- The design and synthesis of potent cyclic peptide VCAM-VLA-4 antagonists incorporating an achiral Asp-Pro mimetic
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The Asp-Pro sequence of the cyclic peptide Ac-HN-Tyr-Cys*-Asp-Pro-Cys*-OH (1) could be replaced with the achiral dipeptide mimetic 1-(2-aminoethyl)cyclpentylcarboxylic acid with retention of potent inhibition of the VCAM-VLA-4 interaction. (C) Elsevier Science Ltd. All rights reserved.
- Fotouhi, Nader,Joshi, Pramod,Fry, David,Cook, Charles,Tilley, Jefferson W.,Kaplan, Gerry,Hanglow, Angela,Rowan, Karen,Schwinge, Virginia,Wolitzky, Barry
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p. 1171 - 1173
(2007/10/03)
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- N-ACYL-N-QUINOLINYL OR ISOQUINOUNYL ALKYLAMINO ACIDS COMPOSITIONS AND METHOD OF USE
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The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula STR1 The compounds and their pharmaceutically acceptable salts can be used as antihypertensives, agents for the treatment of glaucoma, or for increasing the flow of the retinal
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- ACYL COMPOUNDS
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Compounds of the formula STR1 in which R 1 is an aliphatic hydrocarbon radical which is unsubstituted or substituted by halogen or hydroxyl, or a cycloaliphatic or araliphatic hydrocarbon radical; X 1 is CO, SO 2, or--O--C(=O)--with the carbon atom of the carbonyl group being attached to the nitrogen atom shown in formula I; X 2 is a divalent aliphatic hydrocarbon radical which is unsubstituted or substituted by hydroxyl, carboxyl, amino, guanidino or a cycloaliphatic or aromatic radical, or is a divalent cycloaliphatic hydrocarbon radical, it being possible for a carbon atom of the aliphatic hydrocarbon radical to be additionally bridged by a divalent aliphatic hydrocarbon radical; R. sub.2 is carboxyl which, if desired, is esterified or amidated, substituted or unsubstituted amino, formyl which, if desired, is acetalized, 1H-tetrazol-5-yl, pyridyl, hydroxyl which, if desired, is etherified, S(O) m--R where m is 0, 1 or 2 and R is hydrogen or an aliphatic hydrocarbon radical, alkanoyl, unsubstituted or N-substituted sulfamoyl or PO n H 2 where n is 2 or 3; X 3 is a divalent aliphatic hydrocarbon; R 3 is carboxyl, 5-tetrazolyl, SO. sub.3 H, PO. sub.2 H 2, PO 3 H 2 or haloalkylsulfamoyl; and the rings A and B independently of one another are substituted or unsubstituted; in free form or in salt form, can be prepared in a manner known per se and can be used, for example, as medicament active ingredients.
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- N-SUBSTITUTED HETEROCYCLIC DERIVATIVES, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE PRESENT
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The invention relates to N-substituted heterocyclic derivatives and its salts. These derivatives have the formula (I) in which the substituents are as defined in the specification. Application: Angiotensin II antagonists
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