Journal ArticleDOI
β-Lactam-Synthon-Interceded, Facile, One-Pot, Diastereoselective Synthesis of Functionalized Tetra/Octahydroisoquinolone Derivatives
Raghu Raj,Vishu Mehra,Pardeep Singh,Vipan Kumar,Gaurav Bhargava,Mohinder P. Mahajan,Sachin Handa,LeGrande M. Slaughter +7 more
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TLDR
In this article, a single-pot synthesis of tetra/octahydro-4H-isoquinoline-1,3-diones was developed and validated by using inter/intramolecular amidolysis of racemic N-aryl-β-lactams followed by intramerolecular iodocyclization protocols.About:
This article is published in European Journal of Organic Chemistry.The article was published on 2011-05-01. It has received 27 citations till now. The article focuses on the topics: Synthon & Intramolecular reaction.read more
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1,2,3-Triazole tethered β-lactam-chalcone bifunctional hybrids: synthesis and anticancer evaluation.
Pardeep Singh,Raghu Raj,Vipan Kumar,Mohinder P. Mahajan,Preet Ms Bedi,Tandeep Kaur,Ajit Kumar Saxena +6 more
TL;DR: The synthesis of novel 1,2,3-triazole tethered β-lactam-chalcone bifunctional hybrids via click chemistry approach utilizing azide-alkyne cycloaddition reactions and their evaluation as anticancer agents against four human cancer cell lines are described.
Journal ArticleDOI
Synthesis, docking and in vitro antimalarial evaluation of bifunctional hybrids derived from β-lactams and 7-chloroquinoline using click chemistry
Pardeep Singh,Parvesh Singh,Malkeet Kumar,Jiri Gut,Philip J. Rosenthal,Kewal Kumar,Vipan Kumar,Mohinder P. Mahajan,Krishna Bisetty +8 more
TL;DR: 1,2,3-Triazole tethered β-lactam and 7-chloroquinoline bifunctional hybrids were synthesized and evaluated as potential antimalarial agents and observed activity profiles were substantiated by docking studies via inhibition of P. falciparum dihydrofolate reductase (PfDHFR), a potential target for the development of new anti-malarials.
Journal ArticleDOI
Azide-alkyne cycloaddition en route to novel 1H-1,2,3-triazole tethered isatin conjugates with in vitro cytotoxic evaluation.
Pardeep Singh,Pooja Sharma,Amit Anand,Preet Mohinder Singh Bedi,Tandeep Kaur,Archna Saxena,Vipan Kumar +6 more
TL;DR: 1H-1,2,3-triazole tethered isatin conjugates synthesized and evaluated for cytotoxicity on four human cancer cell lines proved to be twice as potent as 5-fluorouracil on THP-1 cell line with 5a and 5c being most active exhibiting IC(50) values of <1 against all cell lines except Caco-2.
Journal ArticleDOI
Recent advances in synthetic facets of immensely reactive azetidines
TL;DR: Azetidines also possess important prospects in other settings such as catalytic processes including Henry, Suzuki, Sonogashira, and Michael additions as mentioned in this paper and represent an important class of strained compounds making them excellent candidates for ring-opening and expansion reactions.
Journal ArticleDOI
β-Lactam-synthon-interceded diastereoselective synthesis of novel thioxo-imidazolines: a convenient access to functionally decorated 4,5-dihydro-imidazoles
TL;DR: In this article, a facile synthesis of an equimolar diastereomeric mixture of 2-thioxo-imidazolines via β-lactam synthon approach using racemic N-aryl β-Lactams was described.
References
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Journal ArticleDOI
Novel 5-HT3 antagonists. Isoquinolinones and 3-aryl-2-pyridones
Matsui T,Sugiura T,Hisao Nakai,Iguchi S,Shigeoka S,Takada H,Yoshihiko Odagaki,Nagao Y,Ushio Y,Kazuyuki Ohmoto +9 more
TL;DR: Synthesis and pharmacological evaluation of a series of 1,2-dihydro-1-[(5-methyl-1-imidazol-4-yl)methyl]-2-oxopyridine 5-HT3 antagonists and structure-activity relationships are discussed.
Journal ArticleDOI
Synthesis and neurotoxicity of tetrahydroisoquinoline derivatives for studying Parkinson's disease.
TL;DR: The modified Pummerer reaction provided a convenient and efficient method for synthesizing various TIQs and one TIQ derivative has been shown to prevent MPTP, TIQ, and 1-benzyl-TIQ induced behavioral abnormalities.
Journal ArticleDOI
The mechanism of 1,2,3,4-tetrahydroisoquinolines neuroprotection: the importance of free radicals scavenging properties and inhibition of glutamate-induced excitotoxicity.
Lucyna Antkiewicz-Michaluk,Jerzy W. Lazarewicz,Antoni Patsenka,Małgorzata Kajta,Elzbieta Zieminska,Elzbieta Salinska,A. Wasik,Krystyna Gołembiowska,Jerzy Vetulani +8 more
TL;DR: The results indicate that 1MeTIQ, in contrast to TIQ, offers a unique and complex mechanism of neuroprotection in which antagonism to the glutamatergic system may play a very important role and suggest the potential of 1Me TIQ as a therapeutic agent in various neurodegenarative illnesses of the central nervous system.
Journal ArticleDOI
Effect of acute and chronic administration of 1,2,3,4-tetrahydroisoquinoline on muscle tone, metabolism of dopamine in the striatum and tyrosine hydroxylase immunocytochemistry in the substantia nigra, in rats.
Elżbieta Lorenc-Koci,M. ŚmiaŁowska,Lucyna Antkiewicz-Michaluk,K. GoŁembiowska,M. Bajkowska,Stanisław Wolfarth +5 more
TL;DR: The results suggest that 1,2,3,4-tetrahydroisoquinoline may be one of the endogenous substances involved in the progress of Parkinson's disease.
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