ChemInform Abstract: Polycyclic N-Heterocyclic Compounds. Part 80. Synthesis and Evaluation of Effects on in vitro Pentosidine Formation of 5,6-Dihydro[1]benzothieno[3′,2′:2,3]thiepino[4,5-d]pyrimidine and Related Compounds.

ChemInform ◽  
2014 ◽  
Vol 46 (3) ◽  
pp. no-no
Author(s):  
Kensuke Okuda ◽  
Yutaka Itsuji ◽  
Takashi Hirota ◽  
Kenji Sasaki
Keyword(s):  
Heterocyclic Compounds ◽  
Related Compounds

scholarly journals Green Synthesis andIn VitroBiological Evaluation of Heteroaryl Chalcones and Pyrazolines of Medicinal Interest

2013 ◽  
Vol 2013 ◽  
pp. 1-4 ◽  
Author(s):  
Vishal Banewar
Keyword(s):  
Green Synthesis ◽  
Elemental Analysis ◽  
Broad Spectrum ◽  
Spectroscopic Data ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Active Compounds

Pyrazolines are well known and important nitrogen containing 5-membered heterocyclic compounds. In the present investigation, a series of various heteroaryl chalcones and pyrazolines were synthesized by condensing formylquinolines with diverse ketones. The newly synthesized 2-pyrazolines were characterized on the basis of elemental analysis and spectroscopic data. All of the newly synthesized target compounds were selected by the NCI forin vitrobiological evaluation. These active compounds exhibited broad spectrum of various biological activities. Most of the compounds showed potent activity.

scholarly journals In vitro actions of NN-dimethyl-2-aminoindane and related compounds

1980 ◽  
Vol 32 (1) ◽  
pp. 751-756
Author(s):  
HILARY J. LITTLE ◽  
J. M. H. REES
Keyword(s):  
Related Compounds

Synthesis of biologically active heterocyclic compounds from allenic and acetylenic nitriles and related compounds

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Marthe Carine Djuidje Fotsing ◽  
Dieudonné Njamen ◽  
Zacharias Tanee Fomum ◽  
Derek Tantoh Ndinteh
Keyword(s):  
Michael Addition ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Biologically Active ◽  
Polycyclic Compounds ◽  
One Step ◽  
Pharmaceutical Properties ◽  
Related Compounds ◽  
Acetylenic Acids ◽  
The Michael Addition

Abstract Cyclic and polycyclic compounds containing moieties such as imidazole, pyrazole, isoxazole, thiazoline, oxazine, indole, benzothiazole and benzoxazole benzimidazole are prized molecules because of the various pharmaceutical properties that they display. This led Prof. Landor and co-workers to engage in the synthesis of several of them such as alkylimidazolenes, oxazolines, thiazolines, pyrimidopyrimidines, pyridylpyrazoles, benzoxazines, quinolines, pyrimidobenzimidazoles and pyrimidobenzothiazolones. This review covers the synthesis of biologically active heterocyclic compounds by the Michael addition and the double Michael addition of various amines and diamines on allenic nitriles, acetylenic nitriles, hydroxyacetylenic nitriles, acetylenic acids and acetylenic aldehydes. The heterocycles were obtained in one step reaction and in most cases, did not give side products. A brief discussion on the biological activities of some heterocycles is also provided.

scholarly journals Synthesis and Acivity of Chiral Amino Alcohols and Amides as New Cholinesterase Inhibitors for Alzheimer's Disease

2021 ◽  
Author(s):  
Safak OZHAN KOCAKAYA ◽  
Ismail Yener ◽  
Abdulselam Ertaş ◽  
Mehmet Karakaplan
Keyword(s):  
Drug Candidate ◽  
Molecular Dynamics Calculations ◽  
The Right ◽  
Potential Inhibitors ◽  
Novel Drug ◽  
Related Compounds ◽  
Candidate Molecule ◽  
Score Evaluation ◽  
Novel Products

