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Synthesis and Pharmacological Screening for Muscle Relaxant, Anticonvulsant, and Sedative Activities of Certain Organic Compounds Produced by Michael Addition
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  • Synthesis and Pharmacological Screening for Muscle Relaxant, Anticonvulsant, and Sedative Activities of Certain Organic Compounds Produced by Michael Addition
  • Synthesis and Pharmacological Screening for Muscle Relaxant, Anticonvulsant, and Sedative Activities of Certain Organic Compounds Produced by Michael Addition
저자명
Said. Makarem M.,Ahmed. Amany A. E.,El-Alfy. Abir T.
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2004년|27권 12호|pp.1194-1201 (8 pages)
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대한약학회
파일정보
정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

Michael addition of certain nucleophiles on ${alpha}$ , ${eta}$-unsaturated ketones 1 led to the formation of adducts 2-7 as well as the reaction of arylidene derivatives with secondary amines afforded the amino compounds 9 and 11. Also, dialkylmalonates were treated with ${alpha}$-cyano cinnamide to afford 13. On the other hand, double Michael cycloaddition of ethylcyanoacetate or tetrachlorophthalic anhydride to the suitable divinylketone were synthesized to produce 15-17. Selected compounds (13 and 6) were screened for muscle relaxant, anticonvulsant, and sedative activities using established pharmacological models. Their activities were compared with that of phenobarbital sodium taken as standard. Compound 6 was the most potent muscle relaxant while compounds 13a and 13c offered the highest anticonvulsant activity. Meanwhile compound 13c showed the highest potentiation of phenobarbital induced sleep in mice.