- Boc-Protection on L-DOPA: an Easy Way to Promote Underwater Adhesion
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The ability of mussels to adhere to underwater surfaces has attracted a lot of attention from the scientific community. As proteins containing L-DOPA (3,4-dihydroxyphenyl-l-alanine) are involved in their adhesion, a common strategy to synthesize adhesives
- Giuri, Demetra,Jacob, Kiran A.,Ravarino, Paolo,Tomasini, Claudia
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Read Online
- Enantioselective Synthesis of Hydantoin and Diketopiperazine-Fused Tetrahydroisoquinolines via Pictet-Spengler Reaction
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An enantioselective synthesis of iso-, isothio-, and isoselenohydantoin and diketopiperazine-fused tetrahydroisoquinolines from l-Dopa was reported. The route consists of an Pictet-Spengler reaction of (S)-2-amino-3-(3,4-dimethoxyphenyl)propanoates with v
- Liu, Shih-I,Haung, Jia-Yun,Barve, Indrajeet J.,Huang, Sheng-Cih,Sun, Chung-Ming
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Read Online
- pH stability and antioxidant power of CycloDOPA and its derivatives
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CycloDOPA (leukodopachrome), a well known metabolite of tyrosine, is a precursor of melanine in mammalian organisms and of the pigment betalain in plants. However, the isolation of cycloDOPA from natural sources has not been widely reported. In the present work, the stabilities of cycloDOPA and cycloDOPA methyl ester at various pH levels were studied. Both compounds were stable under acidic conditions. By contrast, both compounds were unstable when the pH was shifted from neutral to basic to form indole derivatives as major products. Based on the pH stability, cycloDOPA and its derivatives were subjected to the DPPH radical scavenging assay for the first time.
- Nakagawa, Shiori,Tachrim, Zetryana Puteri,Kurokawa, Natsumi,Ohashi, Fumina,Sakihama, Yasuko,Suzuki, Takeyuki,Hashidoko, Yasuyuki,Hashimoto, Makoto
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Read Online
- L-DOPA AND/OR DOPA DECARBOXYLSE INHIBITORS CONJUGATED TO SUGAR FOR THE TREATMENT OF DOPAMINE-RESPONSIVE DISORDERS
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The present invention provides conjugates comprising a sugar such as mannitol and one or more L-DOPA and/or DOPA decarboxylse inhibitors including, inter alia, L- DOPA, carbidopa, benserazide, or a combination thereof, wherein the sugar is conjugated to t
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Paragraph 00221; 00222; 00223
(2020/07/05)
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- PROCESS FOR PREPARING PURIFIED LEVODOPAMIDE FREE BASE
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Disclosed herein, in part, are processes making and purifying L-dopamide free base, such as purified pharmaceutically acceptable L-dopamide free base substantially free of L-dopa. Such processes are useful for providing L-dopamide for the treatment of neu
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Paragraph 126; 127
(2020/03/05)
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- A Novel N-Substituted Valine Derivative with Unique Peroxisome Proliferator-Activated Receptor γbinding Properties and Biological Activities
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A proprietary library of novel N-Aryl-substituted amino acid derivatives bearing a hydroxamate head group allowed the identification of compound 3a that possesses weak proadipogenic and peroxisome proliferator-Activated receptor γ(PPARI) activating properties. The systematic optimization of 3a, in order to improve its PPARγagonist activity, led to the synthesis of compound 7j (N-Aryl-substituted valine derivative) that possesses dual PPARI/PPARα agonistic activity. Structural and kinetic analyses reveal that 7j occupies the typical ligand binding domain of the PPARγagonists with, however, a unique high-Affinity binding mode. Furthermore, 7j is highly effective in preventing cyclin-dependent kinase 5-mediated phosphorylation of PPARγserine 273. Although less proadipogenic than rosiglitazone, 7j significantly increases adipocyte insulin-stimulated glucose uptake and efficiently promotes white-To-brown adipocyte conversion. In addition, 7j prevents oleic acid-induced lipid accumulation in hepatoma cells. The unique biochemical properties and biological activities of compound 7j suggest that it would be a promising candidate for the development of compounds to reduce insulin resistance, obesity, and nonalcoholic fatty liver disease.
