ABSTRACT
A number of 6- [3- pyridyl] nicotinonitrile derivatives were synthesized for their potential cardiotonic activity. This was achieved by reacting ketones [1] with ethyl cyanoacetate to give [II] or [III] depending on the reaction conditions. Similarly cyclocondensation of the same substrates [I] with malononitrile afforded the corresponding derivatives [IV] or [V]
Subject(s)
Chemistry, PharmaceuticalABSTRACT
The synthesis of a novel series of substituted-aminocoumarins [II], [III] and [IV] and the preliminary evaluation of their in vitro antimicrobial activity are described. The reaction of 4- hydroxycoumarin [I] with a number of primary or cyclic secondary amines afforded the corresponding 4-aminocoumarins derivatives [II]. Likewise, reacting the same substrate with different sulpha-drugs furnished the respective 4-[4-[N-substituted-sulphamoylphenyl]] -aminocoumarins [III]. On the other hand, Mannich reaction of [I] with formaldehyde and certain amines yielded the desired 4-hydroxy 3- substituted-aminomethyl-coumarins [IV]. The antimicrobial screening has revealed that some of these novel compounds possess moderate activity against Bacillus subtilis and Bacillus pumitis
Subject(s)
AntibiosisABSTRACT
A novel series of compounds comprising 2-mercaptobenzothiazole and thiadiazoles, 1, 2, 4-triazoles and 1, 3, 4-oxadiazolines was synthesized. Cyclization of semi-carbazides and thiosemicarbazides [III] by either conc. sulphuric acid or 2N sodium hydroxide yielded the thiadiazoles [IV] and the triazoles [V] respectively. On the other hand, acylated 1, 3, 4-oxadiazolines [VII] were formed by treating N2-arylidenehydrazides [VI] with acetic anhydride. Six compounds were subjected to in vitro testing for antimicrobial activity