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Bioorganic and Medicinal Chemistry Letters

Volumn 5, Issue 12, 1995, Pages 1219-1224

Novel prostanoid thromboxane A2 antagonists

(5) Klar, U a Kuhnke, J a Pletsch, A a Rehwinkel, H a Schreyer, R a

a BAYER PHARMA AG (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

12 (4 CHLOROBENZENESULFONAMIDO) 9 FLUORO 13,14,15,16,17,18,19,20 OCTANOR 5 PROSTANOIC ACID; PROSTANOID; THROMBOXANE A2 RECEPTOR; THROMBOXANE A2 RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DRUG SYNTHESIS; STRUCTURE ACTIVITY RELATION; THROMBOCYTE AGGREGATION;

EID: 0028998886 PISSN: 0960894X EISSN: None Source Type: Journal
DOI: 10.1016/0960-894X(95)00199-4 Document Type: Article

Times cited : (3)

References (11)

1
- 84921202861
- Joachim K.-D.; Klar U.; Pletsch A.; Rehwinkel H.; and Skuballa W. Prostaglandins, accepted for publication.

2
- 0024273549
- (1988) Drugs Future , vol.13 , pp. 999
- Lefer¹

3
- 0025808691
- (1991) J. Org. Chem. , vol.56 , pp. 2122
- Ohtani¹ Matsuura² Watanabe³ Narisada⁴

4
- 0025866914
- (1991) Drugs Future , vol.16 , pp. 701
- Perzborn¹ Boberg² Bühner³

5
- 84921202860
- The structures of all synthesized compounds were at least confirmed by high resolution NMR-spectroscopy.

6
- 0348174862
- (1982) Tetrahedron Lett. , vol.23 , pp. 4481
- Pradhan¹ Kolhe² Mistry³

7
- 84921202859
- To simplify the discussion, the prostaglandin numbering concerning the five membered ring will be maintained throughout this paper regardless of the changes made in the side chains.

8
- 0022653788
- (1986) J. Med. Chem. , vol.29 , pp. 313
- Skuballa¹ Schillinger² Stürzebecher³ Vorbrüggen⁴

9
- 84921202858
- 3H-SQ 29548 on platelet membranes is 20 nM. Unlabelled SQ 29548 or test compounds are added at concentrations up to 10 μM; nc means no competition; np not parallel. A detailed experimental description is given in Klar U.; Pletsch A.; Rehwinkel H.; Schreyer R. Biomed. Chem. Lett., submitted for publication.

10
- 84921202857
- −3 M and diluted 1:1 with Tyrode buffer); stirred continuously at 1000 rpm; where the optical density of unstimulated platelets was taken to represent 0% aggregation and that of platelet poor plasma to represent 100% aggregation. Test substances were added to PRP to investigate pro-aggregatory activity; in the absence of pro-aggregatory activity; the effects of test substance on aggregation induced by the stable TP-mimetic U 46619 (1 μM) were assessed following pre-incubation with test substance for 1 minute. All values are given in micromolar concentrations and represent a single determination; ne means not effective at concentrations up to 10 μM. Data given in brackets are determined using gel-filtered platelets.

11
- 84921202856
- These values correspond to the 9α-fluoro-epimer.

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