Pharmacological and Structure-Activity Relationship Evaluation of 4-aryl-1-Diphenylacetyl(thio)semicarbazides

Molecules

Monika Wujec¹  Ewa Kᆝzierska³  Edyta Kuśmierz¹  Tomasz Plech¹  Andrzej Wrl²  Agata Paneth¹  Jolanta Orzelska³  Sylwia Fidecka³ 

[1] Department of Organic Chemistry, Medical University, Chodźki 4a, 20-093 Lublin, Poland; E-Mails:;History of Medical Sciences Department, Medical University, Szkolna 18, 20-124 Lublin, Poland; E-Mail:;Department of Pharmacology and Pharmacodynamics, Medical University, Chodźki 4a, 20-093 Lublin, Poland; E-Mails:

关键词: (thio)semicarbazides;    conformational analysis;    electrostatic properties;    CNS activity;    analgesic activity;    serotonergic activity;   

DOI  :  10.3390/molecules19044745

来源: mdpi

【 摘 要 】

This article describes the synthesis of six 4-aryl-(thio)semicarbazides (series a and b) linked with diphenylacetyl moiety along with their pharmacological evaluation on the central nervous system in mice and computational studies, including conformational analysis and electrostatic properties. All thiosemicarbazides (series b) were found to exhibit strong antinociceptive activity in the behavioural model. Among them, compound 1-diphenylacetyl-4-(4-methylphenyl)thiosemicarbazide 1b was found to be the most potent analgesic agent, whose activity is connected with the opioid system. For compounds from series a significant anti-serotonergic effect, especially for compound 1-diphenylacetyl-4-(4-methoxyphenyl)semicarbazide 2b was observed. The computational studies strongly support the obtained results.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.