Screening Of Analgesic Activity Research Articles

SYNTHESIS AND ANALGESIC ACTIVITY OF METHYL-1-ANTIPYRYL-4-AROYL-2,3-DIOXO-2,3,5,10-TETRAHYDROBENZO[B]PYRROLO[2,3-E][1,4]DIAZEPINE-10A(1H) –CARBOXYLATES

In order to obtain new biologically active compounds, methyl-1-antipyryl-4-aroyl-2,3-dioxo-2,3,5,10-tetrahydrobenzo[b]pyrrolo[2,3-e][1,4]diazepine was synthesized-10a(1H)-carboxylates by reacting 1-antipyryl-4-aroyl-5-methoxycarbonyl-1H-pyrrole-2,3-diones with o-phenylenediamine. The structures of the obtained compounds were confirmed by 1H NMR, IR spectroscopy, X-ray diffraction and elemental analysis. The presence of several electrophilic centers in the structure of antipyryl-substituted 1H-pyrrole-2,3-diones gives them a high reactivity with respect to binucleophilic reagents. Apparently, the described interaction is carried out by the initial nucleophilic attack of one aminogroup of o-phenylenediamine on the C5 carbon atom of the pyrrole-2,3-dione ring, followed by the attack of another aminogroup on the carbonyl carbon atom of the aroyl fragment, closing the diazepine ring. The described reaction is a convenient preparative method for the synthesis of previously undescribed methyl-1-antipyryl-4-aroyl-2,3-dioxo-2,3,5,10-tetrahydrobenzo[b]pyrrolo[2,3-e][1,4]diazepine-10a(1H)-carboxylates, which are of interest as pharmacological substances. The described interaction proceeds quickly and with high yields. The obtained compounds were screened for analgesic activity, as a result of which a more pronounced effect was found in some products compared to the reference drug (diclofenac sodium). A preliminary assessment of acute toxicity was carried out, according to which the derivatives of 2,3,5,10-tetrahydrobenzo[b]pyrrolo[2,3-e][1,4]diazepine proved to be safe for further studies. The survival rate of animals in all groups is 100% after 24 h and 100% after 14 days. Screening of analgesic activity was performed by the hot plate method. Registration of time was carried out from the moment of placement on a hot surface until the appearance of a behavioral response to nociceptive stimulation 60 and 120 min after the administration of substances. For citation: Lyadov V.A., Makrushin D.E., Denislamova E.S., Maslivets A.N., Triandafilova G.A., Solodnikov S.I. Synthesis and analgesic activity of methyl-1-antipyryl-4-aroyl-2,3-dioxo-2,3,5,10-tetrahydrobenzo[b]pyrrolo[2,3-e][1,4]diazepine-10a(1H) –carboxylates. ChemChemTech [Izv. Vyssh. Uchebn. Zaved. Khim. Khim. Tekhnol.]. 2024. V. 67. N 5. P. 17-23. DOI: 10.6060/ivkkt.20246705.6939.

Antioxidant, Analgesic, Antimicrobial and Molecular Docking Studies of the Leaves of Oroxylum indicum (L.) Kurz.

This study presents the findings of in vivo, in vitro and in silico investigations of the Oroxylum indicum (L.) Kurz leaf extracts. Various fractions namely chloroform (CF), ethyl acetate (EAF), n-hexane (HF) and aqueous fractions (AF) obtained from the crude extract were subjected to biological investigations. In DPPH based free radical scavenging assay, CF and MF fractions showed potent antioxidant activity with IC50 9.70 g/ml and 10.46 g/ml as compared to IC50 8.56g/ml for the standard ascorbic acid. The CF and HF fractions of O. indicum (L.) Kurz leaves exhibited mild antimicrobial activity. In analgesic activity screening by acetic acid induced writhing method, EAF showed significant writhing inhibition of 68% and 72%, at doses 150 mg/kg and 300 mg/kg, respectively. In tail immersion method, EAF also showed potent analgesic activity with reaction time of 1.816 ± 0.047 and 2.15 ± 0.041 min, after 30 minutes following oral doses of 150 mg/kg and 300 mg/kg, respectively. Molecular docking of previously isolated compounds from O. indicum (L.) Kurz leaf extracts were docked against cyclooxygenase-1 (COX-1) and cyclooxygenase -2 (COX-2) and revealed that the flavonoids baicalein and chrysin may be responsible for the analgesic activity. Lipinski’s rule of five was also calculated for the compounds to assess drug likeliness. Dhaka Univ. J. Pharm. Sci. 21(1): 85-94, 2022 (June)

