Antihypotensive activity

Glushkov VA, Stryapunina OG, Dolzhenko AV et al (2009) Synthesis and antiaggregant and antihypotensive activity of benzo-annelated azabicyclo[m.n.0]alkanes. Pharm Chem J 43 245-248... 

The ability to smoothly convert 343 into the C2-symmetric chiral epoxide tmns-(2S,3S) 2,3-epoxybutane (344) [122] has been exploited for the preparation of (3 S, 47 )-4-(/er -butyldimethylsilyloxy)-l-iodo-3-methylpentane (345), which is used to prepare the crucial intermediate 346 necessary for the convergent synthesis of Lacrimin A (347), a chemically modified Milbemycin having antihypotensive activity [123] (Scheme 77). 

The same chromophore as is found in the arcyriaflavins occurs also in rebeccamycin (516) and in its dechloro derivative, two antitumour antibiotics isolated from Nocardia aerocoligenes 510). Also closely related to these compounds are staurosporin (517), an antibiotic from Streptomyces staurosporeus which exhibits pronounced antihypotensive activity 258), and other carbohydrate bridged bisindoles (575). Due to the small amounts of Arcyria metabolites available from the... 

Purslane contains large amounts of /-norepinephrine (/-noradrenaline 0.25% in fresh herb), a neurohormone that has vasopressor and antihypotensive activities and reduces hemorrhage at the tissue level (jiangsu martindale). 

Hexahydro-l-phenyl-3jFf-oxazolo[3,4-a]pyridin-3-imines (292) have antihypotensive and central nervous system stimulant activity which is stereochemically dependent. Most active is the (-)-trans form of the parent compound (292 R = H, Ar = Ph) (80MI42902). Useful stimulant activity for the central nervous system has also been claimed for 2,3,5,6-tetrahydro-7H-oxazolo[3,2-a]pyrimidin-7-ones (74GEP2253555) and quinazoline homo-logues (293) (74GEP2252122). 

Drim-8-en-l 1-oic acid (158) is a convenient synthon for the preparation of polyfunctional drimanes. This acid has been used as an intermediate in the total synthesis of 1,6,7-tridesoxyforskolin (159), a related compound to forskolin (160), possessing ionotropic, antihypotensive and other activities [106]. Optically active compound (159) was isolated together with forskolin from the plant Coleus forskohlii [107]. 

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