Relevant bibliographies by topics / Piperidine derivatives

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  1. Journal articles
  2. Dissertations / Theses
  3. Books
  4. Book chapters
  5. Conference papers

Academic literature on the topic 'Piperidine derivatives'

Author: Grafiati
Published: 4 June 2021
Last updated: 25 April 2022

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Journal articles on the topic "Piperidine derivatives"

1

Jílek, Jiří, Miroslav Rajšner, Vladimír Valenta, et al. "Synthesis of piperidine derivatives as potential analgetic agents." Collection of Czechoslovak Chemical Communications 55, no. 7 (1990): 1828–53. http://dx.doi.org/10.1135/cccc19901828.

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Reaction of N-(1-(2-phenylethyl)-4-piperidinyl)propionanilide (I) with phosphorus pentasulfide gave the thioamide VI. Acylation of N-(1-(2-phenylethyl)-4-piperidinyl)aniline with 2-(methoxy)acetic and 2-(methylthio)acetic anhydrides afforded the amides II and III. Treatment of 4-anilino-1-benzylpiperidine-4-methanol with thionyl chloride gave the spirocyclic sulfurous acid ester amide XIV. Reduction of the hydrochloride of ethyl 3-(1-ethoxycarbonyl-4-phenylimino-3-piperidinyl)propionate (XXII) with sodium cyanoborohydride gave the perhydro-1,6-naphthyridine derivative XIX, a model compound in
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Romero, Nancy, Sylvain Bernès, Luis F. Roa, Joel L. Terán, and Dino Gnecco. "Crystal structures of two chiral piperidine derivatives: 1-[(1R)-2-hydroxy-1-phenylethyl]piperidin-4-one and 8-[(1S)-1-phenylethyl]-1,4-dioxa-8-azaspiro[4.5]decane-7-thione." Acta Crystallographica Section E Crystallographic Communications 71, no. 10 (2015): 1207–11. http://dx.doi.org/10.1107/s2056989015017119.

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The crystal structures of the two title piperidine derivatives show different conformations for the six-membered heterocycle. TheN-substituted 4-piperidinone 1-[(1R)-2-hydroxy-1-phenylethyl]piperidin-4-one, C13H17NO2, (I), has a chair conformation, while the piperidine substituted in position 2 with a thiocarbonyl group, 8-[(1S)-1-phenylethyl]-1,4-dioxa-8-azaspiro[4.5]decane-7-thione, C15H19NO2S, (II), features a half-chair conformation. Comparison of the two structures, and data retrieved from the literature, suggests that the conformational flexibility is mainly related to the hybridization
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Klegraf, Ellen, and Horst Kunz. "Stereoselective Synthesis of 3-Substituted and 3,4-Disubstituted Piperidine und Piperidin-2-one Derivatives." Zeitschrift für Naturforschung B 67, no. 4 (2012): 389–405. http://dx.doi.org/10.1515/znb-2012-0413.

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The stereoselective synthesis of 3-substituted and 3,4-disubstituted piperidine and piperidin-2-one derivatives was achieved starting from 2-pyridone. After N-galactosylation and subsequent O-silylation, nucleophilic addition of organometallic reagents proceeded with high regio- and stereoselectivity at 4-position. Substituents at position 3 were stereoselectively introduced by reaction of electrophiles with amide enolates of the N-galactosyl-2-piperidones.
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Prisyazhnyuk, Vladimir, Matthias Jachan, Irene Brüdgam, Reinhold Zimmer та Hans-Ulrich Reissig. "Addition of lithiated methoxyallene to aziridines – a novel access to enantiopure piperidine and β-amino acid derivatives". Collection of Czechoslovak Chemical Communications 74, № 7-8 (2009): 1069–80. http://dx.doi.org/10.1135/cccc2009012.

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Addition of lithiated methoxyallene to aziridine derivatives provided the expected primary addition products. The less substituted carbon of the aziridine ring was attacked selectively. The primary adducts could be converted to enantiopure piperidine derivatives or β-amino acid derivatives. The unexpected reactions lead to a tricyclic sulfonamide and to alkynyl-substituted aminoethers. The efficient two-step conversion of a piperidone derivative to a benzomorphan demonstrates the potential of this approach to biologically active compounds.
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Kantlehner, Willi, Markus Vettel, and Bernhard Eppinger. "Orthoamide und Iminiumsalze, LXXVI [1]. Ein weiterer Beitrag zur Chemie der Trialkoxyacetonitrile/ Orthoamides and Iminium Salts LXXVI [1]. A Further Contribution to the Chemistry of Trialkoxyacetonitriles." Zeitschrift für Naturforschung B 67, no. 4 (2012): 373–88. http://dx.doi.org/10.1515/znb-2012-0412.

