An environment friendly synthesis of 2-amino-3-cyano-4-aryl-7,7-dimethyl-5-oxo-4H-5,6,7,8-tetrahydrobenzo[b]pyran, 2aryl benzimidazole and 2-aryl-4, 5-dihydro-1H-imidazole derivatives using Mg-Al hydrotalcite as an efficient catalyst has been developed. The excellent efficiency of the catalyst can be attributed to its Lewis acidic sites which resulted in higher reaction yields for different sub...

Successful implementation of ultrasound irradiation for the rapid synthesis of a novel series of 3-[1-(4-substituted-5-(aryldiazenyl)thiazol-2-yl)hydrazono)ethyl]-2H-chromen-2-ones 5a-h, via reactions of 2-(1-(2-oxo-2H-chromen-3-yl)ethylidene) thiosemicarbazide (2) and the hydrazonoyl halides 3(4), was demonstrated. Also, a new series of 5-arylidene-2-(2-(1-(2-oxo-2H-chromen-3-yl)ethylidene)hyd...

Ko143 is a tetracyclic, synthetic analog of the fungal metabolite fumitremorgin C. potent and specific inhibitor membrane-bound efflux transporter ABCG2, it reverses ABCG2-mediated drug resistance in cancer cells. Here, we describe an improved synthesis that relies on highly selective, substrate-controlled reduction imine formed Bischler–Napieralski reaction with amide derived from 6-methoxy-l-...

A simple, efficient and cost effective method is described for the synthesis of Biginelli type heterocyclic compounds of dihydropyrimidinones analogous. They were prepared from a reaction mixture consisting of substituted benzaldehydes, thiourea and ethylacetoacetate using ammonium dihydrogenphosphate as catalyst. The procedure for the preparation of the compounds is environmentally benign and ...

We have developed a liquid-phase route for combinatorial synthesis of novel substituted 5-(1,2,4-oxadiazol-5-yl)-3,4-dihydropyrimidine-2(1H)-thiones. Biginelli-type three-component condensation of 1-(3-aryl-1,2,4-oxadiazol-5-yl)acetones, thiourea, and benzaldehydes is shown to result in new 5-(1,2,4-oxadiazol-5-yl)-3,4-dihydropyrimidine-2(1H)-thione heterocyclic system. If salicylaldehydes are ...

A series of simple heterocyclic chalcone analogues have been synthesized by Claisen Schmidt condensation reactions between substituted benzaldehydes and heteroaryl methyl ketones and evaluated for their antibacterial activity. The structures of the synthesized chalcones were established by IR and ¹H-NMR analysis. The biological data shows that compounds p₅, f₆ and t₅ had strong activities again...

In an effort to develop new antibacterial drugs, some novel bisindolylmethane derivatives containing Schiff base moieties were prepared and screened for their antibacterial activity. The synthesis of the bisindolylmethane Schiff base derivatives 3-26 was carried out in three steps. First, the nitro group of 3,3'-((4-nitrophenyl)-methylene)bis(1H-indole) (1) was reduced to give the amino substit...

Chalcones 1~8 and 5-deoxyflavonoids 9~22 were synthesized in good yields by aldol condensation, Algar-Flynn-Oyamada reaction, glycosidation, and deacetylation reaction, respectively, starting from 2-acetyl phenols substituted by methoxy or methoxymethoxy group and appropriately benzaldehydes substituted by methoxy, methoxymethoxy group, or chlorine. Among them, 13 and 17~22 are new compounds. T...

Since the discovery of the antituberculous activity of isonicotinic acid hydrazide (isoniazid), many related chemical compounds have been studied in the hope of finding compounds still more potent, less toxic, and of longer-lasting activity. Isonicotinylhydrazones of substituted benzaldehydes have been studied by several groups of investigators. A total of 25 derivatives have been reported to b...