- Peiretti, Franck,Montanari, Roberta,Capelli, Davide,Bonardo, Bernadette,Colson, Cécilia,Amri, Ez-Zoubir,Grimaldi, Marina,Balaguer, Patrick,Ito, Keiichi,Roeder, Robert G.,Pochetti, Giorgio,Brunel, Jean Michel
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p. 13124 - 13139
(2020/12/02)
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- Substituted pyrrole chromone compound or pharmaceutically acceptable salt thereof and preparation method and application thereof
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The invention discloses a substituted pyrrole chromone compound or pharmaceutically acceptable salt thereof and a preparation method and application thereof. The structure of the compound or the pharmaceutically acceptable salt thereof is shown in the for
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Paragraph 0081; 0087-0089
(2019/01/23)
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- CRYSTALLINE LEVODOPA AMIDE FREE BASE AND METHODS OF MAKING AND USING SAME
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A crystalline levodopa amide free base and a process of making it are provided. Particularly, a substantially pure crystalline levodopa amide free base is disclosed, suitable for the preparation of pharmaceutical compositions for treatment of diseases or
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Paragraph 0129; 0130
(2019/03/12)
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- PROCESS FOR PREPARING PURIFIED LEVODOPA AMIDE
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Disclosed herein, in part, are processes of large scale purification of a L- dopamide pharmaceutically acceptable salt and processes of making a purified pharmaceutically acceptable L-dopamide and pharmaceutically acceptable L-dopamide salts substantially
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Paragraph 0157; 0158
(2019/03/12)
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- Rosmarinic acid derivative as well as preparation method and application thereof
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The invention relates to a rosmarinic acid derivative as well as a preparation method thereof. The rosmarinic acid analog provided by the invention or a salt which comprises a medicine of the analog and is clinically acceptable has good application prospe
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Paragraph 0012
(2019/12/25)
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- Synthesis and biological evaluation of clovamide analogues with catechol functionality as potent Parkinson's disease agents in vitro and in vivo
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In this study, seven clovamide analogues (1–7) were designed and synthesized, and the neuroprotection of 1–7 as well as 8–15 (prepared in our previous work) against H2O2-induced oxidative stress was evaluated in SH-SY5Y cells. Results showed that 1–7 with catechol groups exhibited better neuroprotective effects than 8–15, and their EC50 values ranged from 4.26 to 23.83 μM, especially 1, indicating that the moiety of catechol governed the activities of these compounds. Furthermore, oral administration of 1 (10 or 20 mg/kg) was demonstrated to possess anti-PD effect through alleviating apoptosis and oxidative stress in vitro and in vivo, and to up-regulate the expression of heme oxygenase-1 (HO-1) via PI3K/AKT/mTOR pathway. Finally, the pharmacokinetic (PK) assessment of 1 was determined in rats. These findings suggested that 1 might be an effective candidate for PD therapy.
- Feng, Jia-Hao,Hu, Xiao-Long,Lv, Xian-Yu,Wang, Bao-Lin,Lin, Jun,Zhang, Xiao-Qi,Ye, Wen-Cai,Xiong, Fei,Wang, Hao
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supporting information
p. 302 - 312
(2018/11/27)
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- Structure-activity relationship of clovamide and its related compounds for the inhibition of amyloid β aggregation
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Alzheimer's disease (AD), a neurodegenerative disorder, is characterized by aggregation of amyloid β-protein (Aβ). Aβ aggregates through β-sheet formation and induces cytotoxicity against neuronal cells. Inhibition of Aβ aggregation by naturally occurring compounds is thus a promising strategy for the treatment of AD. We have already reported that caffeoylquinic acids and phenylethanoid glycosides, which possess two or more catechol moieties, strongly inhibited Aβ aggregation. Clovamide (1) containing two catechol moieties, isolated from cacao beans (Theobroma cacao L.), is believed to exhibit preventive effects on Aβ aggregation. To investigate the structure-activity relationship of clovamide (1) for the inhibition of Aβ aggregation, we synthesized 1 and related compounds 2–11 through reaction between L-DOPA, D-DOPA, L-tyrosine, or L-phenylalanine and caffeic acid, p-coumaric acid, or cinnamic acid, and compounds 12 and 13 were derived from 1. Among tested compounds 1–13, those containing one or two catechol moieties exhibited potent anti-aggregation activity, whereas the non-catechol-type related compounds showed little or no activity. This suggests that at least one catechol moiety is essential for inhibition of Aβ42 aggregation, and this activity increases depending on the number of catechol moieties. Consequently, clovamide (1) and its related compounds may be a promising therapeutic option for inhibiting Aβ-mediated pathology in AD.
