143699-92-7Relevant academic research and scientific papers
Synthesis and biological evaluation of novel azetidine derivatives as dopamine antagonist
Metkar, Shashikant D.,Bhatia, Manish S.,Desai, Uday V.
, p. 5982 - 5989 (2013)
In this study, azetidine derivatives were evaluated for their potency as dopaminergic antagonist. The study comprised derivatives substituted in 3-position with amide moiety. Further, the phenyl moiety of amide was modified at 2, 3, or 4-position. The substituted compounds were biologically evaluated for their affinity for D2 and D4 receptors. The most potent D2 and D4 antagonist among these compounds appeared to be the N-(1-benzhydryl-azetidin-3yl)-2-bromo-benzamide and N-(1-benzhydryl-azetidin-3yl)-4-bromo-benzamide, respectively. Various docking interactions of CPPMA with the D4 receptor and the same for compound 5 i.e., N-(1-benzhydryl-azetidin-3yl)-4-bromo-benzamide were found to have good correlation with observed biological activity.
AMINO HETEROARYL COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF
-
, (2014/12/09)
The present invention refers to aminoheteroaryl compounds of the following formula (I) as well as the preparation method and use thereof, wherein R1 and R3 are defined in the Description in details. The aminoheteroaryl compounds of t
Aminoheteroaryl compounds and preparation method and use thereof
-
, (2014/12/09)
The present invention refers to aminoheteroaryl compounds of the following formula (I) as well as the preparation method and use thereof, wherein R1 and R3 are defined in the Description in details. The aminoheteroaryl compounds of t
PYRAZOLE DERIVATIVE
-
Page/Page column 67, (2008/06/13)
Not available
N-HETEROCYCLYL-SUBSTITUTED AMINO-THIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS
-
Page 41, (2010/02/08)
Aminothiazole compounds with N-containing cycloalkyl at the 2-amino position which are represented by the Formula (I), or a pharmaceutically acceptable prodrug of said compound, or pharmaceutically acceptable salt of said compound, modulate and/or inhibit the cell proliferation and activity of protein kinases.
Nicotinoyl azide (NCA)-mediated Mitsunobu reaction: An expedient one-pot transformation of alcohols into azides
Papeo, Gianluca,Posteri, Helena,Vianello, Paola,Varasi, Mario
, p. 2886 - 2892 (2007/10/03)
A practical and simple method that allows preparation of azides from alcohols is described. The process involves oxyphosphonium-type activation and it is based upon the use of nicotinoyl azide (NCA), a cheap and easily accessible azide ion source.
Bis-piperidinyl-pyrimidin-2-ones as alpha 1a adrenergic receptor antagonists
-
, (2008/06/13)
Pyrimidinone, oxazolidinone, and (alkyl)aryl derivatives, their synthesis, and their use as alpha 1a adrenergic receptor antagonists are disclosed. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are
Alpha 1a adrenergic receptor antagonists
-
, (2008/06/13)
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
7-substituted-6-fluoro-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid compounds and 7-(substituted triazolyl pyrrolidin-1-yl) 4-oxoquinoline-3-carboxylic acid derivatives useful as antibacterial agents
-
, (2008/06/13)
Substituted quinoline compounds and intermediates thereto, processes for producing those compounds and intermediates, pharmaceutical compositions using those compounds, methods for treating bacterial infections using those compounds, and methods for disin
