Volume : 10, Issue : 04, April – 2023
Title:
35.SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF CARBONYL DERIVATIVES OF ADENINE
Authors :
Tyagi Alka *
Abstract :
Objective: In this study, a variety of adenine semicarbazide derivatives were created using adenine as a starting material followed by synthesis of their semicarbazone derivatives.
Methods: The antibacterial activity was assessed using a cup-plate method. Analgesic, anticonvulsant activity, and neurotoxicity of the compounds were assessed using a model of chemically induced convulsions; acetic acid induced writhing response model and the rotarod test on male albino mice. Results: The compounds AA2, AA3, AA4, AA5 and AA10 were found to be good peripheral analgesics showing % analgesic activity 67, 55.5, 54.1, 47.5 and 88.4% respectively & compound AA10 was the most active among all the derivatives tested for the central analgesic activity. AA3, AA7 and AA10 were found to be exhibiting good antibacterial activity. The findings showed that the compounds 2-(2-oxoindolin-3-ylidene)-N-(9H-purin-6-yl) hydrazinecarboxamide (AA3) and 2-((E)-3-phenylallylidene)-N-(9H-purin-6-yl) hydrazinecarboxamide (AA10) were the most active, powerful, and least poisonous ones.
Conclusion: The present work involves pharmacological evaluation of adenine derivatives. The outcomes obtained from the work are significant for further research concentrating on examining prospective options for treatments for epilepsy.
Keywords: Epilepsy, Anticonvulsant, Analgesic, Adenine, antiepileptic.
Cite This Article:
Please cite this article in press Tyagi Alka et al, Synthesis And Pharmacological Evaluation Of Carbonyl Derivatives Of Adenine., Indo Am. J. P. Sci, 2023; 10 (04).
Number of Downloads : 10
References:
1. Das M, Sehgal VK, Singh H. Case Report ADVERSE DRUG REACTIONS OF ANTI-EPILEPTIC DRUGS IN PEDIATRIC AGE GROUP IN A TERTIARY CARE TEACHING HOSPITAL ; A CROSS-SECTIONAL STUDY. 2022;15(3):2–5.
2. Allers K, Essue BM, Hackett ML, Muhunthan J, Anderson CS, Pickles K, et al. The economic impact of epilepsy: A systematic review. BMC Neurol [Internet]. 2015;15(1). Available from: http://dx.doi.org/10.1186/s12883-015-0494-y
3. Sander JWAS, Shorvon SD. Incidence and prevalence studies in epilepsy and their methodological problems: A review. J Neurol Neurosurg Psychiatry. 1987;50(7):829–39.
4. Kotsopoulos IAW, Van Merode T, Kessels FGH, De Krom MCTFM, Knottnerus JA. Systematic review and meta-analysis of incidence studies of epilepsy and unprovoked seizures. Epilepsia. 2002;43(11):1402–9.
5. Beghi E. The Epidemiology of Epilepsy. Neuroepidemiology. 2020;54(2):185–91.
6. Ngugi AK, Bottomley C, Kleinschmidt I, Sander JW, Newton CR. Estimation of the burden of active and life-time epilepsy: A meta-analytic approach. Epilepsia. 2010;51(5):883–90.
7. Singh A, Trevick S. The Epidemiology of Global Epilepsy. Neurol Clin. 2016;34(4):837–47.
8. Selvam TP, Karthick V, Kumar PV, Ali MA. Antiepileptic Activity of Novel 2- ( substituted benzylidene ) -7- ( 4- vatives. 2013;3:204–11.
9. Guan L, Sui X, Chang Y, Yan Z, Tong G, Qu Y. Design , Synthesis and Anticonvulsant Activity Evaluation of 7-Substituted –[ 1 , 2 , 4 ] -Triazolo [ 4 , 3- f ] Pyrimidine Derivatives. 2012;3:1076–83.
10. Prakash CR, Raja S. Design, synthesis and antiepileptic properties of novel 1-(substituted benzylidene)-3-(1-(morpholino/piperidino methyl)-2, 3-dioxoindolin-5-yl) urea derivatives. Eur J Med Chem. 2011;46(12):6057–65.
11. Said SA, Amr AEGE, Sabry NM, Abdalla MM. Analgesic, anticonvulsant and anti-inflammatory activities of some synthesized benzodiazipine, triazolopyrimidine and bis-imide derivatives. Eur J Med Chem. 2009;44(12):4787–92.
