α-Ketoheterocycles Able to Inhibit the Generation of Prostaglandin E2 (PGE2) in Rat Mesangial Cells

被引：1

作者：

Psarra, Anastasia ^{[1
]}

Theodoropoulou, Maria A. ^{[1
]}

Erhardt, Martin ^{[2
]}

Mertiri, Marina ^{[1
]}

Mantzourani, Christiana ^{[1
]}

Vasilakaki, Sofia ^{[1
]}

Magrioti, Victoria ^{[1
]}

Huwiler, Andrea ^{[2
]}

Kokotos, George ^{[1
]}

机构：

[1] Natl & Kapodistrian Univ Athens, Dept Chem, Athens 15771, Greece

[2] Univ Bern, Inst Pharmacol, CH-3010 Bern, Switzerland

来源：

BIOMOLECULES | 2021年 / 11卷 / 02期

基金：

瑞士国家科学基金会;

关键词：

anti-inflammatory; inhibition; alpha-ketobenzothiazoles; mesangial cells; prostaglandin E-2;

D O I：

10.3390/biom11020275

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：

Prostaglandin E-2 (PGE(2)) is a key mediator of inflammation, and consequently huge efforts have been devoted to the development of novel agents able to regulate its formation. In this work, we present the synthesis of various alpha-ketoheterocycles and a study of their ability to inhibit the formation of PGE(2) at a cellular level. A series of alpha-ketobenzothiazoles, alpha-ketobenzoxazoles, alpha-ketobenzimidazoles, and alpha-keto-1,2,4-oxadiazoles were synthesized and chemically characterized. Evaluation of their ability to suppress the generation of PGE(2) in interleukin-1 beta plus forskolin-stimulated mesangial cells led to the identification of one alpha-ketobenzothiazole (GK181) and one alpha-ketobenzoxazole (GK491), which are able to suppress the PGE(2) generation at a nanomolar level.

引用

页码：1 / 19

页数：19

共 50 条

[1] Small Peptides Able to Suppress Prostaglandin E2 Generation in Renal Mesangial Cells
Vasilakaki, Sofia
Pastukhov, Oleksandr
Mavromoustakos, Thomas
Huwiler, Andrea
Kokotos, George
MOLECULES, 2018, 23 (01):
[2] Regulation of parietal cells apoptosis by prostaglandin E2 (PGE2)
Pausawasdi, N
Ramamoorthy, S
Stepan, V
Crofford, LJ
Todisco, A
GASTROENTEROLOGY, 2004, 126 (04) : A81 - A81
[3] Functional nuclear prostaglandin E2 (PGE2) receptors
Bhattacharya, M
Dumont, I
Varma, D
Chemtob, S
FASEB JOURNAL, 1999, 13 (04): : A462 - A462
[4] CALCIUM DEPENDENCY OF PROSTAGLANDIN-E2 (PGE2) PRODUCTION IN CULTURED MESANGIAL CELLS
SWIDLER, MA
BONVENTRE, JV
CLINICAL RESEARCH, 1986, 34 (02): : A611 - A611
[5] PROSTAGLANDIN E2(PGE2) BINDING TO MURINE MAMMARY-TUMOR CELLS
FULTON, AM
HANCHIN, CM
BUTLER, WB
PROCEEDINGS OF THE AMERICAN ASSOCIATION FOR CANCER RESEARCH, 1986, 27 : 15 - 15
[6] Prostaglandin E2 (PGE2) induces headache in healthy subjects
Wienecke, T.
Olesen, J.
Oturai, P. S.
Ashina, M.
CEPHALALGIA, 2009, 29 (05) : 509 - 519
[7] Prostaglandin E2 (PGE2) and Roflumilast Involvement in IPF Progression
Moshkovitz, Noa
Epstein Shochet, Gali
Shitrit, David
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 2023, 24 (15)
[8] Mammalian oocytes are targets for prostaglandin E2 (PGE2) action
Diane M Duffy
Lynda K McGinnis
Catherine A VandeVoort
Lane K Christenson
Reproductive Biology and Endocrinology, 8
[9] Mammalian oocytes are targets for prostaglandin E2 (PGE2) action
Duffy, Diane M.
McGinnis, Lynda K.
VandeVoort, Catherine A.
Christenson, Lane K.
REPRODUCTIVE BIOLOGY AND ENDOCRINOLOGY, 2010, 8
[10] ANTIHYPERTENSIVE EFFECT OF PROSTAGLANDIN E2 (PGE2) IN RENOVASCULAR HYPERTENSION
MUIRHEAD, EE
LEACH, BE
BROWN, GB
DANIELS, EG
HINMAN, JW
JOURNAL OF LABORATORY AND CLINICAL MEDICINE, 1967, 70 (06): : 986 - &

← 1 2 3 4 5 →