CAS: 7423-93-0; 3-Chloro-L-Tyrosine

相似化合物

478183-58-3 192315-36-9 15106-62-4

上下游产品

L-tyrosine (S)-3-benzyloxycarbonyl-4-(4-hydroxyphenyl)methyloxazolidin-5-one 2-mon°Chlorophenol sodium pyruvate 3-bromo-5-chloro-l(-)-tyrosine 2-(3-chloro-4-hydroxyphenyl)ethylamine Tyr Fm°C-L-3-chlorotyrosine

L-酪氨酸置于盐酸,溶剂黄146体系中,用 二甲基亚砜 作为反应溶剂,化学反应 0.03H,以89.21%的收率获得产物3-氯-L-酪氨酸
参考文献:一类新型的酪氨酸衍生物,具有pge 2介导的抗癌特性,是双重5-Lox和cox-2 / Mpges1抑制剂†
标题:一类新型的酪氨酸衍生物,具有pge 2介导的抗癌特性,是双重5-Lox和cox-2 / Mpges1抑制剂†
摘要:白三烯和前列腺素途径分别受酶lox和cox / Mpges1控制,并负责炎症反应.由mpges1产生的pge 2导致炎症以及癌症的发展.在hela细胞中合成,表征和测试了一系列19种新型酪氨酸衍生物,并针对5-Lox进行了体外测试,并测试了它们对pge 2的反应生成.发现6B-V和6C-I具有对5-Lox和pge 2产生的最大抑制作用.化合物6B-V已发现β-内啡肽通过破坏5-Lox酶的氧化还原循环起作用,并且其活性与市售药物zileuton相当.在临床试验中,另一种化合物6C-I的活性与licofelone相当,发现它主要抑制mpges1的mrna表达.它还将hela细胞停滞在细胞周期的s和g2 / M期,表明其抗癌活性.同样,化合物6B-Iv和6B-Viii抑制炎症级联反应中的lt和pg途径.苯环中存在碘似乎有利于抑制5-Lox,而氯有利于抑制pge 2生产.这些线索可以进一步优化和发展为抗炎和抗癌药物.
DOI:10.1039/c8Nj04385J

专利信息

专利号:US-12421534-B2
优先权日:2021-11-10
标 题 :Engineered enzymes and method for the synthesis of diverse tyrosine analogs
发明人：ALMHJELL PATRICK J; ARNOLD FRANCES H
权利人:CALIFORNIA INST OF TECHN
摘要:Provided herein is an engineered tryptophan synthase β-subunit (TrpB) that catalyzes the synthesis of tyrosine, tyrosine analogs, or salts thereof. Also provided herein are methods for preparing tyrosine, tyrosine analogs, or a salt thereof using the engineered TrpB described herein.

专利号:US-12351573-B2
优先权日:2019-05-09
标 题:Compounds for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; CHENG KAI FAN
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

专利号:US-2023159450-A1
优先权日:2020-05-08
标 题 :Dimers for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; ALTITI AHMAD
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

专利号:US-2004101523-A1
优先权日:1989-07-27
标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension
发明人：REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
权利人:SEARLE & CO
摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.

专利号:WO-9101724-A1
优先权日:1989-07-27
标题 :Renal-selective prodrugs for the treatment of hypertension
发明人：REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
权利人:SEARLE & CO
摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as depa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitors compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-Y-glutamyl fusaric acid is preferred.

专利号:WO-9201667-A1
优先权日:1990-07-25
标题 :Renal-selective prodrugs for control of renal sympathetic nerve activity in the treatment of hypertension
发明人：REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
权利人:SEARLE & CO
摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kydney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase-inhibitors, of which N-acetyl-η-glutamyl fusaric acid hydrazide [represented in formula (a)] is preferred.