Synthesis and pharmacological evaluation of novel thienopyrimidine and triazolothienopyrimidine derivatives

被引：0

作者：

Jameel Ahmed S. Mulla

Mohammed Iqbal A. Khazi

Shridhar I. Panchamukhi

Young-Dae Gong

Imtiyaz Ahmed M. Khazi

机构：

[1] Karnatak University,Department of Chemistry

[2] K.L.E. University’s College of Pharmacy,Department of Pharmaceutics

[3] Dongguk University,Center for Innovative Drug Library Research, Science College

来源：

Medicinal Chemistry Research | 2014年 / 23卷

关键词：

Thienopyrimidine; Triazolothienopyrimidine; Gewald reaction; Analgesic; Anti-inflammatory; Antibacterial activity;

D O I：

暂无

中图分类号：

学科分类号：

摘要：

Novel tricyclic thienopyrimidines (2, 3, 5, 8) and triazole-fused tetracyclic thienopyrimidines (6a–c and 9a–c) were synthesized from the precursor 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carbonitrile (1). The structures of newly synthesized compounds were established by spectral and analytical data. The title compounds were screened for analgesic, anti-inflammatory, ulcerogenicity index, and antibacterial activities. Test compounds exhibited significant activity, the compounds (6a–c) and (9a–c) showed more potent analgesic activity, and the compounds (6c) and (9c) showed more potent anti-inflammatory activity than the reference standard Diclofenac Sodium. All the synthesized compounds exhibited remarkable antibacterial activity.

引用

页码：3235 / 3243

页数：8

共 122 条

[1]

Alagarsamy V(2006)Synthesis, analgesic, anti-inflammatory, ulcerogenic index and antibacterial activities of novel 2-methylthio-3-substituted-5,6,7,8-tetrahydrobenzo (b) thieno[2,3-d]pyrimidin-4(3H)-ones Eur J Med Chem 41 1293-1300

[2]

Meena S(2007)Synthesis of some new bioactive 3-amino-2-mercapto-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4(3H)-one derivatives Eur J Med Chem 42 719-728

[3]

Ramseshu KV(1990)Synthesis and pharmacological activities of some 3-substituted thienopyrimidin-4-one-2-thiones Eur J Med Chem 25 635-639

[4]

Solomon VR(1998)Synthesis of 7H-tetrazolo[1,5-c]pyrrolo[3,2-e]pyrimidines and their reductive ring cleavage to 4-aminopyrrolo[2,3-d]pyrimidines J Heterocycl Chem 35 1295-1300

[5]

Thirumurugan K(2011)The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes Eur J Med Chem 46 71-76

[6]

Dhanabal K(1973)Effect of bilateral adrenalectomy on production of restraint ulcers in the stomach of albino rats Can J Physiol Pharmacol 51 748-750

[7]

Murugan M(1985)The effect of biological variables on the antiulcerogenic effect of vegetable plantain banana Planta Med 51 85-88

[8]

Ashalatha BV(1995)Polycyclic azines with heteroatoms in the 1- and 3-position. 40. Synthesis of heterocyclic immunomodulators. 2. 3-Mercaptoalkylthieno(2,3-d)pyrimidine-2,4(1H,3H)-diones: synthesis and testing of immunostimulant activity Arch Pharm 328 231-234

[9]

Narayana B(1997)Synthesis of some biologically active agents derived from thieno[2,3-d]pyrimidine derivatives Pharmazie 52 753-758

[10]

Vijaya Raj KK(1980)Heat and other physiological stress-induced analgesia: catecholamine mediated and naloxone reversible response Life Sci 27 185-188

← 1 2 3 4 5 6 7 8 9 10 →