Synthesis, spectral characterization, and pharmacological screening of some 4-[{1-(aryl)methylidene}-amino]-3-(4-pyridyl)-5-mercapto-4H-1,2,4-triazole derivatives
Background : Pain is an unpleasant and subjective sensation that results from a harmful sensorial stimulation, which alerts the body about current or potential damage to its tissues and organs. Fever is a complex physiological response triggered by infections or aseptic stimuli. Elevation in body te...
| Main Authors: | , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Wolters Kluwer Medknow Publications
2010-01-01
|
| Series: | Journal of Pharmacy and Bioallied Sciences |
| Subjects: | |
| Online Access: | http://www.jpbsonline.org/article.asp?issn=0975-7406;year=2010;volume=2;issue=2;spage=109;epage=112;aulast=Siddiqui |
| _version_ | 1811283285541650432 |
|---|---|
| author | Anees A Siddiqui Ravinesh Mishra Rajiv Kumar Mohd Rashid Somila Khaidem |
| author_facet | Anees A Siddiqui Ravinesh Mishra Rajiv Kumar Mohd Rashid Somila Khaidem |
| author_sort | Anees A Siddiqui |
| collection | DOAJ |
| description | Background : Pain is an unpleasant and subjective sensation that results from a harmful sensorial stimulation, which alerts the body about current or potential damage to its tissues and organs. Fever is a complex physiological response triggered by infections or aseptic stimuli. Elevation in body temperature occurs when the concentration of prostaglandin E 2 (PGE 2 ) increases within parts of the brain. Triazole derivatives have been found to possess various pharmacological and biological activities, such as, anti-inflammatory, analgesics, antipyretic, and antifungal. Materials and Methods : Various 4-[{1-(aryl)methylidene}-amino]-3-(4-pyridyl)-5-mercapto-4H-1,2,4-triazole derivatives were synthesized by a sequence of reactions starting from isonicotinic acid hydrazide. The synthesized compounds were screened for in-vivo analgesic by the tail-flick method and anti-pyretic activities at a dose of 25 and 100 mg/kg body weight respectively. The antipyretic activity was evaluated using Brewer′s yeast induced pyrexia in rats. Fever was induced by subcutaneously injecting 20 ml/kg of 20% aqueous suspension of Brewer′s yeast in normal saline. Results and Discussion : The analgesic screening results revealed that the compounds 3b, 3c, and 3d exhibited excellent analgesic activity at 60 and 90 minutes compared to the standard drug (Analgin). Results revealed that the compounds 3a, 3e, and 3f significantly decreased the temperature of pyretic (P<0.001) rats at one, three and six hours after compound administration as compared to Aspirin (standard drug). Conclusion : Compounds 3b, 3c, and 3d exhibited significant analgesic activity comparable with the standard drug analgin, using the tail flick model. Compounds 3a, 3e, and 3f showed significant anti-pyretic activities comparable with the standard drug aspirin using the yeast-induced pyrexia model. |
| first_indexed | 2024-04-13T02:08:42Z |
| format | Article |
| id | doaj.art-cf2d67bcf748454bb104b7fe4c8eab05 |
| institution | Directory Open Access Journal |
| issn | 0975-7406 0976-4879 |
| language | English |
| last_indexed | 2024-04-13T02:08:42Z |
| publishDate | 2010-01-01 |
| publisher | Wolters Kluwer Medknow Publications |
| record_format | Article |
| series | Journal of Pharmacy and Bioallied Sciences |
| spelling | doaj.art-cf2d67bcf748454bb104b7fe4c8eab052022-12-22T03:07:23ZengWolters Kluwer Medknow PublicationsJournal of Pharmacy and Bioallied Sciences0975-74060976-48792010-01-012210911210.4103/0975-7406.67014Synthesis, spectral characterization, and pharmacological screening of some 4-[{1-(aryl)methylidene}-amino]-3-(4-pyridyl)-5-mercapto-4H-1,2,4-triazole derivativesAnees A SiddiquiRavinesh MishraRajiv KumarMohd RashidSomila KhaidemBackground : Pain is an unpleasant and subjective sensation that results from a harmful sensorial stimulation, which alerts the body about current or potential damage to its tissues and organs. Fever is a complex physiological response triggered by infections or aseptic stimuli. Elevation in body temperature occurs when the