Results 171 to 180 of about 3,651 (206)

Stereoselective synthesis of conformationally constrained reverse turn dipeptide mimetics

Tetrahedron Letters, 2001
Abstract Peptide side chains play critical roles in the event of molecular recognition. In order to study the bioactive conformation of parent peptides, a concise and straightforward five-step synthesis of [5.5]-bicyclic reverse turn dipeptide mimetic scaffolds with side chain functionality at the i +1 and i +2 positions has been developed.
Wei Qiu, Xuyuan Gu, Vadim A Soloshonok, Michael D Carducci, Victor J Hruby   +4 more
openaire   +1 more source

Morphiceptin Analogues Containing a Dipeptide Mimetic Structure:  An Investigation on the Bioactive Topology at the μ-Receptor

Journal of Medicinal Chemistry, 2005
We describe the design, the conformational behavior, and the biological activity at the mu-opioid receptor of new morphiceptin analogues. In these analogues a recently described dipeptide mimetic structure replaces both the N- and the C-terminal Xaa-Pro dipeptide of morphiceptin. Conformational investigation on the most active analogue, compared to the
GRIECO, PAOLO, L. Giusti, CAROTENUTO, ALFONSO, P. Campiglia, V. Calderone, T. Lama, GOMEZ MONTERREY, ISABEL MARIA, G. Tartaro, M. R. Mazzoni, NOVELLINO, ETTORE   +9 more
openaire   +6 more sources

Renin inhibitors containing new P1-P1' dipeptide mimetics with heterocycles in P1'

Journal of Medicinal Chemistry, 1992
A series of renin inhibitors containing new P1-P1' dipeptide mimetics are presented. The P1-P1' mimetics were obtained from (4S,5S)-3-(tert-butoxycarbonyl)-4-(cyclohexylmethyl)-5-[(omega- mesyloxy)alkyl]-2,2-dimethyloxazolidines 5b, 9, and 11b by nucleophilic substitution of the mesylate groups with the sodium salts of mercapto- and hydroxyheterocycles.
P, Raddatz, A, Jonczyk, K O, Minck, F, Rippmann, C, Schittenhelm, C J, Schmitges   +5 more
openaire   +2 more sources

Enediyne-bridged dipeptide mimetics

2008
Enediyne-bridged dipeptide mimetics were prepared in a straightforward manner and characterized by spectroscopic and mass spectrometry methods. Further, thermal reactivity of synthesized enediyne compounds towards the Bergman cycloaromatization were studied by differential scanning calorimetry.
Gredičak, Matija, Jerić, Ivanka
openaire   +1 more source

Dipeptide Mimetic of the BDNF GSB-106 with Antidepressant-Like Activity Stimulates Synaptogenesis

Доклады академии наук, 2018
Dipeptide mimetic of the brain-derived neurotrophic factor bis(N-monosuccinyl-L-seryl-L-lysine) hexamethylenediamide (working name GSB-106), which reproduces the homodimeric structure of BDNF and the beta-turn of its fourth loop, activates TrkB, AKT, and ERK, exhibits neuroprotective and antidepressant activity, and is able to stimulate neurogenesis in
T A, Gudasheva, P Yu, Povarnina, T A, Antipova, S B, Seredenin   +3 more
openaire   +2 more sources

An acyliminium ion route to and “Anti” phe-gly dipeptide mimetics

Bioorganic & Medicinal Chemistry Letters, 1991
Abstract The synthesis of two series of constrained mimetics of the dipeptide phenylalanylglycine oriented in the “anti” conformation (X1 = 180°) are described. These benzolactams differ about the geometry of the internal amide bond (ω1=0° or 180°). Solution NMR studies support specific conformational assignments for these mimetics. The synthesis of
Gary A. Flynn, Timothy P. Burkholder, Edward W. Huber, Philippe Bey   +3 more
openaire   +1 more source

Synthesis of GSK3β mimetic inhibitors of Akt featuring a novel extended dipeptide surrogate

Bioorganic & Medicinal Chemistry Letters, 2011
Akt is a cardinal nodal point in PI3K signaling pathway and confers resistance to apoptosis through inactivation of regulatory substrates such as GSK3β. Efforts to inhibit the kinase activity of Akt have largely focused on targeting the ATP-binding domain of Akt.
Sujeewa, Ranatunga, Juan R, Del Valle
openaire   +2 more sources

Anxiolytic Action of Dipeptide Mimetic of the BDNF Loop 2 in Adult Animals

Bulletin of Experimental Biology and Medicine
We studied the anti-anxiety effect of a low-molecular-weight mimetic of the BDNF loop 2, hexamethylenediamide bis-(-N-hexanoyl-L-seryl-L-lysine) (GTS-201) in adult animals. GTS-201 at a dose of 5 mg/kg after acute intraperitoneal administration to outbred male and female rats increased the time spent in the open arms and the number of entries into the ...
L G, Kolik, A V, Nadorova, E M, Grigorevskikh, N M, Sazonova, T A, Gudasheva   +4 more
openaire   +2 more sources

Substrate-Controlled and Organocatalytic Asymmetric Synthesis of Carbocyclic Amino Acid Dipeptide Mimetics

The Journal of Organic Chemistry, 2010
The asymmetric synthesis of a carbocyclic delta-amino acid representing the P(2)/P(3) subunit of a nonpeptidic truncated peptidomimetic molecule is described relying on two independent approaches.
Stephen, Hanessian, Dilip K, Maji, Subramaniyan, Govindan, Riccardo, Matera, Marina, Tintelnot-Blomley   +4 more
openaire   +2 more sources

Angiogenic Effects of Dimeric Dipeptide Mimetic of Loop 4 of Nerve Growth Factor

Bulletin of Experimental Biology and Medicine, 2016
Angiogenic action of compound GK-2, a dimeric dipeptide mimetic of loop 4 of nerve growth factor (NGF), was studied in in vitro and in vivo experiments.
S A, Kryzhanovskii, T A, Antipova, I B, Tsorin, E S, Pekeldina, V N, Stolyaruk, S V, Nikolaev, A V, Sorokina, T A, Gudasheva, S B, Seredenin   +8 more
openaire   +2 more sources