Mukesh D. Nikam

超声辅助多组分反应:水介质中以β-环糊精为可重复使用的超分子催化剂绿色合成氮取代的1,8-二氧-十氢吖啶

We demonstrate a superficial method for the synthesis of N-substituted 1,8-dioxo-decahydroacridines using β-cyclodextrin as a supramolecular, biodegradable, and reusable catalyst in aqueous medium. The reaction product is in excellent yield with moderate to excellent selectivity. The mechanistic transformation presumably proceeds via a one-pot, multicomponent cyclization of dimedone in the presence of aromatic aldehydes and aromatic amines/INH, undergoing a tandem Michael addition reaction. The proposed approach in this study provides a highly efficient and environmentally benign route to N-substituted 1,8-dioxo-decahydroacridines.

Synthesis, molecular docking and biological evaluation of some novel tetrazolo[1,5-a]quinoline incorporated pyrazoline and isoxazoline derivatives

A series of new pyrazolines (4a–4g) and isoxazolines (5a–5g) have been synthesized in good-to-excellent yield from the corresponding chalcones (3a–3g) under ultrasound irradiation. The newly synthesized compounds were characterized and screened for their in vitro antimicrobial activity against different bacterial and fungal strains by standard agar dilution method and in vitro antioxidant activity by using DPPH method. Some of the synthesized compounds displayed significant antimicrobial and antioxidant activity. Docking study of the synthesized compounds has been performed, and results showed good binding mode in the active site of fungal enzyme P450 cytochrome lanosterol 14 α-demethylase. ADMET properties of synthesized compounds showed good drug-like properties.

Lithium bromide catalyzed efficient and convenient synthesis of 2-arylbenzothiazole derivatives

A new and efficient protocol was developed for synthesis of benzothiazoles using lithium bromide as catalyst under environmentally friendly conditions. The developed synthetic protocol represents a novel and very simple route for preparation of 2-substituted benzothiazole derivatives. In addition, an ultrasound irradiation technique is successfully implemented for carrying out the reactions in shorter reaction times.

Synthesis, Antioxidant, Anti-Inflammatory, and Antimicrobial Screening of Newer Thiophene-Fused Arylpyrazolyl 1,3,4-Oxadiazoles

GRAPHICAL ABSTRACT Abstract A series of newer 1,3,4-oxadiazole derivatives 3a–h, 5a–h containing a thiophene fused with pyrazole moiety of pharmacological significance have been synthesized. The compounds were characterized by 1H NMR, IR, and mass spectral techniques. The compounds were screened for their in vitro antioxidant, anti-inflammatory and antimicrobial activities. Among them, Compounds 3b (EC50–14.98) and 3f (EC50–12.21) showed significant antioxidant activity. Compound 3a (EC50–15.23) showed good anti-inflammatory activity. Compound 3d was found as the most active derivative against bacterial and fungal strains.

AN EFFICIENT AND GREEN PROTOCOL FOR THE SYNTHESIS OF DIHYDROPYRANO [2,3-C] PYRAZOLES IN AQUEOUS MEDIUM USING THIAMINE HYDROCHLORIDE AS A CATALYST

A green and expedient approach for the synthesis of dihydropyrano[2,3-c] pyrazoles via four-component reaction of ethyl acetoacetate, hydrazine hydrate, aromatic aldehydes and malononitrile at room temperature under ultrasound irradiation is described. The reaction has been catalyzed by thiamine hydrochloride in aqueous medium. This protocol afforded several advantages such as inexpensive, easily available catalyst, simple operational procedure, excellent yield, use of aqueous medium and ultrasound irradiation that is considered to be relatively eco-friendly.