📜马尿酸,L-组氨酰-L-亮氨酸置于angiotensin I Converting Enzyme体系中,用 水,二甲基亚砜 作为反应溶剂,化学反应生成 马脲酰组氨酰亮氨酸hhl 参考文献:Novel Fluorogenic Substrates Containing Bimane System For Microdetermination Of Angiotensin I Converting Enzyme. 标题:Novel Fluorogenic Substrates Containing Bimane System For Microdetermination Of Angiotensin I Converting Enzyme. 摘要:作为一种灵敏的荧光分析法,用于检测血管紧张素转化酶活性的含吲哚乙酸的联苯胺肽,即1,7-二氧-2,5,6-三甲基-1H,7H,吡唑[1,2-α]吡唑-3-基-甲硫甲酰基-甘氨酰(或l-苯丙氨酰)-L-色氨酰-L-亮氨酸(或l-脯氨酸),已被合成,并被证明是用于微量测定血管紧张素i转化酶活性的强效荧光底物. DOI:10.1248/cpb.37.145
专利号:US-2004033532-A1 优先权日:2002-08-08 标题 :Use of three-dimensional crystal structure coordinates to design and synthesize domain-selective inhibitors for angiotensin-converting enzyme (ACE) 发明人:EHLERS MARIO R W; HOLMQUIST BARTON 摘要:It has now been discovered that the use of the three-dimensional crystal structure coordinates of angiotensin-converting enzyme (ACE) will enable the design and synthesis, by means of computational chemistry and structure-guided drug design, of inhibitors of ACE that are highly selective and specific for either the N domain or the C domain of the enzyme, for the treatment of diverse diseases. The invention also relates to methods and processes for the structure-guided design and synthesis of dual N- and C-domain ACE inhibitors, and inhibitors that operate by competitive, non-competitive, uncompetitive, and irreversible mechanisms.
专利号:US-7951834-B2 优先权日:2005-05-27 标题 :Angiotensin I-converting enzyme (ACE) inhibitors 发明人:STURROCK EDWARD; NCHINDA ALOYSIUS; CHIBALE KELLY 权利人:UNIV CAPE TOWN 摘要:This invention relates to a process for the synthesis of ketomethylene derivatives of the tripeptide Phe-Gly-Pro (“keto-ACEâ€?, compound 5 a ) and analogues thereof. The synthesis process proceeds via an α,β-unsaturated keto intermediate. A key feature of the process involves a Horner-Emmons olefination of the, -unsaturated keto-phosphonate with ethyl glyoxylate. Keto-ACE analogues produced by the process of the invention display C-domain selectivity.
专利号:US-4410520-A 优先权日:1981-11-09 标题 :3-Amino-[1]-benzazepin-2-one-1-alkanoic acids 发明人:WATTHEY JEFFREY W H 权利人:CIBA GEIGY CORP 摘要:Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-2,3,4,5-tetrahydro-1H-[1]benzaz epin-2-ones and functional derivatives are angiotension converting enzyme inhibitors and are useful as antihypertensive agents. Synthesis of, compositions and methods of treatment utilizing such compounds are included.
专利号:SU-1709912-A3 优先权日:1986-01-06 标题 :Method for the synthesis of 4-phenylbutylphosphonic acid proline-containing ester
专利号:RU-2012556-C1 优先权日:1988-09-05 标 题:Method of synthesis of cycloalkylglutaramide derivatives or theirs pharmaceutically acceptable salts
专利号:US-6998259-B1 优先权日:1999-05-20 标题:Enzymatic treatment of whey proteins for the production of antihypertensive peptides and the resulting products 发明人:DAVIS MARTIN E; RAO ANAND; GAUTHIER SYLVIE; POULIOT YVES; GOURLEY LINE; ALLAIN ANNE-FRANCOISE 权利人:DAVISCO FOODS INTERNAT 摘要:Enzymatic digests of whey protein concentrates were prepared using animal, bacterial and fungal proteases, and evaluated for antihypertensive activities. The highest ACE-inhibitory activity was obtained with the purified peptide β-1g (f142–148) obtained by chemical synthesis, for which an IC 50 value of 0.04 mg powder.ml −1 was found. The hydrolysates derived from BiPROâ„¢ whey protein isolate and β-1g both gave higher antihypertensive activities (IC 50 values of 0.29 to 0.90 mg powder.ml −1 ) than the other hydrolysates tested (IC 50 values of 0.96 and 1.30 mg powder.ml −1 ). The recovered hydrolysate can be used to treat hypertension in mammals such as humans and domestic pets such as dogs and cats.
参考文献:10.1016/0162-3109(96)00018-5 摘要:Hecker M, Bara AT, Busse R. Potentiation of the biological efficacy of bradykinin by ACE inhibitors: a shift in the affinity of the B2 receptor Immunopharmacology. 1996 Jun;33(1-3):93–4. doi: 10.1016/0162-3109(96)00018-5. 摘要:Giugliano G, Grieco P, Ialenti A, Mottola M, Perissutti E, Santagada V. Synthesis and biological evaluation of proline derivatives as potential angiotensin converting enzyme inhibitor. Boll Soc Ital Biol Sper. 1996 Jan;72(1-2):29–36. 参考文献:10.1007/s10529-008-9702-9 摘要:Ponrasu T, Charles RE, Sivakumar R, Divakar S. Syntheses of alpha-tocopheryl glycosides by glucosidases. Biotechnol Lett. 2008 Aug;30(8):1431–9. doi: 10.1007/s10529-008-9702-9. 参考文献:10.1007/s11357-012-9497-4 摘要:Arutyunyan TV, Korystova AF, Kublik LN, Levitman MKh, Shaposhnikova VV, Korystov YN. Effects of taxifolin on the activity of angiotensin-converting enzyme and reactive oxygen and nitrogen species in the aorta of aging rats and rats treated with the nitric oxide synthase inhibitor and dexamethasone. Age (Dordr). 2013 Dec;35(6):2089–97. 参考文献:10.1007/s12010-012-0024-y 摘要:He H, Liu D, Ma C. Review on the Angiotensin-I-Converting Enzyme (ACE) Inhibitor Peptides from Marine Proteins. Applied Biochemistry and Biotechnology. 2012 Dec 29;169(3):738–49. doi: 10.1007/s12010-012-0024-y.