- Tsunoda, Tatsuhiko,Takase, Mio,Shigemori, Hideyuki
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p. 3202 - 3209
(2018/05/05)
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- Crown-ether-modified cyclic dipeptides as supramolecular chiral catalysts
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With the objective to develop supramolecular catalysts for useful chemical transformations, we report here a rapid and efficient solid-phase synthesis of novel cyclic dipeptides (crown-CDPs) with a diversity of L-DOPA derived crown ether substituents and
- Bérubé, Christopher,Voyer, Normand
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p. 184 - 195
(2017/10/26)
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- Large Amino Acid Transporter 1 Selective Liposomes of l -DOPA Functionalized Amphiphile for Combating Glioblastoma
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Despite significant progress in neurosurgery and radiation therapy during the past decade, overall survivability (OS) of glioblastoma patients continues to be less than 2 years. The scope of systemic chemotherapy is greatly limited by poor drug transport
- Bhunia, Sukanya,Vangala, Venugopal,Bhattacharya, Dwaipayan,Ravuri, Halley Gora,Kuncha, Madhusudana,Chakravarty, Sumana,Sistla, Ramakrishna,Chaudhuri, Arabinda
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p. 3834 - 3847
(2017/11/15)
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- GLYCOAMINO ACID AND USE THEREOF
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An object of the present invention is to provide an amino acid precursor which shows improvement in the properties (particularly water-solubility, stability in water, bitter taste etc.) of amino acid, and can be converted to amino acid in vivo etc. The present invention relates to a compound for an amino acid precursor, which is a compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof.
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Paragraph 0288-0290
(2017/01/26)
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- The Regioselective Synthesis of o -Nitrobenzyl DOPA Derivatives
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Photocaged DOPA derivatives may serve for non-invasive unmasking of the catechol fragment in biological systems. This would enable efficient control of the redox and metal-coordinating properties associated with the free catechol moiety, in particular, in biosynthetically produced adhesive proteins and synthetic peptides. Synthetic routes towards photocaged DOPA derivatives are reported herein. A new method for preparing para -alkylated DOPA starting from 3,4-dihydroxybenzaldehyde is described for the first time.
- Schneider, Tobias,Martin, Joshua,Durkin, Patrick M.,Kubyshkin, Vladimir,Budisa, Nediljko
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p. 2691 - 2699
(2017/06/13)
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- Synthesis of clovamide analogues that inhibit no production in activated BV-2 microglial cells
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A series of methyl ester of clovamide analogues, where the hydroxyl group of catechol moiety in caffeic acid and L-3,4-dihydroxyphenylalanine (L-dopa) was replaced with various functional groups, were synthesized and their inhibitory effects on nitric oxi
- Park, Ju-Young,Kim, Byung-Wook,Lee, Hae Un,Choi, Dong-Kug,Yoon, Sung-Hwa
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p. 1475 - 1482
(2017/09/23)
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- COPPER CATALYZED [18F]FLUORINATION OF IODONIUM SALTS
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Copper-catalyzed radiofluorination of iodonium salts, iodonium salts, and compounds obtained by copper-catalyzed radiofluorination of iodonium salts are disclosed. Diagnostic and therapeutic methods involving such compounds also are disclosed.
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Paragraph 0083
(2017/04/28)
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- GLYCOAMINO ACID AND USE THEREOF
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An object of the present invention is to provide glycoamino acid as an amino acid precursor with improved properties (particularly water-solubility, stability in water, bitter taste etc.). The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a salt thereof.
