Naphthylalkyl lactamimides as inhibitors of blood platelet aggregation

Abstract

Grisar, et at. measurement was determined on 15 and was found to be consistent with the formula C19H161602180 within 4 ppm. The location of the 180 in warfarin was checked by the ratio of m/e 267/m/e 265 fragment ions (Table II).23 References(1) K.

Five-, Six-, and Seven-membered Lactim Ethers. Methods of Synthesis and Chemical Properties. (Review)

“…The reaction of lactim ethers with aniline derivatives 75 was carried out by heating in xylene (3 h) [108] or at 140-150°C (10 h) [100], and as a result the cyclic amidines 76 were obtained. The reactions of lactim ethers with primary amines or their hydrochlorides 77, containing bi-or tricyclic condensed fragments separated from the amino group by a carbon atom or (in one example [97]) by a CH=CH group (here R 2 = cyclo-C 3 H 5 ), were reported in the patents [100,101,109,111] and papers [97,110].…”

“…In most cases the products 78 were obtained with yields of 50-82% [97,110] by keeping the reagents at 20°C for seven days without a solvent [97][98][99][100][101][102][103][104][105][106][107][108][109][110][111] or in alcohol [95] or by boiling in methanol (3 h) [110] or xylene (10 h) [100].…”

“…The products 93 [127] and 94 [126] were obtained from lactim ethers and the salts 91 and 92 respectively. It should be noted in conclusion that many of the compounds synthesized by the reactions of lactim ethers with amines exhibit a wide range of biological activity: They are inhibitors of the coagulation of blood [102,[104][105][106][109][110][111][112], exhibit hypoglycemic activity [91, 93-95, 104, 108, 109], antiviral activity [92,93,103], anti-inflammatory activity [104], antitumor activity [119], and antidiabetic activity [92], and have also been recommended as fungicides [87,125,128] or additives that increase the productivity of animals [100].…”

Substituted 3,4-pentadienyldiamines as inhibitors of platelet aggregation

“…This procedure was used for the preparation of most compounds listed in Table I. 5) 10 (3) flC, H, and N analyses were found within ±0.4% of calculated values except where indicated. */« vitro effect of test compound on the inhibition of platelet aggregation caused by adenosine diphosphate in human platelet-rich plasma.…”

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jV-(2-Butyl-2-ethyl-5-methyl-3,4-hexadienyl)-l,3-propanediamine (10, RMI 10,277) was found to inhibit in vitro and in vivo ADP-induced platelet aggregation with minimal release of procoagulant platelet factor 3 (PF3). The diamines 26, 30, 39, and 47 and the triamine 9 were also found to have high in vitro potency of about ten times that of previously known agents, excepting prostaglandin PGE].

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