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An improved procedure for the preparation of trimethoxyacetonitrile (3a) starting from trichloroacetonitrile and sodium methanolate is described. Carbanions, obtained by the action of sodium hydride on nitriles, ethyl acetate and methylketones, react with trialkoxyacetonitriles 3 to give α- imino-orthocarboxylic acid trialkylesters 12, 14 and 20, which form an equilibrium with the tautomeric enamines 13, 15 and 21. The enamines 21 react with N,N-dimethylformamide dimethylacetal (24) to give amidines 25 which are cyclized to pyridinium salts 28 and 29 on treatment with benzyl bromide and acetyl
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Du, Rui, Liangliang Han, Zhongqiang Zhou, and Victor Borovkov. "Efficient Synthesis of Novel Quinolinone Derivatives via Catalyst-free Multicomponent Reaction." Letters in Organic Chemistry 17, no. 5 (2020): 403–7. http://dx.doi.org/10.2174/1570178616666190828092728.

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The synthesis of 3-(aryl(piperidin-1-yl)methyl)-4-hydroxyquinolin-2(1H)-one derivatives via catalyst-free multicomponent reaction is described. The reaction of 4-hydroxyquinolin-2(1H)-one, piperidine, and 4-chlorobenzaldehyde was carried out in different solvents and under solvent-free conditions at room temperature. The best solvent in terms of the yield and reaction time was found to be dichloromethane. Most substituted benzaldehydes reacted with 4-hydroxyquinolin-2(1H)-one and piperidine to afford corresponding products in good-to-excellent yields. Aldehydes with electronwithdrawing groups
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López-Rodríguez, Alberto, Gema Domínguez, and Javier Pérez-Castells. "Synthesis of Novel Iminosugar Derivatives Based on a 2-Azabi­cyclo[4.1.0]heptane Skeleton." Synthesis 49, no. 20 (2017): 4606–12. http://dx.doi.org/10.1055/s-0036-1589109.

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Iminosugars are good starting points for the development of different kinds of drugs. Many are polyhydroxylated piperidines that behave as biomimetics of their corresponding pyranoses analogues. In the interaction with carbohydrate processing enzymes, selectivity is a crucial issue and the benefits of introducing a cyclopropane bridge in a piperidine structure is demonstrated. The synthesis of novel bicyclic piperidine-based iminosugars using a sulfur ylide cyclopropanation as the key synthetic step is described.
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Ivanović, Milovan, Ivana Jevtić, Ljiljana Došen-Mićović, Evica Ivanović, and Nina Todorović. "Synthesis of Orthogonally Protected (±)-3-Amino-4-anilidopiperidines and (±)-3-N-Carbomethoxyfentanyl." Synthesis 49, no. 14 (2017): 3126–36. http://dx.doi.org/10.1055/s-0036-1588985.

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The synthesis of orthogonally protected cis- and trans-3-amino-4-anilidopiperidine derivatives has been accomplished in six steps, starting from readily accessible 4-piperidone derivatives. The last three steps, i.e., N-acylation, Hofmann rearrangement, and carbamate cleavage, involved separated (±)-cis and (±)-trans intermediates. Complete retention of configuration was observed at position 3 of the piperidine ring. Specifically protected positions 1 and 3 at the piperidine scaffold allow for selective deprotection and introduction of diverse substituents at the respective nitrogen sites. The
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Shafi, S. Syed, R. Rajesh, and S. Senthilkumar. "Synthesis and Biological Properties of New Piperidine Substituted Benzothiazole Derivatives." Asian Journal of Organic & Medicinal Chemistry 6, no. 3 (2021): 181–85. http://dx.doi.org/10.14233/ajomc.2021.ajomc-p333.