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Page/Page column 9
(2016/08/17)
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- Synthesis and antiproliferative activity of two diastereomeric lignan amides serving as dimeric caffeic acid-l-DOPA hybrids
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Two new diastereomeric lignan amides (4 and 5) serving as dimeric caffeic acid-l-DOPA hybrids were synthesized. The synthesis involved the FeCl3-mediated phenol oxidative coupling of methyl caffeate to afford trans-diester 1a as a mixture of en
- Magoulas, George E.,Rigopoulos, Andreas,Piperigkou, Zoi,Gialeli, Chrysostomi,Karamanos, Nikos K.,Takis, Panteleimon G.,Troganis, Anastassios N.,Chrissanthopoulos, Athanassios,Maroulis, George,Papaioannou, Dionissios
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supporting information
p. 132 - 144
(2016/05/24)
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- An aryl benzofuranacetic such amide derivatives and medical use (by machine translation)
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The invention refers to an aryl benzofuranacetic such amide derivatives and medical use, preparation method, the derivatives having anti-oxidation activity, with xanthine oxidase inhibiting activity, can be used for the preparation of anti-oxidation, and
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Paragraph 0140; 0141; 0142; 0143; 0144; 0145; 0146
(2016/10/31)
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- Synthesis and evaluation of xanthine oxidase inhibitory and antioxidant activities of 2-arylbenzo[b]furan derivatives based on salvianolic acid C
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Xanthine oxidase (XO) is the key enzyme in humans which is related to a variety of diseases such as gout, hyperuricemia and cardiovascular diseases. In this work, a series of 2-arylbenzo[b]furan derivatives were synthesized based on salvianolic acid C, and they were evaluated for xanthine oxidase inhibitory and antioxidant activities. Compounds 5b, 6a, 6e and 6f showed potent xanthine oxidase inhibitory activities with IC50values ranging from 3.99 to 6.36?μM, which were comparable with that of allopurinol. Lineweaver-Burk plots analysis revealed that the representative derivative 6e could bind to either xanthine oxidase or the xanthine oxidase-xanthine complex, which exhibited a mixed-type competitive mechanism. A DPPH radical scavenging assay showed most of the hydroxyl-functionalized 2-arylbenzo[b]furan derivatives possessed the potent antioxidant activity, which was further validated on LPS-stimulated RAW 264.7 macrophages model. The structure-activity relationships were preliminary analyzed and indicated that the structural skeleton of 2-arylbenzo[b]furan and phenolic hydroxyl groups played an important role in maintaining xanthine oxidase inhibitory effect and antioxidant property for the series of derivatives. Meanwhile, molecular docking studies were performed to further confirm the structure-activity relationships and investigate the proposed binding mechanisms of compounds 5d, 6d and 10d binding to the protein.
- Tang, Hong-Jin,Zhang, Xiao-Wei,Yang, Lin,Li, Wei,Li, Jia-Huang,Wang, Jin-Xin,Chen, Jun
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p. 637 - 648
(2016/09/14)
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- Synthesis of cross-linkable 2,5-diketopiperazine derivatives
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Synthesis of cross-linkable diketopiperadine derivatives is described. Cross-linkable aamino acid methyl esters were subjected to peptide synthesis with Boc-protected glycine or L-tyrosine. No protection of cross-linkable functional groups (catechol and p
- Yoshida, Takuma,Wang, Lei,Nakagawa, Shiori,Tachrim, Zetryana Puteri,Sakihama, Yasuko,Hashidoko, Yasuyuki,Hashimoto, Makoto
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p. 544 - 548
(2015/10/05)
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- Development of an iron(II)-catalyzed aerobic catechol cleavage and biomimetic synthesis of betanidin
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An aerobic iron(II)-catalyzed cleavage of catechols was developed. This reaction allows for the preparation of 2-methoxy-2H-pyrans that can be employed as versatile building blocks for synthesis. The utility of this biomimetic oxidative cleavage is featured in the synthesis of betanidin, a natural colorant with antioxidant properties. Cut and paste: An aerobic iron(II)-catalyzed oxidative cleavage of catechol was developed. This reaction allows the preparation of 2H-pyrans that can be employed as versatile building blocks for synthesis. The utility of this biomimetic cleavage is featured in the synthesis of betanidin, the aglycone of red beets' principal colorant and itself a valuable antioxidant (see scheme).
- Guimond, Nicolas,Mayer, Peter,Trauner, Dirk
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supporting information
p. 9519 - 9523
(2014/08/18)
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- Copper-catalyzed [18F]fluorination of (Mesityl)(aryl)iodonium salts
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A practical, rapid, and highly regioselective Cu-catalyzed radiofluorination of (mesityl)(aryl)iodonium salts is described. This protocol utilizes [18F]KF to access 18F-labeled electron-rich, -neutral, and -deficient aryl fluorides under a single set of mild conditions. This methodology is applied to the synthesis of protected versions of two important radiotracers: 4-[18F]fluorophenylalanine and 6-[ 18F]fluoroDOPA.
- Ichiishi, Naoko,Brooks, Allen F.,Topczewski, Joseph J.,Rodnick, Melissa E.,Sanford, Melanie S.,Scott, Peter J.H.
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supporting information
p. 3224 - 3227
(2014/07/08)
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- Design, synthesis and biological evaluation of peptide derivatives of l-dopa as anti-parkinsonian agents
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A series of dipeptide derivatives of l-dopa were synthesized and investigated for their pharmacological activity using the unilaterally 6-hydroxydopamine (6-OHDA)-lesioned rat as an experimental model of Parkinson's disease. Among them, (S)-isopropyl 2-(2-amino-2-methylpropanamido)-3-(3,4- dihydroxyphenyl)propanoate (4g) was found to be the most active compound, with 106% AUC activity and 149% peak activity of l-dopa after oral administration.
