Showing papers by "Arun Kumar Sinha published in 2022"
TL;DR: This review summarizes the developmental process, synthesis and structure activity relationship (SAR) around arylthioindole/indolylaryl sulfone scaffolds for antiviral/anti-HIV non-nucleoside reverse transcriptase inhibitor (NNRTIs) activities and offers perspective for further development of 3-indolyLarylsulfones as an anti-viral agent including their potential against novel COVID-19 infection.
4 citations
TL;DR: In this paper , neutral ionic liquid (NIL) was used for Friedel-Crafts-type reaction of (het)arenes with carbonyls using NIL method enabled to afford a densely functionalized bis(indolyl)methanes in good to excellent yields.
3 citations
TL;DR: In this article , a series of chalcone derivatives were synthesized and investigated against the chloroquine-sensitive P. falciparum 3D7 (Pf3D7) strain and chloroquINE-resistant P. k1 strain to establish their structure-activity relationship.
Abstract: A series of novel chalcone derivatives were synthesized and investigated against the chloroquine-sensitive P. falciparum 3D7 (Pf3D7) strain and chloroquine-resistant P. falciparum K1 strain to establish their structure-activity relationship. In this study, compound 7 was found most active as well as less cytotoxic (IC50 = 4.12 µM and 3.14 µM for Pf3D7 and PfK1 respectively; CC50 = 46.18 µM). Compound 7 was studied for effect on parasite growth and the microscopic examination showed excessive DNA damage in the trophozoite stage. The parasite recovery after drug removal was poor due to the dramatic genotoxic effect of compound 7. It suggested that 7-chloro quinoline and triazole linkage were crucial for antimalarial potential. Graphical abstract
2 citations
TL;DR: In this paper , a multicomponent 5-stage reaction in one pot was proposed by combining two known name reactions viz. Gould-Jacobs reaction and Heck reaction for the synthesis of stilbene/biaryl-quinolone hybrid molecules from readily available 4-iodoaniline, (diethyl-2-(ethoxymethylene)malonate) EMME and styrene/aryl boronic acid.
1 citations
TL;DR: In this paper , a successful attempt is made to develop a one-pot protocol for the synthesis of 2-hydroxystilbene derivatives via hydrolysis of natural coumarins followed by in situ decarboxylative Heck coupling with haloarenes.
Abstract: 2-Hydroxystyrylbenzene scaffold is found in various compounds that are widely applicable in medicinal chemistry as well as material chemistry. Here, a successful attempt is made to develop a one-pot protocol for the synthesis of 2-hydroxystilbene derivatives via hydrolysis of natural coumarins followed by in situ decarboxylative Heck coupling with haloarenes. Fine tuning of the reaction conditions allowed exclusive formation of 2-hydroxystyrylbenzenes over other possible side products i.e. benzofuran/substituted coumarins.
1 citations
TL;DR: In this article , a biocatalytic divergent approach of therapeutically important five-membered benzazole heterocyclic compounds such as benzothiazoles and benzimidazoles has been described wherein Bovine serum albumin (BSA) and water play cooperative role for oxidative cyclo-condensation reaction between 2-mercapto/amino anilines and aromatic aldehydes under air at room temperature.
1 citations
01 Jan 2022
TL;DR: These reactions have emerged as a powerful and widely used strategy for the generation of carbon–sulfur bonds due to several associated benefits including versatile synthetic procedures, wide functional-group tolerance, high atom economy with few to no byproducts, and simple purification.
Abstract: The clickable addition reaction between thiols and unsaturated compounds leading to the generation of (branched/linear) thioethers or (branched/linear) vinyl sulfides is known as the hydrothiolation reaction. Based upon the nature of unsaturation, i.e. double bond or triple bond, hydrothiolation reactions are classified as thiol–ene and thiol–yne click reactions, respectively. These reactions have emerged as a powerful and widely used strategy for the generation of carbon–sulfur bonds due to several associated benefits including versatile synthetic procedures, wide functional-group tolerance, high atom economy with few to no byproducts, and simple purification. The hydrothiolation reactions have numerous trapping applications in the fields of polymer chemistry, nanoengineering, pharmaceuticals, natural products, and perhaps most importantly in medicinal chemistry for the synthesis of many drugs and bioactive molecules.