No description
-
2001 (v1)PublicationUploaded on: April 14, 2023
-
1991 (v1)Publication
No description
Uploaded on: April 14, 2023 -
1996 (v1)Publication
No description
Uploaded on: December 4, 2022 -
2015 (v1)Publication
No description
Uploaded on: April 14, 2023 -
1993 (v1)Publication
No description
Uploaded on: December 5, 2022 -
2002 (v1)Publication
Cyclic nucleotide phosphodiesterases (PDEs) catalyse the hydrolysis of the second messengers adenosine-3,5-cyclic phosphate cAMP and cGMP. At least 11 different PDE types have been described: each of these groups a number of subtypes and splice variants. The PDE types differ in their amino acid sequence, substrate specificity,...
Uploaded on: March 31, 2023 -
2003 (v1)Publication
In PUVA (Psoralen plus UVA) chemotherapy 8-methoxypsoralen is the most widely used compound, although its efficacy is endowedwith undesired side effects. In order to have an evident anti-proliferative activity with a reduced phototoxicity, many linear and angular derivatives have been synthesised. In this paper we describe a QSAR study in...
Uploaded on: April 14, 2023 -
1994 (v1)Publication
The synthesis of some 5-substituted 4-isoxazoleacetic acids starting from 5-substituted 4-isoxazolemethanols via their conversion to 4-(bromomethyl)isoxazoles, 4-isoxazoleacetonitriles and acid hydrolysis of the latter is described. 5-Ethyl- and 5-propyl-4-isoxazoleacetic acids showed in the writhing test an analgesic activity comparable to...
Uploaded on: March 31, 2023 -
1982 (v1)Publication
No description
Uploaded on: April 14, 2023 -
1982 (v1)Publication
No description
Uploaded on: March 31, 2023 -
1997 (v1)Publication
No description
Uploaded on: April 14, 2023 -
2008 (v1)Publication
No description
Uploaded on: April 14, 2023 -
2008 (v1)Publication
No description
Uploaded on: April 14, 2023 -
2003 (v1)Publication
A new class of cardiotonic agents characterized by a 2-pyridone structure was synthesized. Appropriate sym-2-dimethylaminomethylene-1,3-diones reacted with methylcyanoacetate to afford the desired compounds. These derivatives were evaluated for their ability in inducing cardiotonic response on guinea pig isolated myocardial preparations....
Uploaded on: April 14, 2023 -
1999 (v1)Publication
No description
Uploaded on: March 31, 2023 -
2009 (v1)Publication
Pyrazolo[3,4-b]pyridines have been recently presented as a novel class of adenosine A1 receptor antagonists. Depending on substitutions on some key positions of their scaffold they show selectivity towards A1, A2A or A3 receptors, which results in a variety of therapeutic potentialities of these ligands. In this work, we present a QSAR study...
Uploaded on: April 14, 2023 -
2002 (v1)Publication
A number of new furo and thienoquinolinones carrying an electron-withdrawing function or unsubstituted at the position 3 were synthesized in order to obtain new potential photochemotherapeutic agents with increased antiproliferative activity and decreased toxic side effects. Our interest in studying the SAR of these derivatives also prompted us...
Uploaded on: April 14, 2023 -
2008 (v1)Publication
Among cannabinoid type-1 (CB1) receptor antagonists, those developed around the 1,5-diarylpyrazole scaffold of rimonabant (Acomplia) are the most extensively investigated. In recent years, many SAR and QSAR reports on this topic have been published, focusing on the substitution and orientation of the N1 and C5 aryl functionalities and on the...
Uploaded on: April 14, 2023 -
2003 (v1)Publication
No description
Uploaded on: March 31, 2023 -
2002 (v1)Publication2- substituted 5-acetyl-1,6-dihydro-6-oxo-3-pyridinecarboxylates: synthesis and cardiotonic activity
A series of milrinone analogues, namely 2-substituted 5-acetyl-1,6-dihydro-6-oxo-3-pyridinecarboxylates 17-23, related carboxylic acids 24-27 and 6-substituted 3-acetyl 1,2-dihydro-2-pyridones 28 and 29, in which the cyano group was replaced by the acetyl function, was prepared. All the compounds were tested for their effects on contractile...
Uploaded on: March 31, 2023 -
2001 (v1)Publication
A series of azole derivatives, isoxazole or pyrimidine analogues of the antifungal drug bifonazole, were synthesized and tested in vitro against representative human pathogenic fungi (Candida albicans, Cryptococcus neoformans and Aspergillus fumigatus). They were also evaluated as antibacterial agents against Staphylococcus aureus and...
Uploaded on: April 14, 2023 -
1999 (v1)Publication
A series of milrinone analogues, namely 6-substituted 3-acetyl-5-acylpyridin-2(1H)-ones 4a-c, e, f and 7-substituted or unsubstituted 3-acetyl-7,8-dihydro-2,5(1H,6H)-quinolinediones 4g-j, in which the cyano group was replaced by the acetyl function, was prepared. In a preliminary pharmacological investigation on spontaneously beating atria from...
Uploaded on: April 14, 2023 -
1995 (v1)Publication
Convenient synthesis of 3-acyl-2H-furo[2,3-h]-1-benzopyran-2-ones, esters of 2-oxo-2H-furo[2,3-h]-1-benzopyran-3-carboxylic acid and 2H-furo[2,3-h]-1-benzopyran-3-carboxamides was accomplished via aromatization of the adducts obtained by a reaction between (E)-5-dimethyl-aminomethylene-6,7-dihydrobenzofuran-4(5H)-one and the appropriate...
Uploaded on: May 11, 2023 -
1991 (v1)Publication
The synthesis of a series of 5-substituted 4-isoxazolecarboxamides by reaction of eight 5-substituted 4-isoxazolecarbonyl chlorides with pyrrolidine, piperidine, morpholine and 4-trifluoromethylaniline is described. Some of these amides showed platelet antiaggregating activity in vitro slightly inferior to that of acetylsalicylic acid, as well...
Uploaded on: March 31, 2023 -
2000 (v1)Publication
A series of indazoloxypropanolamines 7 and 8, pindolol isosteres, were synthesized to extend the structure activity relationship (SAR) which was observed in an earlier series of related derivatives. Compounds 7, characterized by methyl substitution on the N-1 indazole nucleus, generally exhibited significant antiarrhythmic, local anaesthetic...
Uploaded on: April 14, 2023