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Nilo Zanatta - One of the best experts on this subject based on the ideXlab platform.
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efficient synthesis and dehydration reaction of Trichloromethyl.ted 2 3 phenyl 5 hydroxy 4 5 dihydro 1h pyrazol 1 yl 4 aryl 5 alkylthiazoles
Heteroatom Chemistry, 2003Co-Authors: Helio G. Bonacorso, Nilo Zanatta, Mauro Neves Muniz, Arci Dirceu Wastowski, Marcos A. P. MartinsAbstract:A convenient method for the synthesis of a novel series of 11, specifically substituted, noncondensed 5,5-bicycles 2-[3-phenyl-5-hydroxy-5-Trichloromethyl.4,5-dihydro-1H-pyrazol-1-yl]-4-aryl-5-alkylthiazoles (3a–k; 65–94% yield) from the reactions of 3-phenyl-5-hydroxy-5-Trichloromethyl.4,5-dihydro-1H-1-pyrazolethiocarboxyamide (1) with substituted 2-bromo-4′-acetophenones (2a–f) and 2-bromo-4′-propiophenones (2g–k) is reported. Dehydration of compounds 3a–k with a mixture of concentrated sulfuric acid/chloroform furnished the corresponding 2-[3-phenyl-5-Trichloromethyl.1H-pyrazol-1-yl]-4-aryl-5-alkylthiazoles (4a–k) in good yields (61–93%). © 2003 Wiley Periodicals, Inc. Heteroatom Chem 14:132–137, 2003; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.10113
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hypothermic and antipyretic effects of 3 methyl and 3 phenyl 5 hydroxy 5 Trichloromethyl.4 5 dihydro 1h pyrazole 1 carboxyamides in mice
European Journal of Pharmacology, 2002Co-Authors: Fabiane R Souza, Helio G. Bonacorso, Marcos A. P. Martins, Nilo Zanatta, Vanessa T Souza, Viviane Ratzlaff, Lysandro P Borges, Marli R Oliveira, Carlos Fernando MelloAbstract:The effect of novel pyrazolines, 3-methyl-5-hydroxy-5-Trichloromethyl.4,5-dihydro-1H-pyrazole-1-carboxyamide (MPCA) and 3-phenyl-5-hydroxy-5-Trichloromethyl.4,5-dihydro-1H-pyrazole-1-carboxyamide (PPCA) on body temperature and endotoxin-induced fever was investigated in mice. The subcutaneous (s.c.) administration of 1.5 mmol/kg dipyrone, MPCA or PPCA and the intracerebroventricular (i.c.v.) administration of 225 nmol dipyrone reduced basal rectal temperature. Intracerebroventricular administration of 225 nmol MPCA or PPCA did not alter basal rectal temperature. The administration of 0.15 mmol/kg (s.c.) or 25 nmol (5 μl) dipyrone (i.c.v.), MPCA or PPCA had no effect on basal rectal temperature, but reversed lipopolysaccharide-induced fever. These results suggest that MPCA and PPCA cause antipyresis, which is similar to that caused by dipyrone, and may be useful antipyretic agents.
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haloacetylated enol ethers xvii 1 a convenient synthesis of 5 Trichloromethyl.1 2 dimethyl 1h pyrazolium chlorides
Synthetic Communications, 2002Co-Authors: Marcos A. P. Martins, Giovani P Bastos, Adilson P Sinhorin, Helio G. Bonacorso, Claudio M P Pereira, Nilo E K Zimmermann, Adriano Rosa, Nilo ZanattaAbstract:ABSTRACT The one-pot synthesis of nine 5-Trichloromethyl.1,2-dimethyl-1H-pyrazolium chlorides 2 from the cyclocondensation of 4-alkoxy-1,1,1-trichloro-3-alken-2-ones [CCl3C(O)C(R2)= C(R1)OR, where R1 = H, Me, Et, n-Pr, (CH2)5CO2Et, CH2Br, Ph, 4-Br-C6H4; R2 = H, Me; and R = Me, Et] with 1,2-dimethylhydrazine is reported. For Part 16, see Ref. [12].
