Showing papers by "Pascal De Tullio published in 1999"
Journal Article•
TL;DR: This review presents the recent developments (since 1995) in the chemistry of CCK receptor ligands.
Abstract: During the last few years, cholecystokinin (CCK) has emerged as an important hormone This polypeptide has been located either in peripheral tissues such as the gastro-intestinal tract and the pancreas as well as in the central nervous system High affinity CCK receptors are divided in two main subtypes: the CCK-A (A for (A for "alimentary") and the CCK-B (B for "brain") receptors The latters are currently associated with the gastrin receptors Since CCK is involved in many different biological processes such as gut function, digestive processes, control of feeding behaviour and neurotransmitter release, the therapeutical potential of cholecystokinin receptor ligands seems to be extremely broad and promising Several families of CCK receptor ligands (peptides, peptidomimetics, peptoids or non-peptides) were prepared during the last twenty years The main goal of these researches was to improve agonistic or antagonistic potency but also to find selective compounds for a specific CCK receptor subtype This review presents the recent developments (since 1995) in the chemistry of CCK receptor ligands
28 citations
TL;DR: The R-isomer of BPDZ 42 was shown to be more potent than its corresponding S-isomers on the endocrine pancreas and S-BPDZ 44 as well as R- andS-B PDZ 42 were found to exhibit tissue selectivity for the pancreatic versus the vascular smooth muscle tissue.
19 citations
TL;DR: In this paper, the position of the CN double bond in the thiadiazine ring may exist under three different tautomeric forms: 2-, 3-, 4-, and 5-position.
13 citations
TL;DR: The use of amino acid derivatives as chiral derivatizing agents (CDA) was investigated in this article, where the (L)-phenylalanine methyl ester was found to be very effective to separate pirlindole enantiomers using a medium pressure liquid chromatographic (MPLC) method.
8 citations
Patent•
30 Nov 1999
TL;DR: 4H-1,2,4,4-Benzothiadiazine 1,1-dioxide derivatives of formula (I), their isomers and salts, are new as discussed by the authors.
Abstract: 4H-1,2,4-Benzothiadiazine-1,1-dioxide derivatives (I), are new. 4H-1,2,4-Benzothiadiazine-1,1-dioxide derivatives of formula (I), their isomers and salts, are new. X = F, Br, Cl, I, or methyl; and R1, R2 = H or 1-6C alkyl.
3 citations
TL;DR: Pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides bearing a short and branched alkylamino side chain in the 3 position, appear to be powerful and tissue selective pancreatic KATP-channel activators.
Abstract: Pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides bearing a short and branched alkylamino side chain in the 3 position, appear to be powerful and tissue selective pancreatic KATP-channel activators. In order to confirm the pharmacophoric model for the activation of pancreatic KATP channels, a structural study was undertaken on representative 3-alkyl-aminopyridothiadiazines. The influence on the biological activity of the stereochemistry associated to the first carbon atom of the 3-alkylamino chain was also examined.
3 citations
TL;DR: In this article, the position of the CN double bond in the thiadiazine ring may exist under three different tautomeric forms: 2-, 3-, 4-, and 5-position.
Abstract: 3-Alkylamino-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide represents a new class of heterocyclic compounds expressing important pharmacological properties. According to the position of the CN double bond in the thiadiazine ring, this heterocyclic ring system may exist under three different tautomeric forms. By means of spectral and X-ray data collected from selected compounds, the most favourable tautomeric form adopted by 3-alkylamino-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides devoid of an alkyl substituent in the 2- or in the 4-position was determined. The present study giving new insights in the geometrical and conformational aspects of pyridothiadiazinedioxides is important considering the pharmacological potentialities of this class of heterocyclic compounds.
2 citations