- Zhou, Tao,Hider, Robert C.,Jenner, Peter,Campbell, Bruce,Hobbs, Christopher J.,Rose, Sarah,Jairaj, Mark,Tayarani-Binazir, Kayhan A.,Syme, Alexander
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p. 5279 - 5282
(2013/09/23)
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- Sustainable and bio-inspired chemistry for robust antibacterial activity of stainless steel
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We report on the original synthesis of a poly(methacrylamide) bearing (oxidized) 3,4-dihydroxyphenylalanine specially designed to (i) insure film growth by covalent coupling, (ii) covalently bind an antibacterial peptide and (iii) contribute to the film c
- Faure, Emilie,Lecomte, Philippe,Lenoir, Sandrine,Vreuls, Christelle,Van De Weerdt, Cecile,Archambeau, Catherine,Martial, Joseph,Jerome, Christine,Duwez, Anne-Sophie,Detrembleur, Christophe
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supporting information; body text
p. 7901 - 7904
(2011/12/16)
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- Synthesis and in vitro cytotoxicity profile of the R-enantiomer of 3,4-dihydroxymethamphetamine (R-(-)-HHMA): Comparison with related catecholamines
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(±)-3,4-Methylenedioxymethamphetamine (MDMA, also known as "ecstasy") is a chiral drug that is essentially metabolized in humans through O-demethylenation into 3,4-dihydroxymethamphetamine (HHMA). There has recently been a resurgence of interest in the po
- Felim, Anne,Herrera, Guadalupe,Neudoerffer, Anne,Blanco, Manuel,O'Connor, Jose-Enrique,Largeron, Martine
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experimental part
p. 211 - 219
(2011/02/22)
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- Design, synthesis and biological evaluation of l-dopa amide derivatives as potential prodrugs for the treatment of Parkinson's disease
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A range of amide derivatives of l-dopa were synthesized and investigated for their pharmacological activity and their ability to be converted to l-dopa using the unilaterally 6-hydroxydopamine (6-OHDA)-lesioned rat, as an experimental model of Parkinson's
- Zhou, Tao,Hider, Robert C.,Jenner, Peter,Campbell, Bruce,Hobbs, Christopher J.,Rose, Sarah,Jairaj, Mark,Tayarani-Binazir, Kayhan A.,Syme, Alexander
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experimental part
p. 4035 - 4042
(2010/10/02)
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- Oxidative nucleophilic substitution (SNOX) of the benzylic position as a tunable synthesis of tetrahydroisoquinoline natural alkaloid analogues
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Synthetic investigations of 1,3-dichloro-5,6-dicyanobenzoquinone-mediated benzylic oxidation is reported for the synthesis of natural alkaloid analogues. Extensive explorations of the oxidative nucleophilic substitution of the benzylic position of β-phenylethylamine derivatives and the synthesis of functionalized tetrahydroisoquinolines of ecteinascidin 743 precursors have been carried out. Starting from L-DOPA, a tunable oxazolidinone group was installed under oxidative benzylic conditions. This derivative 13 was submitted to benzylic oxidation reactions using a wide range of carboxylic acids and subsequent chemical transformations of these compounds were attempted. Moreover, an efficient synthesis of an aromatic ketone derivative 20 was achieved and gave rise to tetrahydroisoquinoline 24 through a direct Pictet-Spengler cyclisation reaction. Subsequently, 24 was transformed into functionahzed α-amino alcohols 31a and 31b, precursors of ecteinascidin 743 analogues. In addition, in order to assess the viability of our synthetic strategy, the reaction of 24 with methyl thioglycolate was performed and the stereoselectivity confirmed by X-ray analysis of 33a. Wiley-VCH Verlag GmbH & Co. KGaA, 2007.
