Lee, Koo published the artcileStructural modification of an orally active thrombin inhibitor, LB30057: replacement of the D-pocket-binding naphthyl moiety, Name: 5,6,7,8-Tetrahydronaphthalene-2-sulfonyl chloride, the publication is Bioorganic & Medicinal Chemistry (1998), 6(6), 869-876, database is CAplus and MEDLINE.
Amidrazonophenylalanine derivative LB30057 (I) was identified as a potent (Ki=0.38 nM), selective, and orally active thrombin inhibitor. As a continuation of studies into benzamidrazone-based thrombin inhibitors, we have structurally modified I by replacing the naphthyl group with a variety of hydrophobic moieties. This study led to discovery of several compounds with significantly enhanced potency in thrombin inhibition without sacrificing selectivity against trypsin and oral absorption. The highest activity was obtained with benzocycloheptyl derivative II (Ki = 0.045 nM).
Bioorganic & Medicinal Chemistry published new progress about 61551-49-3. 61551-49-3 belongs to chlorides-buliding-blocks, auxiliary class Liquid Crystal &OLED Materials, name is 5,6,7,8-Tetrahydronaphthalene-2-sulfonyl chloride, and the molecular formula is C10H11ClO2S, Name: 5,6,7,8-Tetrahydronaphthalene-2-sulfonyl chloride.
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