Synthesis of Novel 6,7,8,9-Tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted Hydrazino Thiazolo (2,3-b) Quinazoline as Potent Antinociceptive and Anti-inflammatory Agents

被引：5

作者：

Selvam, T. Panneer ^{[1
]}

Kumar, P. Vijayaraj ^{[2
]}

机构：

[1] DCRM Pharm Coll, Dept Pharmaceut Chem, Inkollu 523167, Andhra Pradesh, India

[2] Isl Coll Technol, Dept Pharm, Balik Pulau 11010, Pulau Pinang, Malaysia

来源：

BULLETIN OF THE KOREAN CHEMICAL SOCIETY | 2010年 / 31卷 / 11期

关键词：

Thiazolo quinazoline; Benzylidine thiazolo quinazoline; Antinociceptive activity; Anti-inflammatory; PHARMACOLOGICAL EVALUATION; ANTIBACTERIAL ACTIVITIES; 2,3-DISUBSTITUTED QUINAZOLIN-4(3H)-ONES; AMINO-3H-QUINAZOLIN-4-ONES; QUINAZOLIN-4-(3H)-ONES; BENZOTHIAZOLES; ACID;

D O I：

10.5012/bkcs.2010.31.11.3265

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted hydrazino thiazolo (2,3-b) quinazolines have been synthesized to meet the structural requirements essential for anti-inflammatory and antinociceptive properties The synthesized series of heterocycles, 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted hydrazino thiazolo (2,3-b) quinazoline by the reaction of 6,7,8,9-tetrahydro-5H-5-hydroxy phenyl thiazolo (2,3-b) quinazolin-3(2H)-one with appropriate hydrazine hydrate and ketones/aldehydes in the presence of anhydrous sodium acetate and glacial acetic acid as presented in Scheme 1 Their antinociceptive activity were evaluated by tail-flick technique, anti-inflammatory was evaluated by carrageenan-induced paw edema test and their ulcerogenicity index determined by reported protocol The compounds exhibited the lowest ulcer index (0 51 +/- 1 63, 0 48 +/- 1 28 and 0 50 +/- 1 53, respectively The 6,7,8,9-tetrahydro-5H-5-hydroxy phenylhydroxy-2-benzylidine-3-(N'-3-pentylidenehydrazino) thiazolo (2,3-b) quinazoline and 6,7,8,9-tetrahydro-5H-5-hydroxy phenyl-2-benzylidine-3-(N'-2-pentylidene-hydrazino) thiazolo (2,3-b) quinazoline exhibited the most potent antinociceptive and anti-inflammatory activities

引用

页码：3265 / 3271

页数：7

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