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a convenient one pot synthesis of 5 carboxyisoxazoles Trichloromethyl.group as a carboxyl group precursor
Tetrahedron Letters, 2000Co-Authors: Marcos A. P. Martins, Giovani P Bastos, Adilson P Sinhorin, Alex F C Flores, Helio G. Bonacorso, Nilo ZanattaAbstract:Abstract The one-pot synthesis of ten 5-carboxyisoxazoles from the cyclocondensation of β-alkoxyvinyl Trichloromethyl.ketones [CCl 3 C(O)C(R 2 )C(R 1 )OR, where R 1 , R 2 =H, Me and R=Me, Et] and 2-trichloroacetyl cyclohexanone with hydroxylamine is reported. This work shows that the Trichloromethyl.group attached to β-alkoxyvinyl Trichloromethyl.ketones (a heterocyclic CCC building block) is an excellent carboxyl group precursor.
Marcos A. P. Martins - One of the best experts on this subject based on the ideXlab platform.
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efficient synthesis and dehydration reaction of Trichloromethyl.ted 2 3 phenyl 5 hydroxy 4 5 dihydro 1h pyrazol 1 yl 4 aryl 5 alkylthiazoles
Heteroatom Chemistry, 2003Co-Authors: Helio G. Bonacorso, Nilo Zanatta, Mauro Neves Muniz, Arci Dirceu Wastowski, Marcos A. P. MartinsAbstract:A convenient method for the synthesis of a novel series of 11, specifically substituted, noncondensed 5,5-bicycles 2-[3-phenyl-5-hydroxy-5-Trichloromethyl.4,5-dihydro-1H-pyrazol-1-yl]-4-aryl-5-alkylthiazoles (3a–k; 65–94% yield) from the reactions of 3-phenyl-5-hydroxy-5-Trichloromethyl.4,5-dihydro-1H-1-pyrazolethiocarboxyamide (1) with substituted 2-bromo-4′-acetophenones (2a–f) and 2-bromo-4′-propiophenones (2g–k) is reported. Dehydration of compounds 3a–k with a mixture of concentrated sulfuric acid/chloroform furnished the corresponding 2-[3-phenyl-5-Trichloromethyl.1H-pyrazol-1-yl]-4-aryl-5-alkylthiazoles (4a–k) in good yields (61–93%). © 2003 Wiley Periodicals, Inc. Heteroatom Chem 14:132–137, 2003; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.10113
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hypothermic and antipyretic effects of 3 methyl and 3 phenyl 5 hydroxy 5 Trichloromethyl.4 5 dihydro 1h pyrazole 1 carboxyamides in mice
European Journal of Pharmacology, 2002Co-Authors: Fabiane R Souza, Helio G. Bonacorso, Marcos A. P. Martins, Nilo Zanatta, Vanessa T Souza, Viviane Ratzlaff, Lysandro P Borges, Marli R Oliveira, Carlos Fernando MelloAbstract:The effect of novel pyrazolines, 3-methyl-5-hydroxy-5-Trichloromethyl.4,5-dihydro-1H-pyrazole-1-carboxyamide (MPCA) and 3-phenyl-5-hydroxy-5-Trichloromethyl.4,5-dihydro-1H-pyrazole-1-carboxyamide (PPCA) on body temperature and endotoxin-induced fever was investigated in mice. The subcutaneous (s.c.) administration of 1.5 mmol/kg dipyrone, MPCA or PPCA and the intracerebroventricular (i.c.v.) administration of 225 nmol dipyrone reduced basal rectal temperature. Intracerebroventricular administration of 225 nmol MPCA or PPCA did not alter basal rectal temperature. The administration of 0.15 mmol/kg (s.c.) or 25 nmol (5 μl) dipyrone (i.c.v.), MPCA or PPCA had no effect on basal rectal temperature, but reversed lipopolysaccharide-induced fever. These results suggest that MPCA and PPCA cause antipyresis, which is similar to that caused by dipyrone, and may be useful antipyretic agents.
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haloacetylated enol ethers xvii 1 a convenient synthesis of 5 Trichloromethyl.1 2 dimethyl 1h pyrazolium chlorides
Synthetic Communications, 2002Co-Authors: Marcos A. P. Martins, Giovani P Bastos, Adilson P Sinhorin, Helio G. Bonacorso, Claudio M P Pereira, Nilo E K Zimmermann, Adriano Rosa, Nilo ZanattaAbstract:ABSTRACT The one-pot synthesis of nine 5-Trichloromethyl.1,2-dimethyl-1H-pyrazolium chlorides 2 from the cyclocondensation of 4-alkoxy-1,1,1-trichloro-3-alken-2-ones [CCl3C(O)C(R2)= C(R1)OR, where R1 = H, Me, Et, n-Pr, (CH2)5CO2Et, CH2Br, Ph, 4-Br-C6H4; R2 = H, Me; and R = Me, Et] with 1,2-dimethylhydrazine is reported. For Part 16, see Ref. [12].