Synthesis and anаlgеsic activity 5-methyl-3-aryl[1,2,4]triazolo[4,3-a]pyrimidin-7-oles derivatives

Pain is a signal of inflammation and disruption of the body. It is the most important protective and adaptive mechanism that ensuring the safety of the individual. A strong and prolonged effect of "pain" irritant arising in injuries or after surgical manipulation transforms the protective reaction of the body to harmful factor that is the cause of secondary violations physiological processes.
 The aim of this work was the synthesis of substances in a series of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidine-7-ol and study the analgesic effect of the synthesized compounds.
 The objects of our research were selected derivatives of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidine-7-ol, which were synthesized by condensation and subsequent cyclization of 6-methyl-2-metylsulfanilpirymidyn-4-ol (1) with the corresponding substituted benzoic acid hydrazide The primary evaluation of analgesic activity conducted on thermal stimulation models («hot plate»).
 A number of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol derivatives were synthesized, and their structure and purity were confirmed by 1H NMR spectroscopy. The analgesic activity of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol was investigated in order to reveal the structure-activity relationship.
 The screening for analgesic activity for 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol derivatives in in vivo experiments on hot plate models showed that the highest activity Was noted for the compound containing the methyl group in the fourth position of the aryl substituent, which is 184.28% of the change in the latent period of the reaction, which exceeds the action of the reference preparation of ketorolac by 71.57%. The introduction of halogens into the aryl moiety leads to a decrease in the analgesic activity of the compounds.
 A series of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidine-7-ol derivatives were synthesized by condensation and subsequent cyclization of 6-methyl-2-metylsulfanylpirymydyn-4-ol with relevant substituted hydrazide of benzoic acid. The structure and purity of obtained compounds were confirmed by 1H NMR spectroscopy. The analgesic activity of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol was investigated in order to reveal the structure-activity relationship.
 The screening of analgesic activity of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pirymidyn-7-ol derivatives in vivo models for «hot plate» shows that the highest activity was noted for compound containing methyl group in the fourth position of the aryl substituent, which is 184.28% change latent period reaction, that exceeds effect reference drug ketorolac at 71.57%. The introduction of halogens in the aryl fragment leads to a decrease analgesic activity of compounds.

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Analgesic Activity of Caesalpinia sappan. Heartwood

The ethanol extract of heartwood of Caesalpinia sappan. Linn (Caesalpiniceae) and three crude fractions [petroleum ether (60–80°C), diethyl ether, and ethyl acetate] were subjected to preliminary qualitative chemical investigation. The ethanol extract and its fractions underwent pharmacological screening for analgesic activity by using acetic acid-induced writhing in albino mice. The ethanol extract and its different fractions of heartwood of Caesalpinia sappan. exhibited significant analgesic activity (p < 0.01). In conclusion, the ethanol extract of heartwood of Caesalpinia sappan. and its three different crude fractions were found to show peripheral analgesic activity.

Synthesis of 4-hydroxypiperidine derivatives and their screening for analgesic activity

Six substituted phenacyl derivatives of 4-hydroxypiperidine were prepared and their structures were confirmed through spectroscopic techniques. These newly synthesized derivatives were also screened for analgesic activity by chemical and thermal methods. Only halogenated phenacyl derivatives demonstrated more or less protection against acetic acid induced writhing in mice where as rest of three derivatives were found inactive when screened by this chemical method. Similarly all the six derivatives were proved inactive by tail flick test.

Analgesic Activity of the Rhizomes of Curcuma zedoaria

Successive extraction of the dried rhizomes of Curcuma zedoaria Rosc. provided hexane, chloroform and methanol extracts. In analgesic activity screening, the chloroform and methanol extracts showed significant activity on Swiss albino mice. Oral administration of the crude extracts at a dose of 400 mg/kg body weight, exhibited 29.5 and 38.0 % inhibition of acetic acid induced writhing in mice, respectively while the hexane extract showed weak analgesic activity in the experiment.&#x0D; &#x0D; Key words: Curcuma zedoaria, Zingiberaceae, Analgesic activity.&#x0D; &#x0D; Dhaka Univ. J. Pharm. Sci. Vol.3(1-2) 2004&#x0D; &#x0D; The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website