ABSTRACT
A series of trans-fused lactams containing the indane nucleus has been prepared. Compound 19 has much enhanced plasma stability compared with its lactone counterpart and shows appreciable in vitro anticoagulant activity.
Subject(s)
Anticoagulants/pharmacology , Indans/pharmacology , Lactams/pharmacology , Thrombin/antagonists & inhibitors , Anticoagulants/chemical synthesis , Binding Sites , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Indans/chemical synthesis , Inhibitory Concentration 50 , Lactams/chemical synthesis , Models, Molecular , Structure-Activity RelationshipABSTRACT
In the Aymara community of 'Utani', hierarchical relationships between middle aged and younger women are evident in the cycle of domestic life. An older woman - mother, sister, step mother, mother-in-law - has unquestioned authority as taskmistress over the labor of girls and young women; although very old women no longer wield such power. Post-marital residence patterns and the family life cycle contribute to the hierarchical relationships among women in an extended family household. When women's community-wide prestige is examined, however, a different pattern is apparent. Prestige among female peers is based less on age than on a woman's reputation for being long-suffering. The paper concludes that these two types of female hierarchy complement each other as part of women's adaptation to the exploitations of peasant life.
ABSTRACT
Three patients presented with axillary vein 'effort thrombosis'. Intravenous streptokinase for 3 days followed by heparin for 10 days restored patency and relieved symptoms. Pretreatment diagnosis and the effect of streptokinase were confirmed venographically and an abnormality in the subclavian vein just medial to the first rib was demonstrated. This stenosis was most severe and had a prominent bypass collateral in the oldest patient. It is proposed that, in the absence of superimposed thrombosis, the damage to the vein in predisposed patients is progressive with age, with establishment of permanent collaterals. Transaxillary first rib resection is advised to prevent compression of the veins in the thoracic outlet.
Subject(s)
Axillary Vein/pathology , Streptokinase/therapeutic use , Subclavian Vein/pathology , Thrombosis/drug therapy , Adult , Age Factors , Collateral Circulation , Constriction, Pathologic/complications , Heparin/therapeutic use , Humans , Ribs/surgery , Thrombosis/complicationsABSTRACT
The following 5-(2-substituted vinyl)-6-aza-2'-deoxyuridines were synthesized: (E)-5-(2-bromovinyl) (2) (6-aza-BVDU), 5-(2-bromo-2-fluorovinyl) (a mixture of E and Z isomers) (3), (E)-5-(2-chlorovinyl) (4), (E)-5-[2-(methylthio)vinyl] (5), 5-(2,2-dibromovinyl) (6), and 5-(3-furyl) (7). The synthesis of 2-6 utilized Wittig-type reactions on 5-formyl-1-(2'-deoxy-3', 5'-di-O-p-toluoyl-beta-D-erythro-pentofuranosyl)-6-azauracil (16). 6-Aza-BVDU (and its alpha-anomer) was also synthesized from (E)-5-(2-bromovinyl)-6-azauracil (12) by using standard deoxyribosidation methodology. Compound 7 was prepared from 5-(3-furyl)-6-azauracil (33) via a ribosidation/deoxygenation sequence. An attempt to prepare the corresponding 5-(2,2-difluorovinyl) analogue afforded instead a mixture of the 5-[(2,2-difluoro-2-methoxy)ethyl] and 5-(2,2,2-trifluoroethyl) derivatives 29 and 30. Compounds 2-7, 29, and 30 were tested for in vitro activity against herpes simplex virus types 1 and 2 (HSV-1, HSV-2). 6-Aza-BVDU (2) exhibited ID50s of 8 micrograms/mL vs. HSV-1 and 190 micrograms/mL vs. HSV-2. BVDU (1) had ID50s of 0.015 and 1.6 micrograms/mL against HSV-1 and HSV-2, respectively. Compound 4 showed a similar profile of activity, but the other analogues were either weakly active or inactive.
