CAS: 39544-74-6; Benzotript

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para-chlorobenzoic acid 4-chloro-benzoyl chloride L-Tryptophan(S)-2-(4-Chloro-benzoylamino)-3-(2-oxo-2,3-dihydro-1H-indol-3-yl)-propionic acid N-(N-4-chlorobenzoyl-L-tryptophanyl)-D-phenylalanine methyl ester

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    📜对氯苯甲酸置于氯化亚砜,N,N-二甲基甲酰胺,Sodium Hydroxide体系中,用 乙醚 作为反应溶剂,化学反应 3.0H,反应生成 N-(4-氯苯甲酰)-L-色氨酸
    参考文献:巯基乙酸硫酯及其水解产物巯基乙酸共同抑制金属-β-内酰胺酶l1 †
    标题:巯基乙酸硫酯及其水解产物巯基乙酸共同抑制金属-β-内酰胺酶l1 †
    摘要:由包括l1在内的金属β-内酰胺酶(mβls)引起的"超级细菌"感染已成为一种新兴威胁.为了探究巯基乙酸硫酯抑制l1是硫酯本身或其水解产物的贡献,合成了十种巯基乙酸硫酯1-10,它们特异性地抑制了l1,Ic 50值在0.17至1.2μm范围内,发现有8种是ic 50值.最佳抑制剂(ic 50 = 0.17μm).这些硫酯使头孢唑啉对表达l1的大肠杆菌的抗菌活性恢复了2-4倍.的uv-Vis监测表明,1,8和9在tris缓冲液(ph 6.0-8.5)中未水解,但被l1水解.进一步的HPLC监测表明1/3的硫酯9被转化为巯基乙酸.std-NMR监测表明,硫酯及其水解产物巯基乙酸共同抑制l1.
    DOI:10.1039/c8Md00091C

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    专利信息


    专利号:US-6787668-B2
    优先权日:2000-04-13
    标 题 :2-amino-4,5 heptenoic acid derivatives useful as nitric oxide synthase inhibitors
    发明人:PITZELE BARNETT S; SIKORSKI JAMES A; WEBBER RONALD KEITH
    权利人:PHARMACIA CORP
    摘要:The present invention is directed to a compound of formula I:or a pharmaceutically acceptable salt thereof, wherein:R1 is selected from the group consisting of H and methyl; andR2 is selected from the group consisting of H and methyl.The compounds possess useful nitric oxide synthetase inhibiting activity, and are expected to be useful in the treatment or prophylaxis of a disease or condition in which the synthesis or over synthesis of nitric oxide forms a contributory part.

    专利号:WO-2006040676-A1
    优先权日:2004-10-12
    标题 :Nitrosated benzopyran compounds as novel cyclooxygenase-2 selective inhibitors
    发明人:TJOENG FOE SIONG; CARTER JEFFERY; SPRINGER JOHN ROBERT; ZUPEC MARK E
    权利人:PHARMACIA & UPJOHN CO LLC; TJOENG FOE SIONG; CARTER JEFFERY; SPRINGER JOHN ROBERT; ZUPEC MARK E
    摘要:This invention specifically relates to novel cyclooxygenase 2 (COX-2) selective inhibitor compounds that donate, transfer or release nitric oxide, stimulate endogenous synthesis of nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase. Compounds of particular interest and their analogs defined by formula (I) wherein Z, X, R1, R2, R3, and R4 are as described in the specification. This invention also relates to pharmaceutical compositions and methods for treating COX-2 mediated disorders, such as inflammation and inflammation related disorders.

    专利号:US-2015150995-A1
    优先权日:2012-08-09
    标题:Conjugated anti-microbial compounds and conjugated anti-cancer compounds and uses thereof
    发明人:TAFT III KARL MILTON; ENGELKING JARRED ROY
    权利人:PONO CORP
    摘要:Disclosed herein are synthesis methods for generation of conjugated anti-microbial compounds and conjugated anti-cancer compounds. Several embodiments, related to the uses of such compounds in the treatment of infections, in particular those caused by drug-resistant bacteria. Some embodiments relate to targeting cancer based on the metabolic signature of tumor cells.

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    主要参考文献


    1: Gaudreau P, Lavigne GJ, Quirion R. Cholecystokinin antagonists proglumide, lorglumide and benzotript, but not L-364,718, interact with brain opioid binding sites. Neuropeptides. 1990 May;16(1):51-5.
    3: Magous R, Bali JP. Evidence that proglumide and benzotript antagonize secretagogue stimulation of isolated gastric parietal cells. Regul Pept. 1983 Nov;7(3):233-41. doi: 10.1021/ci3003655. Epub 2013 Jan 4.

    合成参考文献


    参考文献:10.1016/0006-8993(85)90764-4
    摘要:Vigna SR, Szecòwka J, Williams JA. Do antagonists of pancreatic cholecystokinin receptors interact with central nervous system cholecystokinin receptors Brain Res. 1985 Sep 23;343(2):394–7. doi: 10.1016/0006-8993(85)90764-4.
    参考文献:10.1016/s0022-3565(25)38883-x
    摘要:Crawley JN, Stivers JA, Hommer DW, Skirboll LR, Paul SM. Antagonists of central and peripheral behavioral actions of cholecystokinin octapeptide. The Journal of Pharmacology and Experimental Therapeutics. 1986 Feb;236(2):320–30. doi: 10.1016/s0022-3565(25)38883-x.
    摘要:Makovec F, Bani M, Chisté R, Revel L, Rovati LC, Rovati LA. Differentiation of central and peripheral cholecystokinin receptors by new glutaramic acid derivatives with cholecystokinin-antagonistic activity. Arzneimittelforschung. 1986;36(1):98–102.
    参考文献:10.1007/bf00504868
    摘要:Verspohl EJ, Wunderle G, Ammon HP, Williams JA, Goldfine ID. Proglumide (gastrin and cholecystokinin receptor antagonist) inhibits insulin secretion in vitro. Naunyn Schmiedebergs Arch Pharmacol. 1986 Mar;332(3):284–7. doi: 10.1007/bf00504868.
    参考文献:10.1007/bf02786123
    摘要:Akiyama T, Tachibana I, Otsuki M. Characterization of a new diphenylpyrazolidinone cholecystokinin antagonist in vitro isolated rat pancreatic acini. Journal of Gastrointestinal Cancer. 1993 Oct;14(2):167–73. doi: 10.1007/bf02786123.
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