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In present work, ethyl 2-aminobenzo[d]thiazole-6-carboxylate was reacted to piperidine using copper(II) bromide to get ethyl 2-(piperidin-1-yl)benzo[d]thiazole-6-carboxylate. The reaction of ethyl 2-(piperidin- 1-yl)benzo[d]thiazole-6-carboxylate with NaOH produces 2-(piperidin-1-yl)benzo[d]thiazole-6- carboxylic acid. The inter-mediate 2-(piperidin-1-yl)benzo[d]thiazole-6-carboxylic acid have been isolated as stable compounds. The chemical structures of synthesized compounds were established based on the 1H & 13C NMR and IR spectral data. The mass of the novel compounds was established wi
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Gelbrich, Thomas, Denise Rossi, and Ulrich J. Griesser. "Two polymorphs and the diethylammonium salt of the barbiturate eldoral." Acta Crystallographica Section C Crystal Structure Communications 68, no. 2 (2012): o65—o70. http://dx.doi.org/10.1107/s0108270111055120.

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Polymorph (Ia) of eldoral [5-ethyl-5-(piperidin-1-yl)barbituric acid or 5-ethyl-5-(piperidin-1-yl)-1,3-diazinane-2,4,6-trione], C11H17N3O3, displays a hydrogen-bonded layer structure parallel to (100). The piperidine N atom and the barbiturate carbonyl group in the 2-position are utilized in N—H...N and N—H...O=C hydrogen bonds, respectively. The structure of polymorph (Ib) contains pseudosymmetry elements. The two independent molecules of (Ib) are connectedviaN—H...O=C(4/6-position) and N—H...N(piperidine) hydrogen bonds to give a chain structure in the [100] direction. The hydrogen-bonded la
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Dissertations / Theses on the topic "Piperidine derivatives"

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Girling, Paul Ricardo. "Novel approaches to piperidine and hydropyridine derivatives." Thesis, Durham University, 2012. http://etheses.dur.ac.uk/6354/.

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Three new modes of reactivity are reported between the reaction of an imine, but-3-en-2-ones and a Lewis acid. These are formal [2+2+2]-, [1+2+1+2]- and [4+2]- cycloadditions, deriving 1,1'-(1,2-dihydropyridine-3,5-diyl)diethanones, 1,1'-(1,4-dihydropyridine-3,5-diyl)diethanones and piperidin-4-ones and respectively. The [2+2+2]- and [1+2+1+2]-cycloadditions proceed when R3 = LG (leaving group), with the [1+2+1+2]-pathway dominating when the imine is easily hydrolysed within the reaction conditions. When R3 ≠ LG, the cycloaddition proceeds through different [4+2]-mechanistic pathways, dependen
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Woods, Gordon Alexander. "Synthetic approaches to functionalised piperidines." Thesis, University of Oxford, 1999. http://ora.ox.ac.uk/objects/uuid:4c6fdb6c-c021-447c-8fc9-35241b552850.

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This thesis is concerned with the synthesis of functionalised piperidines. The piperidine unit is found in numerous alkaloids and other natural products, and has also been incorporated into synthetic compounds of significant therapeutic or strategic synthetic potential. Although numerous syntheses of individual piperidine compounds have been published, there are few general routes to this class of compounds, and there is therefore a need for such routes to be developed. Bicyclic lactams derived from (S)-pyroglutamic acid have been shown to be useful synthons in the synthesis of pyrrolidines. A
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Smith, Peter Duncan. "Synthesis of pipecolic acid derivatives via aza-Diels-Alder reactions." Thesis, Heriot-Watt University, 2000. http://hdl.handle.net/10399/552.

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Moraux, Thomas. "Synthesis and evaluation of α-fluoro analogues of capsaicin and 2-(aminomethyl)piperidine derivatives". Thesis, University of St Andrews, 2011. http://hdl.handle.net/10023/2094.

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Chapter 1 gives an overview of the fluorine chemistry field, from its early developments to recent applications in medicinal chemistry. The development of asymmetric electrophilic or nucleophilic installation of fluorine in organic molecules is highlighten. Chapter 2 of this thesis discusses the enantioselective synthesis of α-fluoroamides. The study is applied to the synthesis of fluoroenantiomers of the bioactive molecule capsaicin and short-chain analogues. The biological activity of these compounds is assayed with the TRPV1 receptor. Results show that enantioselective α-fluoroamides (R)-97
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Petrov, Ravil Rashitovich. "Part I. Application of 2-Hydroxymethylacrylic Acid, a Product of Baylis-Hillman Reaction, for the Synthesis of Novel N-backbone-to-Side-Chain Cyclic Peptide Analogs: Strategies and Side Reactions Part II. Synthesis and Biological Activities of Chimeric Bioactive Peptides Featuring Amino Acids Coupled to 4-Anilino-N-Phenethyl-Piperidine." Diss., The University of Arizona, 2007. http://hdl.handle.net/10150/194330.

