Category: 321565-33-7

Tsuno, Naoki published the artcilePharmacological evaluation of novel (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives as TRPV4 antagonists for the treatment of pain, COA of Formula: C5H5ClN2O2S, the publication is Bioorganic & Medicinal Chemistry (2017), 25(7), 2177-2190, database is CAplus and MEDLINE.

A novel series of (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives were identified as selective transient receptor potential vanilloid 4 (TRPV4) channel antagonist and showed analgesic effect in Freund’s Complete Adjuvant (FCA) induced mech. hyperalgesia model in guinea pig and rat. Modification of right part based on the compound I which was disclosed in the previous communication led to the identification of compound II as a flagship compound In this paper, the authors described the details about design, synthesis and structure-activity relationship (SAR) anal.

Bioorganic & Medicinal Chemistry published new progress about 321565-33-7. 321565-33-7 belongs to pyrimidines, auxiliary class Pyrimidine, name is 2-Chloro-5-methanesulfonylpyrimidine, and the molecular formula is C5H6N2O2, COA of Formula: C5H5ClN2O2S.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia

Bolli, Martin H. published the artcileNovel Benzo[1,4]diazepin-2-one Derivatives as Endothelin Receptor Antagonists, Computed Properties of 321565-33-7, the publication is Journal of Medicinal Chemistry (2004), 47(11), 2776-2795, database is CAplus and MEDLINE.

Since its discovery in 1988 by Yanagisawa et al., endothelin (ET), a potent vasoconstrictor, has been widely implicated in the pathophysiol. of cardiovascular, cerebrovascular, and renal diseases. Many research groups have embarked on the discovery and development of ET receptor antagonists for the treatment of such diseases. While several compounds, e.g., ambrisentan, are in late clin. trials for various indications, one compound (bosentan, Tracleer) is being marketed to treat pulmonary arterial hypertension. Inspired by the structure of ambrisentan, a novel class of ET receptor antagonists based on a 1,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepin-2-one scaffold was designed. The preparation as well as the in vitro and in vivo structure-activity relationships of these derivatives are reported. Potent dual ET_A/ET_B receptor antagonists with affinities in the low nanomolar range have been identified. In addition, several compounds efficiently reduced arterial blood pressure after oral administration to Dahl salt-sensitive rats. In this animal model, the efficacy of (αR,5R)-rel-α-[(4,6-dimethyl-2-pyrimidinyl)oxy]-2,3,4,5-tetrahydro-2-oxo-5-phenyl-1-[(2,4,6-trifluorophenyl)methyl]-1H-1,4-benzodiazepine-5-acetic acid (I) was superior to that of racemic ambrisentan.

Journal of Medicinal Chemistry published new progress about 321565-33-7. 321565-33-7 belongs to pyrimidines, auxiliary class Pyrimidine, name is 2-Chloro-5-methanesulfonylpyrimidine, and the molecular formula is C5H5ClN2O2S, Computed Properties of 321565-33-7.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia