- Highly Convergent Total Synthesis and Assignment of Absolute Configuration of Majusculamide D, a Potent and Selective Cytotoxic Metabolite from Moorea sp.
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The total synthesis of majusculamide D (MJS-D) is described, a lipopentapeptide originally isolated from Lyngbya majuscula and reisolated from a Moorea sp. MJS-D possesses selective and potent cancer cell toxicity. A scalable and convergent strategy with a minimal number of purifications produced significant quantities of MJM-D for in vivo evaluations. The absolute configuration of the 1,3-dimethyl-octanamide motif was determined by synthesis of this fragment via ZACA chemistry.
- Caro-Diaz, Eduardo J. E.,Valeriote, Frederick A.,Gerwick, William H.
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supporting information
p. 793 - 796
(2019/02/07)
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- Pharmaceutical combination of an atypical antipsychotic and an NMDA modulator for the treatment of schizophrenia,bipolar disorder, cognitive impairment and major depressive disorder
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This disclosure features combinations of NMDA modulators and atypical antipsychotics. The disclosure provides for example, methods of treating schizophrenia, bipolar disorder, and/or cognitive impairment disorder in a patient in need thereof, comprising administering e.g., rapastinel and an atypical antipsychotic.
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Paragraph 0179; 0216; 0217
(2018/10/11)
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- Clickable glycopeptoids for synthesis of glycopeptide mimic
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Structurally diverse novel glycopeptoids were synthesized which can be attached to biologically important peptides by click reaction to improve their potential to be used in medicinal chemistry. Triazole-linked αβ-hydrid glycopeptoids were synthesized that mimic the conserved linkage region of N-linked glycoproteins in eukaryotes. The amide bonds were replaced with triazole rings, and αβ-hybrid peptoids were introduced as the backbone modification in peptidomimetics. In addition to their facile synthesis, these modifications have the possibility of introducing otherwise impossible conformations in the peptide backbone.
- Singhamahapatra, Anadi,Sahoo, Laxminarayan,Loganathan, Duraikkannu
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p. 10329 - 10336
(2013/11/06)
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- Towards nucleopeptides containing any trifunctional amino acid
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Nucleopeptides incorporating, besides the linking residue, other trifunctional amino acids such as lysine, arginine, tryptophan, serine, threonine and tyrosine have been obtained following stepwise solid-phase assembly. The best alternatives for the prote
- Robles, Jordi,Beltran, Make,Marchan, Vicente,Perez, Yolanda,Travesset, Isaura,Pedroso, Enrique,Grandas, Anna
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p. 13251 - 13264
(2007/10/03)
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