In the present work, we propose the synthesis of novel nicotinamide subsituted phthlocyanine photosensitizer (PS) and characterized by FTIR, UV–visible, H-NMR and MALDI Toff spectroscopy. ...Nicotinamide plays a vital rule in the central nervous system and its potential as a therapeutic for neurodegenerative disease. Nicotinamide substituted PS (
3
) efficiently produced ROS via type-1 process as measured by DCF assay. We observed that our PS after red light illumination (22 J/cm
2
) killed gram positive
S. aureus
upto 3 log reduction. Furher the addition of Potassium Iodide (100 mM) significantly potentiated PS at lower concentrations and enhanced the bacterial killing upto 6 log reduction against the
S. aureus
. We further found that the synergistic effect of PS and KI also eradicated the gram negative
E. coli
strain at lower concentraion of PS and found to killed
E. coli
upto 5 log reduction under the red light illumination at 22 J/cm
2
of light dose. The conjugation of such biologically important form of vitamin B
3
with PS would be a great addition and could pav the way for the novel photodynamic agent in the treatement of cancer and infectious diseases.
Graphic abstract
A new symmetrical Nicotinamide tetrasubstituted zinc phthalocyanine (
3
) was synthesized. Upon addition of potassium Iodide with PS, the PS exhibited significant photodynamic activity with 5-6 logs reduction in bacterial load was achieved.
Unlike the comprehensive development of tandem multi‐metallic catalysis, bimetallic synergistic catalysis has been challenging to achieve high stereoselectivity with the generation of ...multi‐stereogenic centers. Herein, an efficient synergistic catalysis for the diastereo‐ and enantioselective synthesis of multi‐substituted tetrahydrofuran derivatives has been developed. Under mild reaction conditions, a series of target molecules with three consecutive stereocenters were synthesized by a palladium(0)/rhodium(III) bimetal‐catalyzed asymmetric decarboxylative 3+2‐cycloaddition of vinylethylene carbonates with α,β‐unsaturated carbonyl compounds. The corresponding adducts were obtained with moderate to high yields (67 %∼98 %) and excellent stereoselectivities (>20 : 1 d.r., up to 99 % ee).
Multimetallic cooperative catalysis represents one of the most efficient method for asymmetric C−C and C‐heteroatom bond forming transformations. An enantioselective 3+2 cycloaddition reaction catalyzed synergistically by the combination of an achiral palladium catalyst and a chiral‐at‐metal rhodium(III) complex has been developed, generating a series of 1,2,3,3‐tetrasubstituted tetrahydrofurans in high yields and stereoselectivities (>20 : 1 d.r., up to 99 % ee).
Chiral‐at‐metal RhIII complexes catalyze the efficient enantioselective Mannich reaction of 2‐acyl imidazoles with 1,3,5‐triazinanes, affording the corresponding adducts in 81–99 % yield with up to ...>99 % enantioselectivity. This protocol performs with 0.1 mol‐% of RhIII complex on gram scale without any loss in enantioselectivity.
An efficient enantioselective Mannich reaction of 2‐acyl imidazoles with 1,3,5‐triazinanes catalyzed by chiral‐at‐metal RhIII complexes has been developed, affording the corresponding adducts in good yields with excellent enantioselectivities.
A synergistic catalysis combination of chiral‐at‐metal rhodium complex and amine catalyst was developed for enantioselective alkylation of aldehydes with α,β‐unsaturated 2‐acyl imidazoles. The ...corresponding adducts were obtained in good yields with excellent enantioselectivities (up to 99% ee).
Enantioselective alkylation of aldehydes with α,β‐unsaturated 2‐acyl imidazoles was achieved by synergistic catalysis combination of chiral‐at‐metal rhodium complex and a chiral amine catalyst. The alkylated aldehydes were obtained in good yields with excellent enantioselectivity (up to 99% ee). Chiral‐at‐metal rhodium complex was found to be a predominant catalyst in controlling stereochemistry of this transformation.
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•New thiazole derivatives were synthesized via “one pot” multicomponent reaction.•Synthetic compounds are hybrid of carbohydrazide and thiazole scaffolds.•Compounds demonstrated ...α-glucosidase inhibitory properties.•Molecular docking studies were carried out.•Compounds may serve as leads for future research.
Current study based on the synthesis of new thiazole derivatives via “one pot” multicomponent reaction, evaluation of their in vitro α-glucosidase inhibitory activities, and in silico studies. All synthetic compounds were fully characterized by 1H NMR, 13C NMR and EIMS. CHN analysis was also performed. These newly synthesized compounds showed activities in the range of IC50=9.06±0.10–82.50±1.70μM as compared to standard acarbose (IC50=38.25±0.12μM). It is worth mentioning that most of the compounds such as 1 (IC50=23.60±0.39μM), 2 (IC50=22.70±0.60μM), 3 (IC50=22.40±0.32μM), 4 (IC50=26.5±0.40μM), 6 (IC50=34.60±0.60μM), 7 (IC50=26.20±0.43μM), 8 (IC50=14.06±0.18μM), 9 (IC50=17.60±0.28μM), 10 (IC50=27.16±0.41μM), 11 (IC50=19.16±0.19μM), 12 (IC50=9.06±0.10μM), 13 (IC50=12.80±0.21μM), 14 (IC50=11.94±0.18μM), 15 (IC50=16.90±0.20μM), 16 (IC50=12.60±0.14μM), 17 (IC50=16.30±0.29μM), and 18 (IC50=32.60±0.61μM) exhibited potent inhibitory potential. Molecular docking study was performed in order to understand the molecular interactions between the molecule and enzyme. Newly identified α-glucosidase inhibitors except few were found to be completely non-toxic.
A synergistic catalysis combination of chiral-at-metal rhodium complex and amine catalyst was developed for enantioselective alkylation of aldehydes with alpha,beta-unsaturated 2-acyl imidazoles. The ...corresponding adducts were obtained in good yields with excellent enantioselectivities (up to 99% ee).
A synergistic catalysis combination of chiral-at-metal rhodium complex and amine catalyst was developed for enantioselective alkylation of aldehydes with α,β-unsaturated 2-acyl imidazoles. The ...corresponding adducts were obtained in good yields with excellent enantioselectivities （up to 99% ee）.
