β-Carboline and γ-lactone moieties have been selected by nature as privileged scaffolds and display a wide range of pharmacological properties. Following nature, we envisaged the preparation of new β-carboline and γ-lactone based molecular hybrids incorporating both the pharmacophores. In this regard, a water-assisted In-mediated environmentally benign and easy to execute single-step tandem Barbier type allylation-lactonisation process has been devised in order to afford the targeted molecular architectures. It is anticipated that aqueous medium plays the key role in allylation as well as in the subsequent lactonisation process for the diastereo-selective synthesis of these conjugates. It is believed that water drives the reaction pathway through dual activation, it increases the electrophilic character of formyl and ester functionalities and simultaneously enhances the nucleophilic potential of the hydroxyl group to facilitate the in situ intramolecular condensation. Importantly, during this synthetic strategy no column chromatographic purification was required at any stage.

An efficient methodolgy has been developed towards the one‐pot synthesis of pyrazolopyridinone fused imidazopyridines from 4‐formyl‐1H‐pyrazole‐3‐carboxylates, pyridin‐2‐amines and tert‐butyl isonitrile as the starting materials. The transformation has been accomplished by using In(OTf)3 assisted Groebke‐Blackburn‐Bienayme (GBB) multicomponent approach to yield the N‐fused imidazo[1,2‐a]pyridine scaffolds which were further served in‐situ HBF4 mediated dealkylation and tandem intramolecular condensation. The current protocol paves the way for the synthesis of biologically interesting molecular frameworks and has advantages in terms of low catalyst loading with appreciable atom economy and easy‐to‐perform reaction conditions with straightforward purification procedure. Importantly, this efficient catalytic system offers a lot of future scope for variety of organic transformations in other MCRs.

~~ ~~Derivatives of 2-aminonaphthothiazole have been synthesized as potential local anesthetics by treating 2aminonaphthothiazole with chloroacetyl chloride whereby chloroacetyl-2-aminonaphthothlazole is obtained. This is subsequently treated with various amines to afford morpholinoacetyl, piperidinoacetyl, dimethylaminoacetyl, N,N-dimethylanillno-p-aminoacetyl, N,N-diethylanilino-paminoacetyl, pyridine-2-aminoacetyl, pyrimidlne-2aminoacetyl, diphenylaminoacetyl, and piperazinoacetyl-2-amlnonaphthothiazole.Some derivatives of 2-aminobenzothiazole ( 7 , 2, 5) and 2aminothiazole (3, 4) are reported to possess considerable local anesthetic activity. It was thought worthwhile to prepare some new compounds from 2-aminonaphthothiazole which may exhibit local anesthetic activity. These compounds are synthesized by chloroacetylation of 2-aminonaphthothiazole with chloroacetyl chloride. The chloroacetylated product was then condensed with different amines. The bases, being liquid, were characterized through their solid derivatives. Experimental Section 2-Aminonaphthothiazole ( 6 ) .It was prepared by oxidation of a-naphthylthiourea with bromine in chloroform medium. Naphthylthiourea (10 g) was suspended in chloroform (50 mL) and a solution of bromine (4 mL) in chloroform was added gradually with cooling and stirring of the reaction mixture. After allowing to stand overnight, the chloroform was evaporated and the residue was treated with a little sodium bisulfite solution to remove the unreacted bromine. The crude product was basified when a soft base crystallizable from aqueous ethanol, mp 190 'C, was obtained.Preparation of Chloroacefyl-2-aminonaphfhothiazole. The solution of about 2.82 g of chloroacetyl chloride in dry ether (20 cm3) was gradually added to a solution of 2-aminonaphthothiazole (5 g) in dry ether (30 cm3). The chloroacetyl-2-aminonaphthothiazole was separated immediately and filtered and res-0021-956817811723-0089$01 .OO/O

The objective of this work was to evaluate grafted soy protein isolate (SPI) for pharmaceutical applications. The present work reports the microwave-assisted preparation of soy protein isolate\grafted[acrylic acid- co -4-(4-hydroxyphenyl)butanoic acid] [SPI- g -(AA- co -HPBA)] hydrogel via graft copolymerization using N , N -methylene-bis-acrylamide and potassium persulphate as the cross-linker and initiator, respectively. The chemical and physical properties of the synthesized polymeric hydrogels were analyzed by Fourier transform infrared spectroscopy, liquid chromatography–mass spectrometry (LCMS), nuclear magnetic resonance 1 H-NMR, X-ray diffraction (XRD), transmission electron microscopy (TEM), scanning electron microscopy (SEM), and thermogravimetric analysis (TGA). The SEM, TEM, and XRD analyses have confirmed the formation of hydrogel SPI- g -(AA- co -HPBA) with the network structure having a layered and crystalline surface. The SPI- g -(AA- co -HPBA) hydrogel was investigated for the sustained and controlled drug delivery system for the release of model drug ciprofloxacin at basic pH for its utilization against bacterial infection in oral cavity. The drug release profile for SPI- g -(AA- co -HPBA) hydrogels was studied using LCMS at the ppb level at pH = 7.4. The synthesized hydrogel was found to be noncytotoxic, polycrystalline in nature with a network structure having good porosity, increased thermal stability, and pH-responsive behavior. The hydrogel has potential to be used as the vehicle for controlled drug delivery in oral cavity bacterial infections.