103301-78-6Relevant articles and documents
Design and synthesis of novel antihypertensive drugs
Moutevelis-Minakakis,Gianni,Stougiannou,Zoumpoulakis,Zoga,Vlahakos,Iliodromitis,Mavromoustakos
, p. 1737 - 1740 (2003)
AT1 antagonists constitute a new generation of drugs for the treatment of hypertension and are designed and synthesized to mimic the C-terminal segment of Angiotensin II (Ang II) and to block its binding action on AT1 receptor. For this reason, the conformational analysis of Ang II and its derivatives as well as the AT1 antagonists belonging to SARTANs class of molecules were studied. Such studies offer the possibility to reveal the stereoelectronic factors responsible for bioactivity of AT1 antagonists and to design and synthesize new analogues with better pharmacological and financial profiles. An example of a novel synthetic non-peptide molecule is given which mimics the His6-Pro7-Phe8 part of Ang II and is based on the (S)-pyroglutamic acid.
Diastereoselective alkylation of 1-benzyl-(5S)-substituted 2-pyrrolidinones
Brena-Valle, Leonardo J.,Sanchez, Rodolfo Carreon,Cruz-Almanza, Raymundo
, p. 1019 - 1026 (1996)
The (S)-glutamic acid derivatives, (5S)-methoxymethyl- and (5S)-benzyloxymethyl N-benzyl-2-pyrrolidinones, compounds 3a and 3b respectively, exhibit good to excellent diastereoselection upon alkylation with primary alkyl bromides or iodides.
Synthesis and evaluation of dual antiplatelet activity of bispidine derivatives of N-substituted pyroglutamic acids
Misra, Ankita,Anil Kumar,Jain, Manish,Bajaj, Kirti,Shandilya, Shyamali,Srivastava, Smriti,Shukla, Pankaj,Barthwal, Manoj K.,Dikshit, Madhu,Dikshit, Dinesh K.
, p. 1 - 12 (2016/01/29)
N-aralkylpyroglutamides of substituted bispidine were prepared and evaluated for their ability to inhibit collagen induced platelet aggregation, both in vivo and in vitro. Some compounds showed high anti-platelet efficacy (in vitro) of which six inhibited
3,7-DIAZABICYCLO[3.3.1 ]NONANE CARBOXAMIDES AS ANTITHROMBOTIC AGENTS
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Page/Page column 14; 15, (2015/04/15)
The present invention relates to the 3,7-diazabicyclo[3.3.1]nonane carboxamides and process for preparation thereof. The present invention further relates to the compounds of general formula (1) possessing anti-thrombotic (anti-platelet) activities. The invention also relates to use of these moieties as inhibitors of collagen induced platelet adhesion and aggregation mediated through collagen receptors both in vitro and in vivo. Further, invention also relates these class of compounds exhibiting anti-platelet efficacy through dual mechanism inhibited both collagen as well as U46619 (thromboxane receptor agonist) induced platelet aggregation. General formula (1) Wherein, R' is; wherein R is selected from alkyl, acyl, tosyl, tert-butyloxycarbonyl, araalkyl or substituted araalkyl groups; R'' is selected preferably from halogen, cyano, lower alkyl, aryl, substituted aryl, and tosyl groups; R1 is selected from hydrogen and lower alkyl groups; R2 is selected from lower alkyl and aryl groups; R3 is selected from tert-butyloxycarbonyl and bezyloxycarbonyl groups; n = 0,1.