Abstract A series of biological active compounds 1–14 have been synthesized and used as potential inhibitors for AChE and BuChE. Potential inhibitor efficacy of these molecules to the target enzymes have been searched in vitro and theoretical by dock and molecular dynamic calculations. The results show that chiral amino alcohol compounds 6, 7 and 9 exhibited good value for medication scores. Among the tested compounds the best inhibition activities have been obtained with compounds 6 for AChE and BuChE by 87.68 and 92.46 % values, respectively at 50µg/mL concentration. The anticipated value of 6 also justified superb correlation with invitro statistics and it could be taken into consideration as drug candidate molecule for designing of novel drug. Potential inhibitory outcomes of those molecules on the right track proteins were investigated the use of Docking and Molecular Dynamics calculations. Dock score evaluation and Lipinski parameters have been proven those ligands are ability inhibitors against applicable enzymes. Our findings endorse that related compounds can be applied as a capacity supply of anti-alzheimer active molecules for designing novel products.

scholarly journals In Vitro Leishmanicidal Activity of Benzophenanthridine Alkaloids from Bocconia pearcei and Related Compounds

2010 ◽  
Vol 58 (8) ◽  
pp. 1047-1050 ◽  
Author(s):  
Hiroyuki Fuchino ◽  
Marii Kawano ◽  
Kanami Mori-Yasumoto ◽  
Setsuko Sekita ◽  
Motoyoshi Satake ◽  
...  
Keyword(s):  
Benzophenanthridine Alkaloids ◽  
Leishmanicidal Activity ◽  
Related Compounds

scholarly journals Evidence that the metabolite repair enzyme NAD(P)HX epimerase has a moonlighting function

2018 ◽  
Vol 38 (3) ◽  
Author(s):  
Thomas D. Niehaus ◽  
Mona Elbadawi-Sidhu ◽  
Lili Huang ◽  
Laurence Prunetti ◽  
Jesse F. Gregory ◽  
...  
Keyword(s):  
Vitamin B6 ◽  
Weakly Bound ◽  
E Coli ◽  
Essentially Normal ◽  
Metabolite Repair ◽  
Mutant Cells ◽  
Dehydratase Activity ◽  
Related Compounds

NAD(P)H-hydrate epimerase (EC 5.1.99.6) is known to help repair NAD(P)H hydrates (NAD(P)HX), which are damage products existing as R and S epimers. The S epimer is reconverted to NAD(P)H by a dehydratase; the epimerase facilitates epimer interconversion. Epimerase deficiency in humans causes a lethal disorder attributed to NADHX accumulation. However, bioinformatic evidence suggest caution about this attribution by predicting that the epimerase has a second function connected to vitamin B6 (pyridoxal 5′-phosphate and related compounds). Specifically, (i) the epimerase is fused to a B6 salvage enzyme in plants, (ii) epimerase genes cluster on the chromosome with B6-related genes in bacteria, and (iii) epimerase and B6-related genes are coexpressed in yeast and Arabidopsis. The predicted second function was explored in Escherichia coli, whose epimerase and dehydratase are fused and encoded by yjeF. The putative NAD(P)HX epimerase active site has a conserved lysine residue (K192 in E. coli YjeF). Changing this residue to alanine cut in vitro epimerase activity by ≥95% but did not affect dehydratase activity. Mutant cells carrying the K192A mutation had essentially normal NAD(P)HX dehydratase activity and NAD(P)HX levels, showing that the mutation had little impact on NAD(P)HX repair in vivo. However, these cells showed metabolome changes, particularly in amino acids, which exceeded those in cells lacking the entire yjeF gene. The K192A mutant cells also had reduced levels of ‘free’ (i.e. weakly bound or unbound) pyridoxal 5'-phosphate. These results provide circumstantial evidence that the epimerase has a metabolic function beyond NAD(P)HX repair and that this function involves vitamin B6.

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