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During my research career in Prof. V.J.Hruby's laboratory I worked on two different projects. The first project, which was initiated by the author, was planned to serve the need of our laboratory for a novel method of peptide cyclization. This method was planned to use recent advances in Pd0-catalyzed asymmetric synthesis combined with the structural richness offered by the Baylis-Hillman chemistry which could open new ways to diverse areas of drug design, molecular immunology and chemotherapy. This approach would provide cyclic peptides featuring N-alkylated amino acids that would confer high
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Anhettigama, Gamaralalage Medha Jaimini Gunaratna. "Design, synthesis and bio-evaluation of piperidines and CGRP peptides; Synthesis of substituted 6-(dimethylamino)-2-phenylisoindolin-1-ones for the inhibition of luciferase." Diss., Kansas State University, 2017. http://hdl.handle.net/2097/38204.

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Doctor of Philosophy<br>Department of Chemistry<br>Duy H. Hua<br>Three research projects are described in this dissertation, and they are: (i) discovery of piperidine derivatives as T-type calcium channel inhibitors for the treatment of epilepsy and neuropathic pain and as protein disulfide isomerase inhibitors for the treatment of influenza viral infection; (ii) discovery of peptide-based calcitonin gene-related peptide receptor antagonists for the treatment of inflammatory pain; and (iii) synthesis of substituted 6-(dimethylamino)-2-phenylisoindolin-1-ones for the inhibition of luciferase.
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Hunter, Darren F. A. "Synthesis of bioactive pyrrolidine and piperidinone derivatives from carbohydrates." Thesis, University of Oxford, 2001. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.418528.

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Wong, Yung-Sing. "Nouveaux intermediaires chiraux de type 1,4-dihydropyridine et equivalents de sels de 3,4-dihydropyridinium pour la synthese asymetrique de piperidines polysubstituees. Application a la synthese enantioselective du 3-ppp et de l'indolizidine 195b." Paris 11, 1994. http://www.theses.fr/1994PA112105.

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L'application de la reaction de zincke a des amines primaires enantiomeriquement pures a donne des sels de pyridinium portant un centre asymetrique directement fixe sur l'azote, a partir de la pyridine correspondante, substituee ou non en position 3. L'etude de la reduction par le dithionite de sodium de ces sels a conduit de maniere efficace a de nouveaux intermediaires 1,4-dihydropyridines chiraux. La reduction des sels n-substitues par une chaine phenylethanol donne des 1,4-dihydropyridines qui s'isomerisent en 3,7,8,8a-tetrahydro-2h-oxazolo3,2-apyridines. Une etude structurale a ete entrep
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Othman, Arige. "Pharmacomodulation on the piperidinol skeleton: Synthesis of novel PIPD1 derivatives as Mycobacterium abscessus agents." Master's thesis, Alma Mater Studiorum - Università di Bologna, 2017. http://amslaurea.unibo.it/13396/.

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Mycobacterium abscessus (M. abscessus) is a rapidly growing mycobacterium which is able to generate different problems in human infections, such as chronic lung diseases, pulmonary diseases and skin infection. M. abscessus is considered as the first emergent opportunistic pathogen and the number of the infections due to this pathogen increases each year. Since the natural multidrug resistance and the absence of specific treatment to fight it, M. abscessus has become a serious problem of the public health. In this context, an original approach of a phenotypic screen was performed and allowed to
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Thaler, Tobias. "Enantiocontrol with Chiral Sulfoxides and Diastereocontrol in the Cross-Couplings of Substituted Cycloalkyl and Piperidinyl Derivatives." Diss., lmu, 2011. http://nbn-resolving.de/urn:nbn:de:bvb:19-134189.

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Books on the topic "Piperidine derivatives"

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Rubiralta, Mario. Piperidine: Structure, preparation, reactivity, and synthetic applications of piperidine and its derivatives. Elsevier, 1991.

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Piperidine - Structure, Preparation, Reactivity, and Synthetic Applications of Piperidine and its Derivatives. Elsevier, 1991. http://dx.doi.org/10.1016/c2009-0-12882-9.

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Book chapters on the topic "Piperidine derivatives"

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Suryavanshi, Padmakar, Vijaykumar Paike, Sandeep More, Rajendra P. Pawar, Sandeep B. Mane, and K. L. Ameta. "Synthesis of Functionalized Piperidine Derivatives Based on Multicomponent Reaction." In Multicomponent Reactions. CRC Press, 2017. http://dx.doi.org/10.1201/9781315369754-11.

