- Discovery of 7-(Prolinol-N-yl)-2-phenylamino-thiazolo[5,4-d]pyrimidines as Novel Non-Nucleoside Partial Agonists for the A2A Adenosine Receptor: Prediction from Molecular Modeling
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We describe the identification of 7-(prolinol-N-yl)-2-phenylamino-thiazolo[5,4-d]pyrimidines as a novel chemotype of non-nucleoside partial agonists for the A2A adenosine receptor (A2AAR). Molecular-modeling indicated that the (S)-2-hydroxymethylene-pyrrolidine could mimic the interactions of agonists' ribose, suggesting that this class of compounds could have agonistic properties. This was confirmed by functional assays on the A2AAR, where their efficacy could be associated with the presence of the 2-hydroxymethylene moiety. Additionally, the best compound displays promising affinity, selectivity profile, and physicochemical properties.
- Bharate, Sandip B.,Singh, Baljinder,Kachler, Sonja,Oliveira, Ana,Kumar, Vikas,Bharate, Sonali S.,Vishwakarma, Ram A.,Klotz, Karl-Norbert,Gutiérrez De Terán, Hugo
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- Synthesis, antiproliferative and apoptosis-inducing activity of thiazolo[5,4-d]pyrimidines
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Thiazolo[5,4-d]pyrimidines are important class of heterocyclic compounds possessing diverse range of biological activities. Herein, we report an efficient synthesis of thiazolo[5,4-d]pyrimidines using recyclable KF/alumina catalyst. The reaction of 4,6-di
- Singh, Baljinder,Guru, Santosh K.,Kour, Smit,Jain, Shreyans K.,Sharma, Rajni,Sharma, Parduman R.,Singh, Shashank K.,Bhushan, Shashi,Bharate, Sandip B.,Vishwakarma, Ram A.
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p. 864 - 874
(2013/12/04)
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- Identification and synthesis of 2,7-diamino-thiazolo[5,4-d]pyrimidine derivatives as TRPV1 antagonists
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We have identified and synthesized a series of 2,7-diamino-thiazolo[5,4-d]pyrimidines as TRPV1 antagonists. An exploration of the structure-activity relationships at the 2-, 5-, and 7-positions of the thiazolo[5,4-d]pyrimidine led to the identification of
- Lebsack, Alec D.,Branstetter, Bryan J.,Hack, Michael D.,Xiao, Wei,Peterson, Matthew L.,Nasser, Nadia,Maher, Michael P.,Ao, Hong,Bhattacharya, Anindya,Kansagara, Mena,Scott, Brian P.,Luo, Lin,Rynberg, Raymond,Rizzolio, Michele,Chaplan, Sandra R.,Wickenden, Alan D.,Guy Breitenbucher
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scheme or table
p. 40 - 46
(2009/04/10)
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- Thiazolopyrimidine modulators of TRPV1
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Certain TRPV1-modulating thiazolopyrimidine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
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Page/Page column 13
(2008/06/13)
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- Single-step syntheses of 2-amino-7-chlorothiazolo[5,4-d]pyrimidines: Intermediates for bivalent thiazolopyrimidines
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A single-step process for the preparation of 2-amino-7-chlorothiazolo[5,4- d]pyrimidines, 2, was achieved by the reaction of the commercially available 4,6-dichloro-5-aminopyrimidine 1 with isothiocyanates. This mild reaction accommodates a variety of fun
- Liu, Jian,Patch, Raymond J.,Schubert, Carsten,Player, Mark R.
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p. 10194 - 10197
(2007/10/03)
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