- Structural and morphological diversity of self-assembled synthetic γ-amino acid containing peptides
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Regulating the nanostructural morphology of synthetic hybrid peptides through external stimuli is still a great challenge. Here, we report the synthesis of constrained amino acid building block gabapentin (Gpn) based hybrid peptides and their structural a
- Konda, Maruthi,Kauffmann, Brice,Rasale, Dnyaneshwar B.,Das, Apurba K.
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- Photosensitized Intermolecular Carboimination of Alkenes through the Persistent Radical Effect
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An intermolecular, two-component vicinal carboimination of alkenes has been accomplished by energy transfer catalysis. Oxime esters of alkyl carboxylic acids were used as bifunctional reagents to generate both alkyl and iminyl radicals. Subsequently, addition of the alkyl radical to an alkene generates a transient radical for selective radical–radical cross-coupling with the persistent iminyl radical. Furthermore, this process provides direct access to aliphatic primary amines and α-amino acids by simple hydrolysis.
- Bellotti, Peter,Glorius, Frank,Patra, Tuhin,Strieth-Kalthoff, Felix
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supporting information
p. 3172 - 3177
(2020/02/05)
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- Novel cilengitide-based cyclic RGD peptides as αvβ3 integrin inhibitors
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In this letter, we report a series of five new RGD-containing cyclic peptides as potent inhibitors to αvβ3 integrin protein. We have incorporated various unnatural lipophilic amino acids into the cyclic RGD framework of cilengitide, which is selective for αvβ3 integrin. All the newly synthesized cyclic peptides were evaluated in vitro solid phase binding assay and investigated for their binding behaviour towards integrin subtypes. All the cyclic peptides were synthesized in excellent yield following solution-phase coupling strategy. The cyclic RGD peptides 1a-e exhibited IC50 of 9.9, 5.5, 72, 11 and 3.3 nM, respectively, towards αvβ3 integrin protein. This finding offers further opportunities for the introduction unusual amino acids into the cyclic peptide framework of cilengitide.
- Dangi, Abha,Marelli, Udaya Kiran,Meena, Chhuttan L.,Reichart, Florian,Sanjayan, Gangadhar J.,Singh, Dharmendra,Zahler, Stefan,Weinmüller, Michael
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supporting information
(2020/02/28)
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- Design, synthesis and anti-bacterial studies of piperazine derivatives against drug resistant bacteria
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In current research, five series of mono- and di-substituted piperazine derivatives have been synthesized. For di-substituted derivatives, ciprofloxacin was selected and hybrids were synthesized via substitution at piperazinyl-N4. In vitro anti
- Tahir, Saba,Mahmood, Tariq,Dastgir, Faiqa,Haq, Ihsan-ul,Waseem, Amir,Rashid, Umer
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supporting information
p. 224 - 231
(2019/02/05)
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- SUBSTITUTED TRIAZOLES AND METHODS RELATING THERETO
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Substituted 1,2,3-triazole compounds are disclosed which have utility in the treatment of a variety of neurological disorders. The compounds provided herein have the general structure wherein R1, R2, R3 and n are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound provided herein in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for treating neurological disorders in a subject in need thereof.
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(2016/08/23)
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- Gabapentin hybrid peptides and bioconjugates
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Synthetic approaches to gabapentin bioconjugates that overcome the tendency of gabapentin to cyclize into its γ-lactam are studied. Gabapentin was converted by N-acylation at its N-terminus into di-, tri-, and tetrapeptides (L-Ala-Gbp, L-Val-Gbp, L-Ala-L-Phe-Gbp, Gly-L-Ala-β-Ala-Gbp). Carboxyl-activated Boc-protected gabapentin was used to N-, O-, and S-acylate small peptides and hormones to give conjugates that could also provide prodrugs containing conformationally constrained gabapentin units.
- Lebedyeva, Iryna O.,Ostrov, David A.,Neubert, John,Steel, Peter J.,Patel, Kunal,Sileno, Sean M.,Goncalves, Kevin,Ibrahim, Mohamed A.,Alamry, Khalid A.,Katritzky, Alan R.
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supporting information
p. 1479 - 1486
(2014/03/21)
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- FUNCTIONALIZED 9-BROMO-CAMPTOTHECIN DERIVATIVES
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The present invention relates to new functionalized 9-bromo-camptothecin derivatives which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them. The invention also relates to the use of these functionalized 9-bromo-camptothecin derivatives in the preparation of conjugates.
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(2014/05/24)
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- Oxadiazolone bioisosteres of pregabalin and gabapentin
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A series of oxadiazolone bioisosteres of pregabalin 1 and gabapentin 2 were prepared, and several were found to exhibit similar potency for the α2-δ subunit of voltage-gated calcium channels. Oxadiazolone 9 derived from 2 achieved low brain upt
- Wustrow, David J.,Belliotti, Thomas R.,Capiris, Thomas,Kneen, Clare O.,Bryans, Justin S.,Field, Mark J.,Williams, Dic,El-Kattan, Ayman,Buchholz, Lisa,Kinsora, Jack J.,Lotarski, Susan M.,Vartanian, Mark G.,Taylor, Charles P.,Donevan, Sean D.,Thorpe, Andrew J.,Schwarz, Jacob B.
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scheme or table
p. 247 - 250
(2009/05/26)
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- Rigidified Compounds for Modulating Heparanase Activity
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Disclosed are novel rigidified compounds having a rhodanine-like residue and at least one aryl or heteroaryl residue linked to the rhodanine-like residue, whereby a core structure of these compounds, as defined in the specification, is characterized as having one or zero free-to-rotate bonds. Also disclosed are pharmaceutical compositions containing these rigidified compounds and uses thereof for modulating the activity of heparanase and hence in the treatment of heparanase-associated diseases and disorders, and uses thereof for modulating the activity of heparin-binding proteins and hence in the treatment of heparin-binding proteins-associated diseases and disorders as well as in the treatment of medical conditions that are at least partially treatable by rhodanine or a rhodanine analog.
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- Prodrugs containing novel bio-cleavable linkers
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The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.
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(2008/06/13)
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- BRANCHED CHAIN AMINO ACID-DEPENDENT AMINOTRANSFERASE INHIBITORS AND THEIR USE IN THE TREATMENT OF DIABETIC RETINOPATHY
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The present invention is directed to a method for the prophylactic and therapeutic treatment of diabetic retinopathy. The method involves the administration of an inhibitor of formulae (I), (II) and (III) of the branch chain amino acid-dependent aminotran
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- Method of treating tinnitus
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The invention relates to a method of treating tinnitus by administering an alpha2delta ligand such as, for example, a compound of Formula and pharmaceutically acceptable salts thereof, wherein R1 is hydrogen or straight or branched lower alkyl, and n is an integer of from 4 to 6.
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- 1-substituted-1-aminomethyl-cycloalkane derivatives (=gabapentin analogues), their preparation and their use in the treatment of neurological disorders
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Novel amines of formulas (1), (1C), (1F), (1G) and (1H) or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; A′ is a bridged ring selected from (1), (2), (3), (4), (5) wherein is the point of attachment; Z1to Z4are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, especially irritable bowel syndrome.
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- Amino acid conjugates providing for sustained systemic concentrations of gaba analogues
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This invention is directed to compounds that provide for sustained systemic concentrations of GABA analogs following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.
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- Method of treating cartilage damage
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The invention relates to a method of preventing or treating cartilage damage by administering a GABA analog such as, for example, a compound of Formula 1and pharmaceutically acceptable salts thereof, wherein R1 is hydrogen or straight or branched lower alkyl, and n is an integer of from 4 to 6.
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