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

被引：14

作者：

Wujec, Monika ^{[1
]}

Kedzierska, Ewa ^{[2
]}

Kusmierz, Edyta ^{[1
]}

Plech, Tomasz ^{[1
]}

Wrobel, Andrzej ^{[3
]}

Paneth, Agata ^{[1
,4
]}

Orzelska, Jolanta ^{[2
]}

Fidecka, Sylwia ^{[2
]}

Paneth, Piotr ^{[4
]}

机构：

[1] Med Univ Lublin, Dept Organ Chem, PL-20093 Lublin, Poland

[2] Med Univ Lublin, Dept Pharmacol & Pharmacodynam, PL-20093 Lublin, Poland

[3] Med Univ Lublin, Hist Med Sci Dept, PL-20124 Lublin, Poland

[4] Tech Univ Lodz, Inst Appl Radiat Chem, PL-90924 Lodz, Poland

来源：

MOLECULES | 2014年 / 19卷 / 04期

关键词：

(thio)semicarbazides; conformational analysis; electrostatic properties; CNS activity; analgesic activity; serotonergic activity; ANTITUBERCULOSIS ACTIVITY; ANTIBACTERIAL ACTIVITY; BODY-TEMPERATURE; DERIVATIVES; ANTICONVULSANT; ANTAGONISTS; DRUGS; ACID; MICE;

D O I：

10.3390/molecules19044745

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

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.

引用

页码：4745 / 4759

页数：15

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