Synthesis and biological evaluation of thiophene [3,2-b] pyrrole derivatives as potential anti-inflammatory agents

被引：75

作者：

Kumar, PR

Raju, S

Goud, PS

Sailaja, M

Sarma, MR

Reddy, GO

Kumar, MP

Reddy, VVRMK

Suresh, T

Hegde, P

机构：

[1] Dr Reddys Labs Ltd, Technol Dev Ctr, Proc Chem R&D, Hyderabad 500049, Andhra Pradesh, India

[2] Dr Reddys Labs Ltd, Dept Pharmacol, Discovery Res, Hyderabad 500049, Andhra Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2004年 / 12卷 / 05期

关键词：

thieno-[3,2-b]-pyrrole; anti-inflammatory; biological activity; rat-paw edema;

D O I：

10.1016/j.bmc.2003.11.003

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：

A series of thiophene [3,2-b] pyrrole derivatives were synthesized and evaluated their abilities to inhibit anti-inflammatory activity. In this series, substituent effects at the N-1, 2 and 5 positions of thiophene [3,2-b] pyrrole were examined. The results obtained are compared to those previously reported anti-inflammatory drugs like Tenidap sodium, Diclofenac sodium and Piroxicam. The results indicated the critical role of the group linked in the N-1 position and 2, 5 positions of thiophene [3,2-b] pyrrole with different functional groups. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：1221 / 1230

页数：10

共 16 条

[1] ANALOGS AND DERIVATIVES OF TENOXICAM .1. SYNTHESIS AND ANTIINFLAMMATORY ACTIVITY OF ANALOGS WITH DIFFERENT RESIDUES ON THE RING NITROGEN AND THE AMIDE NITROGEN
BINDER, D
HROMATKA, O
GEISSLER, F
SCHMIED, K
NOE, CR
BURRI, K
PFISTER, R
STRUB, K
ZELLER, P
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1987, 30 (04) : 678 - 682
[2] Thieno[3,2-b]- and thieno[2,3-b]pyrrole bioisosteric analogues of the hallucinogen and serotonin agonist N,N-dimethyltryptamine
Blair, JB
Marona-Lewicka, D
Kanthasamy, A
Lucaites, VL
Nelson, DL
Nichols, DE
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (06) : 1106 - 1111
[3] CATRY TJ, 1988, ARTHRITIS RHEUM, V31, pS89
[4] CAVANAUGH MJ, 1995, RHEUMATOL EUR, V2, pD135
[5] ERAS J, 1984, J HETEROCYCLIC CHEM, V27, P215
[6] PREPARATION + REACTIONS OF 5-CARBETHOXYTHIENO(3,2-B)PYRROLE + SOME OF ITS DERIVATIVES
GALE, WW
SNYDER, HR
SCOTT, AN
[J]. JOURNAL OF ORGANIC CHEMISTRY, 1964, 29 (08) : 2160 - &
[7] GARCIA F, 1985, SYNTHESIS-STUTTGART, P143
[8] GRANGER DN, 1994, ARTHRITIS RHEUM, V37, P1053
[9] Kadin SB, 1985, US Patent, Patent No. [4,556,672, 4556672]
[10] SYNTHESIS OF 6-SUBSTITUTED THIENO[3,2-B]PYRROLES
KEENER, RL
SKELTON, FS
SNYDER, HR
[J]. JOURNAL OF ORGANIC CHEMISTRY, 1968, 33 (04) : 1355 - &

← 1 2 →