12. Shalaby AFA, Abdulla MM, Amr AEGE, Hussain AA. Synthesis, reactions, and anti-arrhythmic activity of substituted heterocyclic systems using 5-chloroanisic acid as starting material. Monatshefte für Chemie-Chemical Mon. 2007;138(10):1019–27.
13. Abd El-Latif NA, Amr AE-GE, Ibrahiem AA. Synthesis, reactions, and pharmacological screening of heterocyclic derivatives using nicotinic acid as a natural synthon. Monatshefte für Chemie-Chemical Mon. 2007;6(138):559–67.
14. Hammam AEFG, Fahmy AFM, Amr AGE, Mohamed AM. Synthesis of novel tricyclic heterocyclic compounds as potential anticancer agents using chromanone and thiochromanone as synthons. Indian J Chem – Sect B Org Med Chem. 2003;42(8):1985–93.
15. Amr AE, Abdulla MM. Synthesis and pharmacological screening of some new pyrimidine and cyclohexenone fused steroidal derivatives. Indian J Heterocycl Chem. 2002;12(2):129–34.
16. Amr AGE, Mohamed AM, Mohamed SF, Abdel-Hafez NA, Hammam AEFG. Anticancer activities of some newly synthesized pyridine, pyrane, and pyrimidine derivatives. Bioorganic Med Chem. 2006;14(16):5481–8.
17. Amr A-GE, Hegab MI, Ibrahiem AA, Abdulla MM. Synthesis and reactions of some fused oxazinone, pyrimidinone, thiopyrimidinone, and triazinone derivatives with a thiophene ring as analgesic, anticonvulsant, and antiparkinsonian agents. Monatshefte für Chemie/Chemical Mon. 2003;134(10):1395–409.
18. Amr AE-GE, Sabry NM, Abdulla MM. Synthesis, reactions, and anti-inflammatory activity of heterocyclic systems fused to a thiophene moiety using citrazinic acid as synthon. Monatshefte für Chemie-Chemical Mon. 2007;138(7):699–707.
19. Spear BB. Pharmacogenetics and antiepileptic drugs. Epilepsia. 2001;42:31–4.
20. Gupta A. Synthesis of novel methoxy substituted benzothiazole derivatives and antibacterial activity against escherichia coli. Asian J Pharm Clin Res. 2018;11(9):416–9.
21. Sridhar SK, Pandeya SN, Stables JP, Ramesh A. Anticonvulsant activity of hydrazones, Schiff and Mannich bases of isatin derivatives. Eur J Pharm Sci. 2002;16(3):129–32.
22. Verma M, Pandeya SN, Singh KN, Stables JP. Anticonvulsant activity of Schiff bases of isatin derivatives. Acta Pharm. 2004;54(1):49–56.
23. Jerome M. Glassman. Agents with analgesic activity and deprndence liability. In: edited by Robert Turner PH, editor. Screening Methods in Pharmacology: Volume II, Volume 2. revised. Elsevier, 2016; p. 227–45.
24. Vogel HG. Drug discovery and evaluation:pharmacological assays,Berlin. New York: Berlin; 2002. 696–713 p.
25. Pandeya SN, Sriram D, Nath G, De Clercq E. Synthesis and antimicrobial activity of Schiff and Mannich bases of isatin and its derivatives with pyrimidine. Farm [Internet]. 1999;54(9):624–8. Available from: https://www.sciencedirect.com/science/article/pii/S0014827X99000750
26. Pandeya SN, Sriram D, Nath G, De Clercq E. Synthesis and antimicrobial activity of Schiff and Mannich bases of isatin and its derivatives with pyrimidine. Farmaco. 1999;54(9):624–8.
27. Pandeya SN, Sriram D, Nath G, DeClercq E. Synthesis, antibacterial, antifungal and anti-HIV activities of Schiff and Mannich bases derived from isatin derivatives and N-[4-(4′-chlorophenyl) thiazol-2-yl] thiosemicarbazide. Eur J Pharm Sci. 1999;9(1):25–31.
28. Pandeya SN, Sriram D. Synthesis and screening for antidacterial activity of schiff’s and mannich bases of isatin and its derivatives. ACTA Pharm Sci. 1998;40(1).