32570-19-7Relevant articles and documents
META SUBSTITUTED PHENYLPYRAZOLO- AND PHENYLPYRROLO- PYRIDAZINE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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Page/Page column 200, (2018/06/22)
The present invention relates to meta substituted phenylpyrazolo-and phenylpyrrolo-pyridazine derivatives of formula (I) having dual pharmacological activity towards both the a28 subunit, in particular the a28-l subunit, of the voltage-gated calcium channel and the NET receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
Design and development of pyrrole carbaldehyde: An effective pharmacophore for enoyl-ACP reductase
Joshi, Shrinivas D.,Kumar, Devendra,More, Uttam A.,Yang, Kap Seung,Aminabhavi, Tejraj M.
, p. 672 - 689 (2016/03/08)
Enoyl-ACP reductase is the key enzyme involved in FAS-II synthesis of mycolic acid in bacterial cell wall and is a promising target for discovering new chemical entity. The designed pharmacophores are the possible better tools to combat mutation in enoyl-ACP enzyme, which leads to a decrease in volume of triclosan binding site. Compound 3a showed H-bonding interactions similar to that of triclosan with enoyl-ACP enzyme and with a better docking score (C score 8.81), while the compound 3f showed additional interaction with MET98.H amino acid residue. The 3D-QSAR computations also support the docking study to develop novel pyrrole-based derivatives. Graphical abstract: Molecular docking 3D-QSAR studies and synthesis of active analogs of pyrrole carbaldehyde as better receptor fit pharmacophore for enoyl-ACP reductase along with in vitro antitubercular activity. (Figure Presented).
Cyclodextrin-based PNN supramolecular assemblies: a new class of pincer-type ligands for aqueous organometallic catalysis
Menuel,Bertaut,Monflier,Hapiot
, p. 13504 - 13512 (2015/08/03)
Water-soluble cyclodextrins (CDs) bearing two nitrogen atoms as metal coordinating sites have been synthesized. An appropriate phosphane could be included within their cavity through the primary face to form self-assembled PNN supramolecular edifices. Once the PNN ligands were coordinated to platinum, the resulting complexes proved to be very effective as catalysts in a domino reaction, where a Pt-catalyzed reduction of nitrobenzene was followed by a Paal-Knorr pyrrole reaction. In the nitrobenzene reduction, the modified CDs acted both as first- and second-sphere ligands. Contrary to an acyclic glucopyranose-based NN ligand unable to interact with a phosphane ligand, the CD-based PNN ligands stabilized the catalytic species in water by supramolecular means. Interestingly, the product and the water-soluble Pt-catalyst could be recovered in two different phases once the reaction was complete.
PHOSPHORUS COMPOUND AND TRANSITION METAL COMPLEX OF THE SAME
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Paragraph 0101-0104, (2015/11/10)
The present invention provides a compound represented by general formula (1) and a transition metal complex containing the compound as a ligand: wherein R1 to R10, N, P, Y, and Z have the meanings as defined in DESCRIPTION.
An efficient synthesis of N-substituted pyrroles catalyzed by MgI2 etherate
Zhang, Yongdong,Weng, Guodong,Chen, Jingyan,Ma, Danting,Zhang, Xingxian
, p. 131 - 135 (2015/02/19)
We describe a convenient and useful procedure for the synthesis of various 2,5-dimethyl-N-substituted pyrrole derivatives by the addition of 2,5-hexadione with aromatic amines, heteroaromatic amines and aliphatic amines catalyzed by MgI2 etherate (MgI2·(OEt2)n) in good to excellent yields.
Indium-mediated one-pot pyrrole synthesis from nitrobenzenes and 1,4-diketones
Lee, Hyunseung,Kim, Byeong Hyo
, p. 6698 - 6708 (2013/07/26)
One-pot reduction-triggered heterocyclizations of nitrobenzene derivatives with 1,4-diketones were investigated. In the presence of indium/AcOH in toluene at 80 C, reaction of nitrobenzenes with 2,5-hexadione produced moderate to excellent yields (40-98%)
Discovery and structure-activity relationships of pyrrolone antimalarials
Murugesan, Dinakaran,Mital, Alka,Kaiser, Marcel,Shackleford, David M.,Morizzi, Julia,Katneni, Kasiram,Campbell, Michael,Hudson, Alan,Charman, Susan A.,Yeates, Clive,Gilbert, Ian H.
supporting information, p. 2975 - 2990 (2013/05/23)
In the pursuit of new antimalarial leads, a phenotypic screening of various commercially sourced compound libraries was undertaken by the World Health Organisation Programme for Research and Training in Tropical Diseases (WHO-TDR). We report here the detailed characterization of one of the hits from this process, TDR32750 (8a), which showed potent activity against Plasmodium falciparum K1 (EC50 ～ 9 nM), good selectivity (>2000-fold) compared to a mammalian cell line (L6), and significant activity against a rodent model of malaria when administered intraperitoneally. Structure-activity relationship studies have indicated ways in which the molecule could be optimized. This compound represents an exciting start point for a drug discovery program for the development of a novel antimalarial.
2,5-dimethylpyrrole protection facilitates copper(I)-mediated methoxylations of aryl iodides in the presence of anilines
Ragan, John A.,Makowski, Teresa W.,Castaldi, Michael J.,Hill, Paul D.
, p. 1599 - 1603 (2007/10/03)
Converting iodoanilines to the corresponding 2,5-dimethylpyrroles was found to facilitate CuCI-mediated methoxide substitution. Examples with ortho-, meta-, or para-relationships between the iodide and aniline are presented. Several other aniline blocking groups were investigated and found not to be successful in this sequence.