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Casy, Alan F., and Robert T. Parfitt. "Further Analgesics Based on Piperidine and Related Azacycloalkanes: Prodines, Promedols, Profadol, and Their Derivatives." In Opioid Analgesics. Springer US, 1986. http://dx.doi.org/10.1007/978-1-4899-0585-7_7.

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KELEN, T., F. TÜDŐS, G. BÁLINT, and A. ROCKENBAUER. "Electron Spin Resonance Study of Hindered Piperidine Derivatives in Polypropylene Matrix in the Presence of Other Additives." In ACS Symposium Series. American Chemical Society, 1985. http://dx.doi.org/10.1021/bk-1985-0280.ch009.

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Shnide, Ravindra S. "Design, Synthesis, and Studies of Novel Piperidine Substituted Triazine Derivatives as Potential Anti-Inflammatory and Antimicrobial Agents." In Green Chemistry and Biodiversity. Apple Academic Press, 2019. http://dx.doi.org/10.1201/9780429202599-15.

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"Mass Spectrometry of Piperidine Derivatives." In Studies in Organic Chemistry. Elsevier, 1991. http://dx.doi.org/10.1016/b978-0-444-88348-3.50009-x.

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"1H NMR Properties of Piperidine Derivatives." In Studies in Organic Chemistry. Elsevier, 1991. http://dx.doi.org/10.1016/b978-0-444-88348-3.50007-6.

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"13C NMR Spectroscopy of Piperidine Derivatives." In Studies in Organic Chemistry. Elsevier, 1991. http://dx.doi.org/10.1016/b978-0-444-88348-3.50008-8.

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Raissi, Hanen, Imen Chérif, Hajer Ayachi, et al. "Structure-Property Relationships in Benzofurazan Derivatives: A Combined Experimental and DFT/TD-DFT Investigation." In Density Functional Theory - Recent Advances, New Perspectives and Applications [Working Title]. IntechOpen, 2021. http://dx.doi.org/10.5772/intechopen.99246.

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In this work we seek to understand and to quantify the reactivity of benzofurazan derivatives toward secondary cyclic amines, like pyrrolidine, piperidine and morpholine, acting as nucleophile groups in SNAr reactions. For this aim, physico-chemical and structural descriptors were determined experimentally and theoretically using the DFT/B3LYP/6-31+ g (d,p) methodology. Thus, different 4-X-7-nitrobenzofurazans (X = OCH3, OC6H5 and Cl) and products corresponding to the electrophilic aromatic substitution by pyrrolidine, piperidine and morpholine, were investigated. Particularly, the HOMO and LUMO energy levels of the studied compounds, determined by Cyclic Voltammetry (CV) and DFT calculations, were used to evaluate the electrophilicity index (ω). The latter was exploited, according to Parr’s approach, to develop a relationship which rationalizes the kinetic data previously reported for the reactions of the 4-X-7-nitrobenzofurazans with nucleophiles cited above. Moreover, the Parr’s electrophilicity index (ω) of these benzofurazans determined in this work were combined with their electrophilicity parameters (E), reported in preceding papers, was found to predict the unknown electrophilicity parameters E of 4-piperidino, 4-morpholino and 4-pyrrolidino-7-nitrobenzofurazan. In addition, the relationship between the Parr’s electrophilicity index (ω) and Hammett constants σ, has been used as a good model to predict the electronic effect of the nucleophile groups. Finally, we will subsequently compare the electrophilicity index (ω) and the electrophilicity parameters (E) of these series of 7-X-4-nitrobenzofurazans with the calculated dipole moment (μ) in order to elucidate general relationships between E, ω and μ.
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Kantlehner, W. "Synthesis from 3-Iodo-4-1-benzopyran-4-one and Piperidine." In Three Carbon-Heteroatom Bonds: Ketenes and Derivatives. Georg Thieme Verlag KG, 2006. http://dx.doi.org/10.1055/sos-sd-024-00408.

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Taber, Douglass F. "C–N Ring Construction: The Harrity Synthesis of Quinolizidine (–)-217A." In Organic Synthesis. Oxford University Press, 2015. http://dx.doi.org/10.1093/oso/9780190200794.003.0054.

