Effect of 4-benzylidenamino-5-phenyl-4Н-1,2,4-triazole-3-thiones and salts of 2-(4-amino-5-phenyl-4Н-1,2,4-triazole-3-ylthio)acetic acid on central component of nociceptive system
Aim. To study the effect of 4-benzylideneamino-5-phenyl-4H-1,2,4-triazole-3-thiones and salts of 2-(4-amino-5-phenyl-4H-1,2,4-triazole-3-yltio)acetic acid on central component of nociceptive system on condition of thermal stimulation of limbs of rats, and also to explore patterns related with the ch...
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| Format: | Article |
| Language: | English |
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Zaporizhzhia State Medical and Pharmaceutical University
2016-08-01
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| Series: | Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki |
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| Online Access: | http://pharmed.zsmu.edu.ua/article/view/70699/67979 |
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| _version_ | 1849251396713447424 |
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| author | Ye. S. Pruhlo |
| author_facet | Ye. S. Pruhlo |
| author_sort | Ye. S. Pruhlo |
| collection | DOAJ |
| description | Aim. To study the effect of 4-benzylideneamino-5-phenyl-4H-1,2,4-triazole-3-thiones and salts of 2-(4-amino-5-phenyl-4H-1,2,4-triazole-3-yltio)acetic acid on central component of nociceptive system on condition of thermal stimulation of limbs of rats, and also to explore patterns related with the chemical structure and pharmacological activity of 1,2,4-triazole derivatives.
Materials and methods. The newly synthesized derivatives of 4-benzylideneamino-5-phenyl-4H-1,2,4-triazole-3-thiones and salts of 2-(4-amino-5-phenyl-4H-1,2,4-triazole-3-ylthio)acetic acid (Table. 1) have been used in the studies. General toxic effect and acute toxicity of compounds had been previously studied by express method of V.B. Prozorovskiy to determine the conditions of test-substance dosing [4]. The study has been conducted on a group of non-linear white rats of both sexes weighing 185-229 g.
Results. The compound that is close to the reference medication – analgin, by its activity, has been revealed. This compound exhibits analgesic activity at considerably lower doses than the proposed reference medication.
Conclusions. Some relations between chemical structure and pharmacological activity of the investigated 1,2,4-triazole derivatives have been established. Thus, condensation of 4-amino-5-phenyl-4H-1,2,4-triazole-3-thione with 4- hydroxybenzaldehyde causes almost no effect on analgesic action of starting thione and 4-(4-hydroxybenzylideneamino)-5-phenyl-4Н-1,2,4-triazole-3-thione, whereas the replacement of 4-hydroxybenzylideneamino substituent by 2-hydroxybenzylideneamino substituent reduces the sensitivity of rats to thermal stimulus. The replacement of morpholine cation in the molecule of morpholine salt of 2-(4-amino-5-phenyl-4H-1,2,4-triazole-3-ylthio)acetic acid by piperidinium cation leads to sudden appearance of analgesic activity. |
| format | Article |
| id | doaj-art-a6942c381fad441b9a3afa1cba4a564d |
| institution | Kabale University |
| issn | 2306-8094 2409-2932 |
| language | English |
| publishDate | 2016-08-01 |
| publisher | Zaporizhzhia State Medical and Pharmaceutical University |
| record_format | Article |
| series | Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki |
