3722-80-3Relevant articles and documents
Green synthesis of novel bis(hexahydro-1H-xanthene-1,8(2H)-diones) employing p-toluenesulfonic acid (p-TSA) as a solid acid catalyst
Darweesh, Ahmed F.,Salama, Soad K.,Abdelhamid, Ismail A.,Elwahy, Ahmed H. M.
, p. 471 - 484 (2020/10/30)
Green synthesis of novel bis(hexahydro-1H-xanthene-1,8(2H)-diones) which are linked to aliphatic or aromatic spacers via ether or ester linkages were performed in good to excellent yields by the reaction of 5,5-dimethyl-1,3-cyclohexanedione with the appropriate bis-aldehydes using p-TSA as an organic acid solid catalyst. The reaction of the bis-aldehydes with barbituric acid or 1,3-dimethylbarbituric acid instead of 5,5-dimethyl-1,3-cyclohexanedione afforded the corresponding Knoevenagel condensation adducts in good yield.
BIVALENT LECA INHIBITORS TARGETING BIOFILM FORMATION OF PSEUDOMONAS AERUGINOSA
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Page/Page column 31-32; 42, (2021/05/15)
The present invention relates to divalent compounds binding to LecA. The compounds are useful to block biofilm formation of Pseudomonas aeruginosa. The invention further relates to pharmaceutical compositions comprising these compounds and to therapeutic methods and uses of these compounds, in particular to therapeutic methods and uses for the treatment of Pseudomonas aeruginosa infections in a subject. The invention also relates to imaging of infections, such as biofilms produced by Pseudomonas aeruginosa, by using these divalent compounds.
Lewis acid catalyzed reactivity switch: Pseudo three-component annulation of nitrosoarenes and (epoxy)styrenes
Purkait, Anisha,Saha, Subhajit,Ghosh, Santanu,Jana, Chandan K.
supporting information, p. 15032 - 15035 (2020/12/22)
A Lewis acid catalyzed annulation reaction via arene functionalization of nitrosoarenes and C-C cleavage of (epoxy)styrene to provide arylquinolines is reported. The Lewis acid catalyst altered the annulation pattern providing arylquinolines instead of oxazolidines. The reaction with styrene resulted in a mixture of 2,4-diarylquinoline and 4-Arylquinoline, while only 3-Arylquinoline was formed from the reaction of epoxystyrene. This journal is
Novel 2-cyanoacrylamido-4,5,6,7-tetrahydrobenzo[b]thiophene derivatives as potent anticancer agents
Sroor, Farid M.,Aboelenin, Mohamad M.,Mahrous, Karima F.,Mahmoud, Khaled,Elwahy, Ahmed H. M.,Abdelhamid, Ismail A.
, (2020/07/15)
Ethyl 2-acrylamido-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylate as well as its corresponding bis-derivatives, 5–10, with aliphatic linkers were synthesized, fully characterized, and tested as novel anticancer agents. The targeted compounds, 5–10, wer
Polyethylene glycol-bonded triethylammonium l-prolinate: A new biodegradable amino-acid-based ionic liquid for the one-pot synthesis of bis(pyrazolyl)methanes as DNA binding agents
Kordnezhadian, Reza,Shekouhy, Mohsen,Karimian, Somaye,Tavaf, Zohreh,Malek-Hosseini, Saeed,Shahsavani, Mohammad Bagher,Amirghofran, Zahra,Yousefi, Reza,Khalafi-Nezhad, Ali
, p. 16995 - 17012 (2020/11/02)
Polyethylene glycol-bonded triethylammonium l-prolinate ([PEG-TEA]LP) was prepared as a new, highly efficient, reusable and biodegradable amino-acid-based ionic liquid catalyst using cheap and easily accessible starting materials. The [PEG-TEA]LP chemical
A rapid synthesis of low-nanomolar divalent LecA inhibitors in four linear steps from d-galactose pentaacetate
Hirsch, Anna K. H.,Imberty, Anne,Kinsinger, Thorsten,Kuhaudomlarp, Sakonwan,Lepsik, Martin,Minervini, Saverio,Titz, Alexander,Yousaf, Sultaan,Zahorska, Eva
, p. 8822 - 8825 (2020/08/17)
Chronic infections with Pseudomonas aeruginosa are associated with the formation of bacterial biofilms. The tetrameric P. aeruginosa lectin LecA is a virulence factor and an anti-biofilm drug target. Increasing the overall binding affinity by multivalent
Prospective new amidinothiazoles as leukotriene B4 inhibitors
Aly, Ashraf A.,Ibrahim, Mahmoud A.A.,El-Sheref, Essmat M.,Hassan, Alaa M.A.,Brown, Alan B.
, p. 414 - 427 (2018/09/18)
An efficient and one-step synthesis of the versatile, hitherto new derivatives resembling LY293111, a prospective potent antagonist of the leukotriene B4 (LTB4) receptor, were reported. The strategy was based on the synthesis of an amidinothiazole ring, c
Governing the DNA-binding mode of styryl dyes by the length of their alkyl substituents-from intercalation to major groove binding
Berdnikova, Daria V.,Sosnin, Nikolai I.,Fedorova, Olga A.,Ihmels, Heiko
, p. 545 - 554 (2018/02/07)
A series of monomeric and homodimeric 4-alkoxystyryl(pyridinium) dyes was synthesized and their DNA-binding properties were investigated. We found that the length of the alkyl substituent has a crucial influence on the binding mode of the dyes, although t
Hybrid Inhibitors of Malarial Dihydrofolate Reductase with Dual Binding Modes That Can Forestall Resistance
Tarnchompoo, Bongkoch,Chitnumsub, Penchit,Jaruwat, Aritsara,Shaw, Philip J.,Vanichtanankul, Jarunee,Poen, Sinothai,Rattanajak, Roonglawan,Wongsombat, Chayaphat,Tonsomboon, Aunchalee,Decharuangsilp, Sasithorn,Anukunwithaya, Tosapol,Arwon, Uthai,Kamchonwongpaisan, Sumalee,Yuthavong, Yongyuth
supporting information, p. 1235 - 1240 (2019/01/04)
The S108N mutation of dihydrofolate reductase (DHFR) renders Plasmodium falciparum malaria parasites resistant to pyrimethamine through steric clash with the rigid side chain of the inhibitor. Inhibitors with flexible side chains can avoid this clash and
Biological activities and docking studies on novel bis 1,4-DHPS linked to arene core via ether or ester linkage
Ibrahim, Nada S.,Mohamed, Magda F.,Elwahy, Ahmed H. M.,Abdelhamid, Ismail A.
, p. 1036 - 1045 (2018/09/29)
Background: Novel bis(1,4-dihydropyridine) derivatives linked to arene core via ester 5-7 as well as ether linkages 10-12 were prepared, and their structures were confirmed by several spectral tools. They were evaluated as anticancer agents on A549 and MC
