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5. Ethyl or methyl 6-substituted 3-(benzoylamino)-2-oxo-2H-pyran-5-carboxylates and 3-(benzoylamino)-7,8-dihydro-2H-1-benzopyran-2,5(6H)-diones with local anesthetic, platelet antiaggregating and other activities

Author

Mosti, L., Menozzi, G., Schenone, P., michele d'amico, Falciani, M., Rossi, F., Mosti, L, Menozzi, G, Schenone, P, D'Amico, Michele, Falciani, M, and Rossi, Francesco

Subjects
Magnetic Resonance Spectroscopy, Spectrophotometry, Infrared, Anti-Inflammatory Agents, Non-Steroidal, In Vitro Techniques, Carrageenan, Rats, Mice, Coumarins, Pyrones, Animals, Edema, Humans, Spectrophotometry, Ultraviolet, Anesthetics, Local, Anti-Arrhythmia Agents, Platelet Aggregation Inhibitors, Pain Measurement
Abstract

The synthesis of ethyl or methyl 6-substituted 3-(benzoylamino)-2-oxo-2H-pyran-5-carboxylates 2 and 3-(benzoylamino)-7,8-dihydro-2H-1-benzopyran-2,5(6H)-diones 4 by reaction of hippuric acid in acetic anhydride with ethyl or methyl 2-dimethylaminomethylene-3-oxoalkanoates and 2-dimethylaminomethylene-1,3-cyclohexanediones, respectively, is described. Some compounds 2 and 4 showed a strong local anesthetic activity in mice and a platelet antiaggregating activity in vitro comparable to that of acetylsalicylic acid, as well as moderate analgesic, antiinflammatory and antiarrhythmic activities in rats and mice.

Published
1994

6. 1-Aryl-1H-pyrazole-5-acetic acids with antiinflammatory, analgesic and other activities

Author

Menozzi, G., Mosti, L., Schenone, P., michele d'amico, Falciani, M., Filippelli, W., Menozzi, G, Mosti, L, Schenone, P, D'Amico, Michele, Falciani, M, and Filippelli, W.

Subjects
Magnetic Resonance Spectroscopy, Fever, Platelet Aggregation, Spectrophotometry, Infrared, Anti-Inflammatory Agents, Non-Steroidal, Acetates, In Vitro Techniques, Carrageenan, Rats, Mice, Animals, Edema, Humans, Pyrazoles, Collagen, Platelet Aggregation Inhibitors, Pain Measurement
Abstract

Reaction of methyl 4-methoxy-2-dimethylaminomethylene-3-oxobutanoate with arylhydrazines gave methyl 1-aryl-5-(methoxymethyl)-1H-pyrazole-4-carboxylates 1 in high yields. Esters 1 were hydrolyzed to the relative carboxylic acids, which were converted by heating to 1-aryl-5-(methoxymethyl)-1H-pyrazoles 3 in good yields. Reaction of 3 with hydrobromic acid afforded the intermediate 1-aryl-5-(bromomethyl)-1H-pyrazoles, which were converted with potassium cyanide to 1-aryl-1H-pyrazole-5- acetonitriles, whose hydrolysis gave the required 1-aryl-1H-pyrazole-5-acetic acids. Some acids 5 showed a strong antiinflammatory and analgesic activity in rats and mice, respectively, as well as moderate antipyretic and in vito platelet antiaggregating effects.

Published
1994

11. 4-substituted 1-methyl-1H-indazoles with analgesic, antiinflammatory and antipyretic activities

Author

Mosti, L., Menozzi, G., Fossa, P., Schenone, P., Lampa, E., Parrillo, C., michele d'amico, Rossi, F., Mosti, L, Menozzi, G, Fossa, P, Schenone, P, Lampa, E, Parrillo, C, D'Amico, Michele, and Rossi, Francesco

Subjects
Mice, Indazoles, 4-Substituted 1-methyl-1H-indazoles, Anti-Inflammatory Agents, Non-Steroidal, Animals, Humans, Blood Pressure, In Vitro Techniques, Antihypertensive Agents, Platelet Aggregation Inhibitors, Rats
Abstract

The synthesis of [(1-methyl-1H-indazol-4-yl)oxy]acetic acid 4, 1-methyl-1H-indazole-4-acetic acid 9, 2-(1-methyl-1H-indazol-4-yl)propanoic acid 15 and [[(1,5,6,7-tetrahydro-1-methyl-4H-indazol-4-ylidene)amino]oxy]acet ic acid 16, as well as of amides and esters derived from 4 and 9, starting from 1,5,6,7-tetrahydro-1-methyl-4H-indazol-4-one is described. Some of the above compounds showed weak antiinflammatory, analgesic, antipyretic and hypotensive activities in rats and mice, as well as moderate platelet antiaggregating effects in vitro.

Published
1992

22. ChemInform Abstract: Synthesis and Cardiotonic Activity of Novel Pyrimidine Derivatives: Crystallographic and Quantum Chemical Studies.

Author

DORIGO, P., primary, FRACCAROLLO, D., additional, SANTOSTASI, G., additional, MARAGNO, I., additional, FLOREANI, M., additional, BOREA, P. A., additional, MOSTI, L., additional, SANSEBASTIANO, L., additional, FOSSA, P., additional, ORSINI, F., additional, BENETOLLO, F., additional, and BOMBIERI, G., additional

Published
2010
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34. New inotropic agents: Milrinone analogs

Author

Dorigo, P., primary, Fraccarollo, D., additional, Gaion, R.M., additional, Santostasi, G., additional, Borea, P.A., additional, Floreani, M., additional, Mosti, L., additional, and Maragno, I., additional

Published
1997
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39. ChemInform Abstract: Reaction of 2‐Dimethylaminomethylene 1,3‐Diones with Dinucleophiles. Part 11. Synthesis, Antiviral (HSV‐1), and Antimycotic Activities of Ethyl or Methyl 2,4‐Disubstituted 5‐Pyrimidinecarboxylates, 2,4‐ Disubstituted 5‐Pyrimidinecarboxylic Acids, and 2,4‐Disubstituted Pyrimidines.

Author

SANSEBASTIANO, L., primary, MOSTI, L., additional, MENOZZI, G., additional, SCHENONE, P., additional, MURATORE, O., additional, PETTA, A., additional, DEBBIA, E., additional, SCHITO, A. P., additional, and SCHITO, G. C., additional

Published
1994
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48. Synthesis and 3D QSAR of New Pyrazolo[3,4-b]pyridines:  Potent and Selective Inhibitors of A<INF>1</INF> Adenosine Receptors

Author

Manetti, F., Schenone, S., Bondavalli, F., Brullo, C., Bruno, O., Ranise, A., Mosti, L., Menozzi, G., Fossa, P., Trincavelli, M. L., Martini, C., Martinelli, A., Tintori, C., and Botta, M.

Abstract

A number of 4-aminopyrazolo[3,4-b]pyridines 5-carboxylic acid esters (2−8) were synthesized and evaluated for their binding affinity at the A1, A2A, and A3 adenosine receptors (AR), in bovine cortical membranes, as well as for their affinity toward human A1AR (hA1AR). Some of the new compounds were characterized by a high affinity and selectivity toward the A1 receptor subtype, showing a significant improvement in comparison with other pyrazolo-pyridines previously reported in the literature. In particular the methyl ester 2h as well as the isopropyl ester 5h, both of them bearing a p-methoxyphenylethylamino side chain at the position 4, presented Ki values of 6 and 7 nM, respectively. To rationalize the relationships between structure and affinity of the novel compounds, a 3D QSAR model was also generated starting from compounds belonging to different classes of known A1AR antagonists.

Published
2005

49. Structure-Based Design, Parallel Synthesis, Structure−Activity Relationship, and Molecular Modeling Studies of Thiocarbamates, New Potent Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitor Isosteres of Phenethylthiazolylthiourea Derivatives

Author

Ranise, A., Spallarossa, A., Cesarini, S., Bondavalli, F., Schenone, S., Bruno, O., Menozzi, G., Fossa, P., Mosti, L., Colla, M. La, Sanna, G., Murreddu, M., Collu, G., Busonera, B., Marongiu, M. E., Pani, A., Colla, P. La, and Loddo, R.

Abstract

In this paper we describe our structure-based ligand design, synthetic strategy, and structure−activity relationship (SAR) studies that led to the identification of thiocarbamates (TCs), a novel class of non-nucleoside reverse transcriptase inhibitors (NNRTIs), isosteres of phenethylthiazolylthiourea (PETT) derivatives. Assuming as a lead compound O-[2-(phthalimido)ethyl]phenylthiocarbamate 12, one of the precursors of the previously described acylthiocarbamates (Ranise, A.; et al. J. Med. Chem. 2003, 46, 768−781), two targeted solution-phase TC libraries were prepared by parallel synthesis. The lead optimization strategy led to para-substituted TCs 31, 33, 34, 39, 40, 41, 44, 45, and 50, which were active against wild-type HIV-1 in MT-4-based assays at nanomolar concentrations (EC50 range:  0.04−0.01 μM). The most potent congener 50 (EC50 = 0.01 μM) bears a methyl group at position 4 of the phthalimide moiety and a nitro group at the para position of the N-phenyl ring. Most of the TCs showed good selectivity indices, since no cytotoxic effect was detected at concentrations as high as 100 μM. TCs 31, 37, 39, 40, and 44 significantly reduced the multiplication of the Y181C mutant, but they were inactive against K103R and K103N + Y181C mutants. Nevertheless, the fold increase in resistance of 41 was not greater than that of efavirenz against the K103R mutant in enzyme assays. The docking model predictions were consistent with in vitro biological assays of the anti-HIV-1 activity of the TCs and related compounds synthesized.

Published
2005

50. Pyrazolo[3,4-d]pyrimidines Endowed with Antiproliferative Activity on Ductal Infiltrating Carcinoma Cells

Author

Carraro, F., Pucci, A., Naldini, A., Schenone, S., Bruno, O., Ranise, A., Bondavalli, F., Brullo, C., Fossa, P., Menozzi, G., Mosti, L., Manetti, F., and Botta, M.

Abstract

Novel 1,4,6-trisubstituted pyrazolo[3,4-d]pyrimidines are reported with preliminary in vitro activity data indicating that several of them are potent inhibitors (better than the reference compound) of Src phosphorylation of the breast cancer cells 8701-BC, known to overexpress Src. The ability of such compounds to significantly reduce 8701-BC cell proliferation suggests that this scaffold could be a promising lead for the development of antitumoral agents able to block Src phosphorylation of breast cancer cells.

Published
2004

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