concentration of prostaglandin E 2 (PGE 2 ) increases within parts of the brain. Triazole derivatives have been found to possess various pharmacological and biological activities, such as, anti-inflammatory, analgesics, antipyretic, and antifungal. Materials and Methods : Various 4-[{1-(aryl)methylidene}-amino]-3-(4-pyridyl)-5-mercapto-4H-1,2,4-triazole derivatives were synthesized by a sequence of reactions starting from isonicotinic acid hydrazide. The synthesized compounds were screened for in-vivo analgesic by the tail-flick method and anti-pyretic activities at a dose of 25 and 100 mg/kg body weight respectively. The antipyretic activity was evaluated using Brewer′s yeast induced pyrexia in rats. Fever was induced by subcutaneously injecting 20 ml/kg of 20% aqueous suspension of Brewer′s yeast in normal saline. Results and Discussion : The analgesic screening results revealed that the compounds 3b, 3c, and 3d exhibited excellent analgesic activity at 60 and 90 minutes compared to the standard drug (Analgin). Results revealed that the compounds 3a, 3e, and 3f significantly decreased the temperature of pyretic (P<0.001) rats at one, three and six hours after compound administration as compared to Aspirin (standard drug). Conclusion : Compounds 3b, 3c, and 3d exhibited significant analgesic activity comparable with the standard drug analgin, using the tail flick model. Compounds 3a, 3e, and 3f showed significant anti-pyretic activities comparable with the standard drug aspirin using the yeast-induced pyrexia model.http://www.jpbsonline.org/article.asp?issn=0975-7406;year=2010;volume=2;issue=2;spage=109;epage=112;aulast=SiddiquiIsonicotinic acid hydrazide124-triazoleanalgesicantipyretic activity |
| spellingShingle | Anees A Siddiqui Ravinesh Mishra Rajiv Kumar Mohd Rashid Somila Khaidem Synthesis, spectral characterization, and pharmacological screening of some 4-[{1-(aryl)methylidene}-amino]-3-(4-pyridyl)-5-mercapto-4H-1,2,4-triazole derivatives Journal of Pharmacy and Bioallied Sciences Isonicotinic acid hydrazide 1 2 4-triazole analgesic antipyretic activity |
| title | Synthesis, spectral characterization, and pharmacological screening of some 4-[{1-(aryl)methylidene}-amino]-3-(4-pyridyl)-5-mercapto-4H-1,2,4-triazole derivatives |
| title_full | Synthesis, spectral characterization, and pharmacological screening of some 4-[{1-(aryl)methylidene}-amino]-3-(4-pyridyl)-5-mercapto-4H-1,2,4-triazole derivatives |
| title_fullStr | Synthesis, spectral characterization, and pharmacological screening of some 4-[{1-(aryl)methylidene}-amino]-3-(4-pyridyl)-5-mercapto-4H-1,2,4-triazole derivatives |
| title_full_unstemmed | Synthesis, spectral characterization, and pharmacological screening of some 4-[{1-(aryl)methylidene}-amino]-3-(4-pyridyl)-5-mercapto-4H-1,2,4-triazole derivatives |
| title_short | Synthesis, spectral characterization, and pharmacological screening of some 4-[{1-(aryl)methylidene}-amino]-3-(4-pyridyl)-5-mercapto-4H-1,2,4-triazole derivatives |
| title_sort | synthesis spectral characterization and pharmacological screening of some 4 1 aryl methylidene amino 3 4 pyridyl 5 mercapto 4h 1 2 4 triazole derivatives |
| topic | Isonicotinic acid hydrazide 1 2 4-triazole analgesic antipyretic activity |
| url | http://www.jpbsonline.org/article.asp?issn=0975-7406;year=2010;volume=2;issue=2;spage=109;epage=112;aulast=Siddiqui |
| work_keys_str_mv | AT aneesasiddiqui synthesisspectralcharacterizationandpharmacologicalscreeningofsome41arylmethylideneamino34pyridyl5mercapto4h124triazolederivatives AT ravineshmishra synthesisspectralcharacterizationandpharmacologicalscreeningofsome41arylmethylideneamino34pyridyl5mercapto4h124triazolederivatives AT rajivkumar synthesisspectralcharacterizationandpharmacologicalscreeningofsome41arylmethylideneamino34pyridyl5mercapto4h124triazolederivatives AT mohdrashid synthesisspectralcharacterizationandpharmacologicalscreeningofsome41arylmethylideneamino34pyridyl5mercapto4h124triazolederivatives AT somilakhaidem synthesisspectralcharacterizationandpharmacologicalscreeningofsome41arylmethylideneamino34pyridyl5mercapto4h124triazolederivatives |