Fattori, Daniela published the artcileDesign and synthesis of novel sulfonamide-containing bradykinin hB2 receptor antagonists. 2. synthesis and structure-activity relationships of α,α-cycloalkylglycine sulfonamides, HPLC of Formula: 6249-56-5, the publication is Journal of Medicinal Chemistry (2007), 50(3), 550-565, database is CAplus and MEDLINE.
Recently, the design and synthesis of a class of selective nonpeptide bradykinin (BK) B2 receptor antagonists (J. Med. Chem. 2006, 3602-3613) was reported. This work led to the discovery of MEN 15442 (I), an antagonist with subnanomolar affinity for the human B2 receptor (hB2R), which also displayed significant and prolonged activity in vivo (for up to 210 min) against BK-induced bronchoconstriction in the guinea-pig at a dose of 300 nmol/kg (it), while demonstrating only a slight effect on BK-induced hypotension. Herein, the further optimization of this series of compounds aimed at maximizing the effect on bronchoconstriction and minimizing the effect on hypotension, with a view to developing topically delivered drugs for airway diseases, is described. It was found that MEN 16132 (II), after intratracheal or aerosol administration, inhibited, in a dose-dependent manner, BK-induced bronchoconstricton in the airways, while showing minimal systemic activity. This compound was selected as a preclin. candidate for the topical treatment of airway diseases involving kinin B2 receptor stimulation.
Journal of Medicinal Chemistry published new progress about 6249-56-5. 6249-56-5 belongs to chlorides-buliding-blocks, auxiliary class Phase Transfer Catalyst,Inhibitor,Natural product, name is 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride, and the molecular formula is C7H16ClNO2, HPLC of Formula: 6249-56-5.
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