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a convenient one pot synthesis of 5 carboxyisoxazoles Trichloromethyl.group as a carboxyl group precursor
Tetrahedron Letters, 2000Co-Authors: Marcos A. P. Martins, Giovani P Bastos, Adilson P Sinhorin, Alex F C Flores, Helio G. Bonacorso, Nilo ZanattaAbstract:Abstract The one-pot synthesis of ten 5-carboxyisoxazoles from the cyclocondensation of β-alkoxyvinyl Trichloromethyl.ketones [CCl 3 C(O)C(R 2 )C(R 1 )OR, where R 1 , R 2 =H, Me and R=Me, Et] and 2-trichloroacetyl cyclohexanone with hydroxylamine is reported. This work shows that the Trichloromethyl.group attached to β-alkoxyvinyl Trichloromethyl.ketones (a heterocyclic CCC building block) is an excellent carboxyl group precursor.
Helio G. Bonacorso - One of the best experts on this subject based on the ideXlab platform.
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efficient synthesis and dehydration reaction of Trichloromethyl.ted 2 3 phenyl 5 hydroxy 4 5 dihydro 1h pyrazol 1 yl 4 aryl 5 alkylthiazoles
Heteroatom Chemistry, 2003Co-Authors: Helio G. Bonacorso, Nilo Zanatta, Mauro Neves Muniz, Arci Dirceu Wastowski, Marcos A. P. MartinsAbstract:A convenient method for the synthesis of a novel series of 11, specifically substituted, noncondensed 5,5-bicycles 2-[3-phenyl-5-hydroxy-5-Trichloromethyl.4,5-dihydro-1H-pyrazol-1-yl]-4-aryl-5-alkylthiazoles (3a–k; 65–94% yield) from the reactions of 3-phenyl-5-hydroxy-5-Trichloromethyl.4,5-dihydro-1H-1-pyrazolethiocarboxyamide (1) with substituted 2-bromo-4′-acetophenones (2a–f) and 2-bromo-4′-propiophenones (2g–k) is reported. Dehydration of compounds 3a–k with a mixture of concentrated sulfuric acid/chloroform furnished the corresponding 2-[3-phenyl-5-Trichloromethyl.1H-pyrazol-1-yl]-4-aryl-5-alkylthiazoles (4a–k) in good yields (61–93%). © 2003 Wiley Periodicals, Inc. Heteroatom Chem 14:132–137, 2003; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.10113
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hypothermic and antipyretic effects of 3 methyl and 3 phenyl 5 hydroxy 5 Trichloromethyl.4 5 dihydro 1h pyrazole 1 carboxyamides in mice
European Journal of Pharmacology, 2002Co-Authors: Fabiane R Souza, Helio G. Bonacorso, Marcos A. P. Martins, Nilo Zanatta, Vanessa T Souza, Viviane Ratzlaff, Lysandro P Borges, Marli R Oliveira, Carlos Fernando MelloAbstract:The effect of novel pyrazolines, 3-methyl-5-hydroxy-5-Trichloromethyl.4,5-dihydro-1H-pyrazole-1-carboxyamide (MPCA) and 3-phenyl-5-hydroxy-5-Trichloromethyl.4,5-dihydro-1H-pyrazole-1-carboxyamide (PPCA) on body temperature and endotoxin-induced fever was investigated in mice. The subcutaneous (s.c.) administration of 1.5 mmol/kg dipyrone, MPCA or PPCA and the intracerebroventricular (i.c.v.) administration of 225 nmol dipyrone reduced basal rectal temperature. Intracerebroventricular administration of 225 nmol MPCA or PPCA did not alter basal rectal temperature. The administration of 0.15 mmol/kg (s.c.) or 25 nmol (5 μl) dipyrone (i.c.v.), MPCA or PPCA had no effect on basal rectal temperature, but reversed lipopolysaccharide-induced fever. These results suggest that MPCA and PPCA cause antipyresis, which is similar to that caused by dipyrone, and may be useful antipyretic agents.