- Aubry, Sylvain,Pellet-Rostaing, Stephane,Lemaire, Marc
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p. 5212 - 5225
(2008/03/18)
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- Racemic and diastereoselective synthesis of aryl and heteroaryl tetrahydroisoquinolines via the Pictet-Spengler reaction
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New tetrahydroisoquinolines were synthesized by the Pictet-Spengler reaction. Influence of a wide range of aryl and heteroaryl aldehydes, was investigated in the cyclization step with 3,4-dimethoxyphenylethylamine 1, L-DOPA 2 and L-3,4-dimethoxyphenylalan
- Aubry, Sylvain,Pellet-Rostaing, Stephane,Faure, Rene,Lemaire, Marc
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p. 139 - 148
(2007/10/03)
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- Synthesis of terminally protected (S)-β3-H-DOPA by Arndt-Eistert homologation: An approach to crowned β-peptides
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Terminally protected Boc-(S)-β3-H-DOPA-OMe has been synthesized from l-DOPA by the Arndt-Eistert homologation procedure. During the synthesis, the side-chain catechol group was temporarily protected by benzylation. The absence of racemization w
- Gaucher, Anne,Dutot, Laurence,Barbeau, Olivier,Hamchaoui, Wahib,Wakselman, Michel,Mazaleyrat, Jean-Paul
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p. 857 - 864
(2007/10/03)
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- 1,2-Benzothiazine 1,1-dioxide P2-P3 peptide mimetic aldehyde calpain I inhibitors
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A series of peptide mimetic aldehyde inhibitors of calpain I was prepared in which the P2 and P3 amino acids were replaced by substituted 3,4-dihydro-1,2-benzothiazine-3-carboxylate 1,1-dioxides. The effect of 2, 6, and 7-benzothiazi
- Wells,Tao,Josef,Bihovsky
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p. 3488 - 3503
(2007/10/03)
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- BENZOTHIAZO AND RELATED HETEROCYCLIC GROUP-CONTAINING CYSTEINE AND SERINE PROTEASE INHIBITORS
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The present invention is directed to novel benzothiazo and related heterocyclic group-containing inhibitors of cysteine or serine proteases. Methods for using the same are also described.
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- The transformation of dihydroxyphenylalanine (DOPA) to metal uptake systems and ionophores
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The crafting of DOPA to metal uptake systems and ionophores, by attachment of ligands to the hydroxyl groups, is illustrated.
- Ranganathan, Subramania,Tamilarasu, Natarajan
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p. 727 - 731
(2007/10/03)
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- STUDIES ON m-CYCLOPHANE FORMATION FROM THE PHOTOLYSIS OF CHLOROACETAMIDE DERIVATIVES
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The synthesis of 12-hydroxy-2-oxa-6-azabicyclotrideca-1(13),9,11-trien-5-one (4) is described.Two routes to (4) based on the photolysis of N-chloroacetamide (2b) and N-chloroacetamide (2c) followed by O-demethylation or O-desilylation, were developed.Extension of the work has given the new m-cyclophane ester derivative (9), whose structure has been confirmed by X-ray crystallography.
- Rezaie, Robert,Bremner, John B.,Blanch, Gregory K.,Skelton, Brian W.,White, Allan H.
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p. 959 - 972
(2007/10/02)
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- Novel, transient pro-drug forms of L-DOPA
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There is provided, novel, transient pro-drug forms of L-DOPA (3,4-dihydroxy-L-phenylalanine), having the formula: STR1 wherein n represents an integer of from 2 to 50 with respect to formula (V-A), and wherein n represents an integer of from 1 to 50 with respect to formula (V-B); R represents a hydrogen atom, an acyl group, STR2 --CO-pyridyl, or --CO--R3, wherein R3 is the residue of any N,N-C1 -C2 dialkylamino acid or a C4 -C6 cycloalkylamino acid; R1 represents --OH, --O-lower alkyl, --O-benzyl, or a naturally occurring protein amino acid; and R2 represents STR3 --CO-pyridyl, a naturally occurring protein amino acid, 3',4'-L-diacyloxy phenylalanine, or --CO-R3. These compounds are all useful in the treatment of Parkinson's Disease.
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- Effervescent enteric coated L-dopa formulation and method of using the same
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Therapeutic levels of L-DOPA are achieved by orally administering a pharmaceutical effervescent-enteric coated tablet comprising: A. a member selected from the group consisting of L-DOPA or a derivative thereof capable of enzymatically cleaving and reverting to L-DOPA in vivo, B. a non-toxic pharmaceutically acceptable inert diluent, C. a non-toxic pharmaceutically acceptable carbon dioxide releasing agent, D. a non-toxic pharmaceutically acceptable effervescing agent, and E. a non-toxic pharmaceutically acceptable enteric coating. This composition is extremely useful in the treatment of Parkinsonism. When administered to warm-blooded animals (e.g., humans), superior therapeutic blood levels of L-DOPA are observed over that normally observed with conventional enteric coated formulations.
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