120777-22-2Relevant academic research and scientific papers
Asymmetric biocatalytic hydrocyanation of pyrrole carboxaldehydes
Purkarthofer, Thomas,Gruber, Karl,Fechter, Martin H.,Griengl, Herfried
, p. 7661 - 7668 (2005)
The asymmetric hydrocyanation of pyrrole-2- and -3-carboxaldehydes substituted with either methyl, benzyl or phenyl in the 1-position catalyzed by the hydroxynitrile lyases from Hevea brasiliensis (HbHNL) and Prunus amygdalus (PaHNL) is reported. The products could be isolated - after O-silylation - with moderate to good enantiomeric purity although the carbonyl activity of the substrates was found to be very low, which is supported by quantum-chemical calculations. Structural effects concerning substrate size and regiochemistry are discussed considering docking calculations based on the X-ray crystal structures of the two enzymes. From these calculations one particular amino acid residue (Trp-128) in the active site of HbHNL could be identified, which plays a major role for the appropriate binding of structurally demanding carbonyl compounds.
1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding
Thurkauf,Yuan,Chen,Wasley,Meade,Woodruff,Huston,Ross
, p. 4950 - 4952 (1995)
A series of 1-phenyl-3-(aminomethyl)pyrroles were prepared in two steps from aniline and their affinities for D2, D3, and D4 dopamine receptor subtypes determined. A 15-fold selectivity for cloned human D4 recep
ANDROGEN RECEPTOR ANTAGONISTS
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Paragraph 0197-0199, (2019/08/26)
Compounds that inhibit the androgen receptor, pharmaceutical compositions comprising one or more of the compounds, as well as methods of treating cancer using such compounds are described.
Direct and efficient synthesis of pyrrole-3-carbaldehydes by Vilsmeier-Haack formylation of pyrroles with sterically crowded amides
Ilyin, Petrv.,Pankova, Alenas.,Kuznetsov, Mikhail A.
experimental part, p. 1353 - 1358 (2012/07/03)
A simple and convenient synthetic method to prepare N-substituted pyrrole-3-carbaldehydes by Vilsmeier-Haack formylation of pyrroles using sterically crowded formamides was developed. The dependence of the formylation regioselectivity on steric features of substrates and reagents is discussed. Georg Thieme Verlag Stuttgart · New York.
NOVEL ANTIMALARIA AGENT CONTAINING HETEROCYCLIC COMPOUND
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Page/Page column 81, (2008/06/13)
Disclosed is an antimalarial agent containing a compound represented by the formula: [wherein A1 represents a 3-pyridyl group that may have a substituent, a 6-quinolyl group that may have a substituent, or the like; X1 represents a group represented by the formula -C(=O)-NH- or the like; E represents a furyl group, a thienyl group or a phenyl group; with the proviso that A1 may have one to three substituents, and E has one of two substituents] or a salt thereof or hydrates thereof.
NOVEL ANTIFUNGAL AGENT COMPRISING HETEROCYCLIC COMPOUND
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Page/Page column 90, (2010/11/08)
The present invention provides an antifungal agent represented by the formula: [wherein A1 represents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; X1 represents a group represented by the formula -NH-C(=O)-, a group represented by the formula -C(=O)-NH-, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that A1 may have 1 to 3 substituents, and E has one or two substituents].
Polycyclic fused heteroring compounds metal complexes and polymerization process
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Page 14, (2010/02/10)
Metal complexes comprising a polycyclic, heteroatom containing fused ring compound comprising at least a cyclopentadienyl ring having fused thereto a 5-membered polyatomic ring containing one or more ring atoms selected from groups 15 or 16 of the Periodic Table of the Elements and lacking substituents forming 6-membered, aromatic fused rings; polymerization catalysts; and olefin polymerization processes using the same are disclosed.
N-PIPERIDINE DERIVATES AS CCR3 MODULATORS
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Page/Page column 50, (2008/06/13)
Compounds of formula I, processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dement
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480
Sbardella, Gianluca,Mai, Antonello,Artico, Marino,Loddo, Roberta,Setzu, Maria Grazia,La Colla, Paolo
, p. 1537 - 1541 (2007/10/03)
Pursuing our search program for new antitubercular drugs we decided to explore the potentiality of oxazolidinone moiety by synthesizing novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480. The new derivatives were tested against atypical mycobacteria as well as against drug resistant Mycobacterium tuberculosis and some of them exhibited a fairly good activity against Mycobacterium avium complex (MAC).
Novel HIV-1 protease inhibitors active against multiple PI-Resistant viral strains: Coadministration with indinavir
Kevin, Nancy J.,Duffy, Joseph L.,Kirk, Brian A.,Chapman, Kevin T.,Schleif, William A.,Olsen, David B.,Stahlhut, Mark,Rutkowski, Carrie A.,Kuo, Lawrence C.,Jin, Lixia,Lin, Jiunn H.,Emini, Emilio A.,Tata, James R.
, p. 4027 - 4030 (2007/10/03)
HIV-1 protease inhibitors (PI) with an N-arylpyrrole moiety in the P 3 position afforded excellent antiviral potency and substantially improved aqueous solubility over previously reported variants. The rapid in vitro clearance of these compounds in human liver microsomes prompted oral coadministration with indinavir to hinder their metabolism by the cyctochrome P450 3A4 isozyme and allow for in vivo PK assessment.
