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2, 3‐Bis(5‐alkyl‐2‐thiono‐1, 3, 5‐thiadiazin‐3‐yl) Propionic Acid: One‐Pot Domino Synthesis and Antimicrobial Activity
Author(s) -
El Bialy Serry A. A.,
Abdelal Ali M.,
ElShorbagi AbdelNasser,
Kheira Samy M. M.
Publication year - 2005
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200400906
Subject(s) - domino , chemistry , antimicrobial , alkyl , biological activity , chemical synthesis , cascade reaction , stereochemistry , organic chemistry , combinatorial chemistry , in vitro , biochemistry , catalysis
In a search for promising antibacterial and antifungal compounds, two new series of 2, 3‐ bis (5‐alkyl‐2‐thiono‐1, 3, 5‐thiadiazin‐3‐yl)propionic acid 1 and their corresponding N, N ‐dimethylpropionamide 6 have been synthesized. The reaction of 2, 3‐diaminopropionate 3 , carbon disulfide, formaldehyde, and the appropriate alkyl amines furnished the title compound 1 . N, N ‐dimethylpropionamides 6 were obtained by the reaction of 1 with dimethyl amine in the presence of POCl 3 . The newly prepared compounds were screened in vitro against certain strains of Gram‐positive and Gram‐negative bacteria and compared with nalidixic acid and ciprofloxacin. Moreover, the title compounds were tested for their antifungal activity in vitro against Candida albicans , phytopathogenic, Penicillum expansum and Trichoderma hazianum , and aflatoxin‐producing Aspergillus flavus . These compounds exhibit varied activity against the tested pathogenic bacteria and remarkable inhibitory effects on growth or sporulation of some of the tested fungal species.