Showing papers by "Bareilly College published in 2016"

Synthesis and Evaluation of Heterocyclic Derivatives of Morpholino-N-Acetyl Indoles for Central Nervous System Depressant Activity

Abstract: In the present work, 2-oxo-3[4`-p(subst/unsubst)-phenyl-2`-thiazolyl/oxazolyl] morpholino-N-acetyl indoles were synthesized. The different heterocyclic moieties were condensed with isatin in ethanol containing few drops of glacial acetic acid which were converted into various Thiazolyl/oxazolyl imino indoles. The imino indoles were condensed with chloro acetyl chloride in K2CO3 which were converted to N-chloro acetyl indole derivatives which on subsequent treatment with morpholino in benzene were converted to title compound.The structures of the synthesized compounds were characterized onthe basis of IR and HNMR spectral data. Among all the synthesized compounds fewselected compounds werescreened for their CNS activity. Chlorpromazine hydrochloride is employed as a reference standard.From the results it is concluded that, synthesized compounds show more depressant activity thanreference standard.

Synthesis of some new 1, 3-di methyl substituted guanidine with possible antibacterial and antifungal activity

Abstract: The compounds containing thiazole, thiadiazole, oxazole, oxadiazole, imidazole, pyrimidine, pyridine & benzothiazole rings have been found to exhibit broad spectrum of biological activities. Derivatives of 1, 2, 4-thiadiazole and 1, 2, 4-thiadiazolidines exhibit antibacterial and antifungal activity 1 . Thiazolyl guanidines2 and various substituted aryl guanidine’s have been found to exhibit antibacterial & antifungal activities3.Keeping all these views in mind attempts were made to synthesized some new 1,3-di methyl Substituted Guanidine. In the present work 2,4 Dimethyl -3,5-(di Aryl imino)-1,2,4-thiadiazolidines were prepared by nitrous acid oxidation of N-methyl –N Aryl thiourea4 & 2,4 dimethyl-3,5-(diaryl imino)-1,2,4-thiazolidines were converted to corresponding 1,3 di methyl substituted guanidine’s by their acid catalyzed re-arrangment5.(Scheme-1) Antibacterial & Antifungal activity of the title compounds were evaluated against two bacteria, E.coli & lactobacillus & two fungi, A.Brassicicola & Aspergillus Niger. N=methyl-N`-Aryl thiourea (1-10) were prepared by refluxing a mixture of different 2-Amino Heterocyclic moieties with methyl iso thiocyanate in Ethanol. A mixture of compound (1-100 and conc. HCl, ethanol was added drop wise & under stirring to a solution of NaNO2 in water afforded 2, 4-dimethyl-3, 5-(di Aryl imino)-1,2,4-thiadiazolidine (11-20) afforded 1,3 di methyl substituted guanidine’s (21-30). Structures of the compounds were established by elemental analysis & spectral data.