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David M. Jenkins of the University of Tennessee devised (J. Am. Chem. Soc. 2011, 133, 19342) an iron catalyst for the aziridination of an alkene 1 with an aryl azide 2. Yoshiji Takemoto of Kyoto University cyclized (Org. Lett. 2011, 13, 6374) the prochiral oxime derivative 4 to the azirine 5 in high ee. Organometallics added to 5 syn to the pendant ester. Hyeung-geun Park of Seoul National University used (Adv. Synth. Catal. 2011, 353, 3313) a chiral phase transfer catalyst to effect the enantioselective alkylation of 6 to 7. Yian Shi of Colorado State University showed (Org. Lett. 2011, 13, 6350) that a chiral Brønsted acid mediated the enantioselective cyclization of 8 to 9. Mattie S.M. Timmer of Victoria University of Wellington and Bridget L. Stocker of Malaghan Institute of Medical Research effected (J. Org. Chem. 2011, 76, 9611) the oxidative cyclization of 10 to 11. They also showed (Tetrahedron Lett. 2011, 52, 4803, not illustrated) that the same cyclization worked well to construct piperidine derivatives. Jose L. Vicario of the Universidad del País Vasco extended (Adv. Synth. Catal. 2011, 353, 3307) organocatalysis to the condensation of 12 with 13 to give the pyrrolidine 14. Jinxing Ye of the East China University of Science and Technology used (Adv. Synth. Catal. 2011, 353, 343) the same Hayashi catalyst to condense 15 with 16 to give 17. André B. Charette of the Université de Montreal expanded (Org. Lett. 2011, 13, 3830) 18, prepared by Petasis-Mannich coupling followed by ring-closing metathesis, to the piperidine 20. Marco Bella of the “Sapienza” University of Roma effected (Org. Lett. 2011, 13, 4546) enantioselective addition of 22 to the prochiral 21 to give 23. Ying-Chun Chen of Sichuan University and Chun-An Fan of Lanzhou University cyclized (Adv. Synth. Catal. 2011, 353, 2721) 24 to 25 in high ee. Andreas Schmid of TU Dortmund showed (Adv. Synth. Catal. 2011, 353, 2501) that ω-laurolactam hydrolases could be used to cyclize the ester 26, but not the free acid, to the macrolactam 27.
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Conference papers on the topic "Piperidine derivatives"

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Kovačková, Soňa, Martin Dračínský, and Dominik Rejman. "Piperidine nucleoside phosphonic acid derivatives." In XVth Symposium on Chemistry of Nucleic Acid Components. Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, 2011. http://dx.doi.org/10.1135/css201112372.

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Méndez, Leonor Yamile Vargas, and Vladimir V. Kouznetsov. "Simple preparation of new piperidine derivatives as AChE inhibitors for pest control." In 14th Brazilian Meeting on Organic Synthesis. Editora Edgard Blücher, 2013. http://dx.doi.org/10.5151/chempro-14bmos-r0250-2.

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García-Domenech, Ramón, Maria Angeles Martinez Rodriguez, Raimundo Segui Lopez-Peñalver, Gemma Alcacer Tomas, Jorge Galvez, and Maria Galvez-Llompart. "Application of molecular topology to the prediction and optimization of mosquito repellent activity of N-acyl-piperidine derivatives ." In MOL2NET 2017, International Conference on Multidisciplinary Sciences, 3rd edition. MDPI, 2017. http://dx.doi.org/10.3390/mol2net-03-04863.

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Hijikata-Okunomiya, A., S. Okamoto, R. Kikumoto, and Y. Tamao. "STEREOGEOMETRY OP THE ACTIVE SITES OF SERINE ENZYMES GATHERED FROM SYNTHETIC THROMBIN-INHIBITORS." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1644606.

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MD-805 is a potent thrombin-inhibitor having the structure of tri-pods; Arg skeletone, N-terminal side and C-terminal side. MD-805 showed weaker inhibitory activity to other enzymes than thrombin. In this report, to gather more detailed informations about the structural features of serine enzymes concerning the specificity, we experimentally examined the structure-activity relationship (SAR) of a number of arginine derivatives including MD-805 and theoretically generated a MD-805-trypsin complex model using the results of X-ray crystallography of MD-805 and BPTI-trypsin complex by calculation
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Peterson, Burl H., Sergey S. Sarkisov, V. N. Nesterov, et al. "New derivatives of cyclohexanone and piperidone compounds for bioluminous sensing." In Biomedical Optics 2006, edited by Samuel Achilefu, Darryl J. Bornhop, and Ramesh Raghavachari. SPIE, 2006. http://dx.doi.org/10.1117/12.641751.

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