36926-36-0Relevant articles and documents
Discovery and SAR of a novel series of Natriuretic Peptide Receptor-A (NPR-A) agonists
Iwaki, Takehiko,Nakamura, Yuji,Tanaka, Taisaku,Ogawa, Yasuyuki,Iwamoto, Osamu,Okamura, Yoshihiko,Kawase, Yumi,Furuya, Mayumi,Oyama, Yoshiaki,Nagayama, Takahiro
, p. 4904 - 4907 (2017)
Novel thienopyrimidine compounds 2 and 3 were discovered from high-throughput screening as Natriuretic Peptide Receptor A (NPR-A) agonists. Scaffold hopping of a thienopyrimidine ring to a quinazoline ring, introduction of the basic functional group and optimization of the substituent on the 6-position of the benzene ring of quinazoline led to improved agonistic activity. We discovered compound 48, which showed potent agonistic activity for NPR-A with an EC50 value of 0.073 μM, indicating 350-fold potency compared to the hit compound 3.
Synthesis of Cyclic and Acyclic Nucleoside Analogues Having a Thiophene or Dihydrothiophene Ring Fused to the d Side of an Uracil
Jourdan, Fabrice,Renault, Jacques,Karamat, Abdesselam,Ladurie, Daniel,Robba, Max
, p. 953 - 958 (2007/10/02)
Synthesis of cyclic and acyclic nucleosides was achieved by alkylation of various new aglycones following the Vorbrueggen and Niedballa's procedure .The analytical results allowed us to conclude that the alkylation ocurred on N1 site led to the β anomeric form for the cyclic nucleosides.