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haloacetylated enol ethers xvii 1 a convenient synthesis of 5 Trichloromethyl.1 2 dimethyl 1h pyrazolium chlorides
Synthetic Communications, 2002Co-Authors: Marcos A. P. Martins, Giovani P Bastos, Adilson P Sinhorin, Helio G. Bonacorso, Claudio M P Pereira, Nilo E K Zimmermann, Adriano Rosa, Nilo ZanattaAbstract:ABSTRACT The one-pot synthesis of nine 5-Trichloromethyl.1,2-dimethyl-1H-pyrazolium chlorides 2 from the cyclocondensation of 4-alkoxy-1,1,1-trichloro-3-alken-2-ones [CCl3C(O)C(R2)= C(R1)OR, where R1 = H, Me, Et, n-Pr, (CH2)5CO2Et, CH2Br, Ph, 4-Br-C6H4; R2 = H, Me; and R = Me, Et] with 1,2-dimethylhydrazine is reported. For Part 16, see Ref. [12].
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a convenient one pot synthesis of 5 carboxyisoxazoles Trichloromethyl.group as a carboxyl group precursor
Tetrahedron Letters, 2000Co-Authors: Marcos A. P. Martins, Giovani P Bastos, Adilson P Sinhorin, Alex F C Flores, Helio G. Bonacorso, Nilo ZanattaAbstract:Abstract The one-pot synthesis of ten 5-carboxyisoxazoles from the cyclocondensation of β-alkoxyvinyl Trichloromethyl.ketones [CCl 3 C(O)C(R 2 )C(R 1 )OR, where R 1 , R 2 =H, Me and R=Me, Et] and 2-trichloroacetyl cyclohexanone with hydroxylamine is reported. This work shows that the Trichloromethyl.group attached to β-alkoxyvinyl Trichloromethyl.ketones (a heterocyclic CCC building block) is an excellent carboxyl group precursor.
Anna V. Dolzhenko - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and biological activity of fluorinated 7-benzylamino-2-phenyl-1,2,4-triazolo[1,5-a][1,3,5]triazin-5-amines
Journal of Fluorine Chemistry, 2015Co-Authors: Gigi N.c. Chiu, Bee Jen Tan, Wai Keung Chui, Anna V. DolzhenkoAbstract:Abstract New fluorinated 7-benzylamino-2-phenyl-1,2,4-triazolo[1,5- a ][1,3,5]triazin-5-amines were designed as potential anticancer agents and a practical method for their preparation was developed. The reaction of benzhydrazide with cyanoguanidine followed by intramolecular cyclocondensation resulted in the formation of triazolylguanidine, which upon condensation with trichloroacetonitrile afforded a key intermediate – 2-phenyl-7-Trichloromethyl.1,2,4-triazolo[1,5- a ][1,3,5]triazin-5-amine. In mild conditions, this intermediate underwent nucleophilic displacement of the Trichloromethyl.group with a series of fluorinated benzylamines providing the target compounds. Antiproliferative activity of the prepared compounds against the lung and breast cancer cells was explored. Together with anticancer effect, some compounds demonstrated anti-angiogenic properties.
Carlos Fernando Mello - One of the best experts on this subject based on the ideXlab platform.
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hypothermic and antipyretic effects of 3 methyl and 3 phenyl 5 hydroxy 5 Trichloromethyl.4 5 dihydro 1h pyrazole 1 carboxyamides in mice
European Journal of Pharmacology, 2002Co-Authors: Fabiane R Souza, Helio G. Bonacorso, Marcos A. P. Martins, Nilo Zanatta, Vanessa T Souza, Viviane Ratzlaff, Lysandro P Borges, Marli R Oliveira, Carlos Fernando MelloAbstract:The effect of novel pyrazolines, 3-methyl-5-hydroxy-5-Trichloromethyl.4,5-dihydro-1H-pyrazole-1-carboxyamide (MPCA) and 3-phenyl-5-hydroxy-5-Trichloromethyl.4,5-dihydro-1H-pyrazole-1-carboxyamide (PPCA) on body temperature and endotoxin-induced fever was investigated in mice. The subcutaneous (s.c.) administration of 1.5 mmol/kg dipyrone, MPCA or PPCA and the intracerebroventricular (i.c.v.) administration of 225 nmol dipyrone reduced basal rectal temperature. Intracerebroventricular administration of 225 nmol MPCA or PPCA did not alter basal rectal temperature. The administration of 0.15 mmol/kg (s.c.) or 25 nmol (5 μl) dipyrone (i.c.v.), MPCA or PPCA had no effect on basal rectal temperature, but reversed lipopolysaccharide-induced fever. These results suggest that MPCA and PPCA cause antipyresis, which is similar to that caused by dipyrone, and may be useful antipyretic agents.