| spelling | doaj-art-a6942c381fad441b9a3afa1cba4a564d2025-08-20T03:56:58ZengZaporizhzhia State Medical and Pharmaceutical UniversityAktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki2306-80942409-29322016-08-012576110.14739/2409-2932.2016.2.70699Effect of 4-benzylidenamino-5-phenyl-4Н-1,2,4-triazole-3-thiones and salts of 2-(4-amino-5-phenyl-4Н-1,2,4-triazole-3-ylthio)acetic acid on central component of nociceptive systemYe. S. PruhloAim. To study the effect of 4-benzylideneamino-5-phenyl-4H-1,2,4-triazole-3-thiones and salts of 2-(4-amino-5-phenyl-4H-1,2,4-triazole-3-yltio)acetic acid on central component of nociceptive system on condition of thermal stimulation of limbs of rats, and also to explore patterns related with the chemical structure and pharmacological activity of 1,2,4-triazole derivatives. Materials and methods. The newly synthesized derivatives of 4-benzylideneamino-5-phenyl-4H-1,2,4-triazole-3-thiones and salts of 2-(4-amino-5-phenyl-4H-1,2,4-triazole-3-ylthio)acetic acid (Table. 1) have been used in the studies. General toxic effect and acute toxicity of compounds had been previously studied by express method of V.B. Prozorovskiy to determine the conditions of test-substance dosing [4]. The study has been conducted on a group of non-linear white rats of both sexes weighing 185-229 g. Results. The compound that is close to the reference medication – analgin, by its activity, has been revealed. This compound exhibits analgesic activity at considerably lower doses than the proposed reference medication. Conclusions. Some relations between chemical structure and pharmacological activity of the investigated 1,2,4-triazole derivatives have been established. Thus, condensation of 4-amino-5-phenyl-4H-1,2,4-triazole-3-thione with 4- hydroxybenzaldehyde causes almost no effect on analgesic action of starting thione and 4-(4-hydroxybenzylideneamino)-5-phenyl-4Н-1,2,4-triazole-3-thione, whereas the replacement of 4-hydroxybenzylideneamino substituent by 2-hydroxybenzylideneamino substituent reduces the sensitivity of rats to thermal stimulus. The replacement of morpholine cation in the molecule of morpholine salt of 2-(4-amino-5-phenyl-4H-1,2,4-triazole-3-ylthio)acetic acid by piperidinium cation leads to sudden appearance of analgesic activity.http://pharmed.zsmu.edu.ua/article/view/70699/67979PainAnalgesic Agents1 2 4-triazole4-amino-1 2 4-triazole |
| spellingShingle | Ye. S. Pruhlo Effect of 4-benzylidenamino-5-phenyl-4Н-1,2,4-triazole-3-thiones and salts of 2-(4-amino-5-phenyl-4Н-1,2,4-triazole-3-ylthio)acetic acid on central component of nociceptive system Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki Pain Analgesic Agents 1 2 4-triazole 4-amino-1 2 4-triazole |
| title | Effect of 4-benzylidenamino-5-phenyl-4Н-1,2,4-triazole-3-thiones and salts of 2-(4-amino-5-phenyl-4Н-1,2,4-triazole-3-ylthio)acetic acid on central component of nociceptive system |
| title_full | Effect of 4-benzylidenamino-5-phenyl-4Н-1,2,4-triazole-3-thiones and salts of 2-(4-amino-5-phenyl-4Н-1,2,4-triazole-3-ylthio)acetic acid on central component of nociceptive system |
| title_fullStr | Effect of 4-benzylidenamino-5-phenyl-4Н-1,2,4-triazole-3-thiones and salts of 2-(4-amino-5-phenyl-4Н-1,2,4-triazole-3-ylthio)acetic acid on central component of nociceptive system |
| title_full_unstemmed | Effect of 4-benzylidenamino-5-phenyl-4Н-1,2,4-triazole-3-thiones and salts of 2-(4-amino-5-phenyl-4Н-1,2,4-triazole-3-ylthio)acetic acid on central component of nociceptive system |
| title_short | Effect of 4-benzylidenamino-5-phenyl-4Н-1,2,4-triazole-3-thiones and salts of 2-(4-amino-5-phenyl-4Н-1,2,4-triazole-3-ylthio)acetic acid on central component of nociceptive system |
| title_sort | effect of 4 benzylidenamino 5 phenyl 4н 1 2 4 triazole 3 thiones and salts of 2 4 amino 5 phenyl 4н 1 2 4 triazole 3 ylthio acetic acid on central component of nociceptive system |
| topic | Pain Analgesic Agents 1 2 4-triazole 4-amino-1 2 4-triazole |
| url | http://pharmed.zsmu.edu.ua/article/view/70699/67979 |
| work_keys_str_mv | AT yespruhlo effectof4benzylidenamino5phenyl4n124triazole3thionesandsaltsof24amino5phenyl4n124triazole3ylthioaceticacidoncentralcomponentofnociceptivesystem |