Sulphonamide-based small molecule VLA-4 antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 21, 2003, Pages 3875-3878

  Stasiak, Marcin ^a,b   Mehlin, Christopher ^a,c   Boni, Erica ^a,c   Vaisar, Tomas ^a,c   Little, Thomas ^a,d   Kim, Hwa Ok ^a,e   Qabar, Maher ^a,e  

^a Molecumetics Ltd   (United States)

^b Corus Pharma ^*  (United States)

^c UNIVERSITY OF WASHINGTON   (United States)

^d CEPTYR Inc   (United States)

^e Aurigene Discovery Technologies   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CD29 ANTIGEN ANTAGONIST; SULFONAMIDE; UNCLASSIFIED DRUG;

ANIMAL MODEL; ARTICLE; ASTHMA; CONTROLLED STUDY; DRUG STRUCTURE; DRUG SYNTHESIS; MONKEY; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

EID: 0141656338     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00760-1     Document Type: Article

References (19)

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14. 50 of 100 nM.
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19. The measurement of eosinophil influx into broncoalveolar lavage (BAL) was done as follows: BALB/C female mice received compound 6 on day 15, 18 and 21 at 15 min before OVA challenge. Twenty-four hours after final OVA challenge, the mice underwent exsanguinations by posterior vena cava puncture and then BAL (0.4 mL of saline three times) was performed on the right lung after tying of the left lung at the mainstem bronchus. Total BAL fluid cells were counted from a 0.05 mL aliquot and the remaining fluid was centrifuged at 1200 rpm (Microcentrifuge, 5415 C, Eppendorf) for 5 min. The cell pellets were resuspended in saline containing 10% BSA (Calbiochem, San Diego, CA, USA) and smears were made on glass slides. Eosinophiles were stained for 5-8 min with Discombe's diluting fluid containing (0.05% aqueous eosin and 5% (v/v) acetone in distilled water, and then counterstained with 0.07% methylene blue.