syst Agents Med Chem 2021 Jun 7. Epub 2021 Jun 7.

Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research (SPER), Jamia Hamdard, New Delhi, 110062, India.

Background: Benzothiazole is an organosulfur heterocyclic compound that has a considerable place in drug discovery due to significant pharmacological actions.

Objective: The main objective of the present study was to synthesize some novel 2-(5-substituted 1,3,4-oxadiazole-2-yl)-1,3-benzothiazole derivatives and evaluate them for their anticonvulsant activity using in silico and in vivo methods.

Method: A set of sixteen 2-(5-substituted 1, 3, 4-oxadiazole-2-yl)-1, 3-benzothiazole derivatives were prepared using multi-step reactions starting from o-amino-thiophenol and characterized by suitable spectral techniques. Read More

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Structural development of salicylanilide-based SPAK inhibitors as candidate antihypertensive agents.

ChemMedChem 2021 Jun 9. Epub 2021 Jun 9.


Hypertension is an important target for drug discovery. We have focused on the with-no-lysine kinase (WNK)-oxidative stress-responsive 1 (OSR1) and STE20/SPS1-related proline-alanine-rich protein kinase (SPAK)-NaCl cotransporter (NCC) signal cascade as a potential target, and we previously developed a screening system for inhibitors of WNK-OSR1/SPAK-NCC signaling. Herein we used this system to examine the structure-activity relationship (SAR) of salicylanilide derivatives as SPAK kinase inhibitors. Read More

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Innovative strategies to enhance the sensory quality of dry fermented sausages containing lactic ingredients by the addition of exogenous enzymes.

Food Sci Technol Int 2021 Jun 9:10820132211022112. Epub 2021 Jun 9.

Teagasc Food Research Centre, Moorepark, Fermoy, Co. Cork, Ireland.

This study investigated the impact of the addition of exogenous enzymes (Accelerzyme CPG, Debitrase DBP20) or cellular preparations (FlavoGard), traditionally used in the cheese industry, to accelerate flavour development of dry fermented sausages with 6% of lactic derivatives content. Sausages were fermented to pH 5.0, dried for 32 days and vacuum packed stored under refrigeration for 60 days. Read More

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Synthesis, antimicrobial, anti-proliferative activities, molecular docking and DFT studies of novel pyrazolo[5,1-c][1, 2, 4]triazine-3-carboxamide derivatives.

J Biomol Struct Dyn 2021 Jun 9:1-17. Epub 2021 Jun 9.

Department of Chemistry, Faculty of Science, Cairo University, Giza, Cairo, Egypt.

In this investigation, we studied the reactivity of 5-aminouracil () with ethyl cyanoacetate () utilizing microwave irradiation to afford the corresponding 2-cyano--(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)acetamide () in excellent yield. The electrophilic azo-coupling reaction of acetamide with aromatic diazonium salts afforded the corresponding hydrazone derivatives The Michael addition cyclization of hydrazone in pyridine to give pyrazolo[5,1-c][1, 2, 4]triazine-3-carboxamide derivatives. The obtained compounds were elucidated against antimicrobial activity and antitumor activity breast cancer cells (MCF-7) and liver cancer cells (HepG2) utilized MTT assay. Read More

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[The Inhibiting Effect of Autophagy Inhibitor ROC-325 on Multiple Myeloma].

Zhongguo Shi Yan Xue Ye Xue Za Zhi 2021 Jun;29(3):797-804

Institute of Hematology, Xuzhou Medical University; Department of Hematology, Xuzhou Medical University Affiliated Hospital, Xuzhou 221002, Jiangsu Province, China,E-mail:

Objective: To investigate the effects of autophagy inhibitor ROC-325 and its combination with bortezomib on the proliferation, apoptosis and autophagy of multiple myeloma cell lines.

Methods: Multiple myeloma cells were treated with ROC-325 at different concentration. The cell proliferation was detected by CCK-8. Read More

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Microsequential injection analysis/lab-on-valve system for the automatic evaluation of acetylcholinesterase inhibitors.

Arch Pharm (Weinheim) 2021 Jun 8:e2100150. Epub 2021 Jun 8.

LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, Porto University, Porto, Portugal.

A miniaturized microsequential injection/lab-on-valve (µSIA-LOV) system was developed and shown to be a useful alternative to perform inhibitory studies on acetylcholinesterase. These studies are essential for the evaluation of the potential therapeutic effect of drugs commonly used in the treatment of Alzheimer's disease. Donepezil, galantamine, and rivastigmine were tested, in addition to compounds based on the xanthone scaffold. Read More

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Hopeless tooth? Prognosis and comprehensive treatment. A case report.

J Med Life 2021 Mar-Apr;14(2):287-294

Department of Endodontics, University of Medicine and Pharmacy Carol Davila, Faculty of Dental Medicine, Bucharest, Romania.

A hopeless tooth from a periodontal point of view, with severe bone resorption, mobility and abnormal tooth migration, is often extracted. In advanced cases, function and esthetics are impaired, and an interdisciplinary treatment is requested. Retaining or not these teeth is based on clinician judgment. Read More

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Comparative phytochemistry of flavaglines (= rocaglamides), a group of highly bioactive flavolignans from species (Meliaceae).

Harald Greger

Phytochem Rev 2021 Jun 4:1-40. Epub 2021 Jun 4.

Chemodiversity Research Group, Faculty of Life Sciences, University of Vienna, Rennweg 14, 1030 Wien, Austria.

Flavaglines are formed by cycloaddition of a flavonoid nucleus with a cinnamic acid moiety representing a typical chemical character of the genus of the family Meliaceae. Based on biosynthetic considerations 148 derivatives are grouped together into three skeletal types representing 77 cyclopenta[]benzofurans, 61 cyclopenta[]benzopyrans, and 10 benzo[]oxepines. Apart from different hydroxy, methoxy, and methylenedioxy groups of the aromatic rings, important structural variation is created by different substitutions and stereochemistries of the central cyclopentane ring. Read More

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