piperidines and 2-amino-1-3-4-thiadiazole

piperidines has been researched along with 2-amino-1-3-4-thiadiazole* in 1 studies

Other Studies

1 other study(ies) available for piperidines and 2-amino-1-3-4-thiadiazole

Article	Year
2-Amino-1,3,4-thiadiazoles in the 7-hydroxy-N-neopentyl spiropiperidine indolinyl series as potent P2Y1 receptor antagonists. Bioorganic & medicinal chemistry letters, 2014, Jun-01, Volume: 24, Issue:11 Blockade of the P2Y1 receptor is important to the treatment of thrombosis with potentially improved safety margins compared with P2Y12 receptor antagonists. Investigation of a series of urea surrogates of the diaryl urea lead 3 led to the discovery of 2-amino-1,3,4-thiadiazoles in the 7-hydroxy-N-neopentyl spiropiperidine indolinyl series as potent P2Y1 receptor antagonists, among which compound 5a was the most potent and the first non-urea analog with platelet aggregation (PA) IC50 less than 0.5 μM with 10 μM ADP. Several 2-amino-1,3,4-thiadiazole analogs such as 5b and 5f had a more favorable pharmacokinetic profile, such as higher Ctrough, lower Cl, smaller Vdss, and similar bioavailability compared with 3. Topics: Animals; Dose-Response Relationship, Drug; Humans; Indoles; Molecular Structure; Piperidines; Rats; Receptors, Purinergic P2Y1; Structure-Activity Relationship; Thiadiazoles	2014

Article

Year

2-Amino-1,3,4-thiadiazoles in the 7-hydroxy-N-neopentyl spiropiperidine indolinyl series as potent P2Y1 receptor antagonists.

Bioorganic & medicinal chemistry letters, 2014, Jun-01, Volume: 24, Issue:11

Blockade of the P2Y1 receptor is important to the treatment of thrombosis with potentially improved safety margins compared with P2Y12 receptor antagonists. Investigation of a series of urea surrogates of the diaryl urea lead 3 led to the discovery of 2-amino-1,3,4-thiadiazoles in the 7-hydroxy-N-neopentyl spiropiperidine indolinyl series as potent P2Y1 receptor antagonists, among which compound 5a was the most potent and the first non-urea analog with platelet aggregation (PA) IC50 less than 0.5 μM with 10 μM ADP. Several 2-amino-1,3,4-thiadiazole analogs such as 5b and 5f had a more favorable pharmacokinetic profile, such as higher Ctrough, lower Cl, smaller Vdss, and similar bioavailability compared with 3.

Topics: Animals; Dose-Response Relationship, Drug; Humans; Indoles; Molecular Structure; Piperidines; Rats; Receptors, Purinergic P2Y1; Structure-Activity Relationship; Thiadiazoles

2014