- Fatty acid analogs and prodrugs
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Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitrites thereof. These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure STR1 in which x is the ethyl or t-butyl ester of an amino acid such as Gly, L-Ala, L-Ile, L-Phe, L-Trp, L-Thr or an amide such as NHCH2 C6 H5 or NH(CH2)2 C6 H5.
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- Fatty acid analogs and prodrugs
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Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof. These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure STR1 in which X is the ethyl or t-butyl ester of an amino acid such as Gly, L--Ala, L--Ile, L--Phe, L--Trp, L--Thr or an amide such as NHCH2 C6 H5 or NH(CH2)2 C6 H5,
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- Stable polypeptides having c-AMP production enhancing activity and the use thereof
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Disclosed are (1) a polypeptide represented by formula (I), or a pharmaceutically acceptable amide, ester or salt thereof: wherein X is hydrogen atom; or a lower alkyl group which may be substituted with a member selected from the group consisting of hydroxy group, substituted or unsubstituted amino group, carboxyl group, carbamoyl group, and substituted or unsubstituted aromatic group; and Y is one of amino acids or peptides consisting of 1 to 16 amino acid residues counted from the N-terminal side of Leu-Ala-Ala-Val-Leu-Gly-Lys-Arg-Tyr-Lys-Gln-Arg-Val-Lys-Asn-Lys SEQ ID NO: 20, and (2) a pharmaceutical composition comprising a polypeptide represented by formula (I), or a pharmaceutically acceptable amide, ester or salt thereof, which has remarkable c-AMP activity and is useful as a nerve activating agent.
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- Peptides related to somatostatin
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Peptides of the formula: STR1 wherein: X is H, --NH2, --NH--Gly--Ala, --NH--D--Ala--Ala, --NH--Gly--Gly--Gly, --NH--acetyl, or --NH--benzoyl; X1 is His or Arg; X2 is His, Glu, Tyr, Trp, or Phe; X3 is Trp, D-Trp, or 6-F-D-Trp; and X4 is a D-α-amino acid; or the reduced, linear form thereof, or a non-toxic, pharmaceutically acceptable acid addition salt thereof; inhibit the release of growth hormone, insulin, and glucagon; and show prolonged inhibition activity. Said peptides are prepared by solid-state methodology.
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- New Side-Chain Protecting Groups for Lysine and Tyrosine Suitable for Solid-Phase Peptide Synthesis
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The syntheses of two new lysine and tyrosine derivatives, Boc-Lys(2-ClZ) and Boc-Tyr(2-BrBzl) have been described.Their use in the solid-phase peptide synthesis of the decapeptide Glu-Arg(NO2)-Gly-Phe-Phe-Tyr-Thr-Pro-Lys-Thr (I) corresponding to the seque
- Salem, Ezzeldin M.,Schou, O.
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- Polypeptides related to somatostatin
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Compounds of the formula: STR1 wherein: X is H, Ala-Gly, Gly-Gly-Gly, Ala-D-Ala, acetyl, or benzoyl; X1 is Arg or His; X2 is Glu or Asp; X3 is Trp or D-Trp; or 6-F-D-Trp; and X4 is Cys- or D-Cys; or a non-toxic pharmaceutically acceptable acid addition salt thereof; inhibit the secretion of growth hormone and glucagon without materially affecting the secretion of insulin.
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