Search

Nitroimidazole substituted at 2nd position of imidazole showing potent biological activities. Two series of nitroimidazole compounds, 5-(1-(substituted)-5-nitro-1H-imidazol-2-yl)-4-(furan-2- yl))thiazol-2-amine and 6-(1-(substituted)ethyl)-5-nitro-1H-imidazol-2-yl)-5-(furan-2-yl)-4H- 1,3,4-thiadiazin-2-amine were synthesized. Synthesized compound were screened against, Clostridium sporogenus and Bacteriodes fragililis. Compound 67-c and 68-c substitued with amino thaidaizine ring showing good activity amongst the series. [ABSTRACT FROM AUTHOR]

Nine nitroimidazoles drugs representing different class were found in the literature to have their respective half wave potential and one electron reduction potential measure under near-identical conditions. The structures of these nine nitroimidazoles were optimized, and resulting physicochemical parameters were regressed against one electron reduction potential (OERPs). A very significant linear correlation (QSAR) was found between OERPs and Extended Huckel Partial Atomic Charges. These findings suggest that it may be possible to estimate OERPs of nitroimidazole in advance to its synthesis. Insofar as the OERPs correlating to DNA damage, radiosensitization efficiency, aerobic cytotoxicity, mutagenicity and hypoxic cytotoxicity; the Extended Huckel Partial Atomic Charges can predict well all these biological activity prior to synthesis of novel nitroimidazoles. [ABSTRACT FROM AUTHOR]

The nitroheterocyclic compounds have proved to be very effective antimicrobial agents and very valuable member of limited armamentarium of antiprotozoal agents. A number of 5-nitoimidazole with substitution at 2-position with various substitutent are found to modify the antibacterial spectrum. Some 2-substituted nitroimidazole analogues were designed, synthesized and characterized. The synthesized compounds were tested for their antibacterial sensitivity against Gram-positive anaerobe (C. sporogenus) and Gramnegative anaerobe (B.fragilis) using macro broth dilution method. All the synthesized compounds exhibit good activity at 10 mcg/ml against Gram-negative anaerobe compared to standard control tinidazole and metronidazole, while remain inactive against Gram-positive anaerobe. [ABSTRACT FROM AUTHOR]

The Ni(II) complex of novel, 2-(1-(substituted)-5-nitro-1H-imidazol-2-yl)-1-(substituted) ethanone have been synthesized and characterized by FTIR, molar conductivity, 1HNMR, MASS. Novel 2-nitroimidazole act as a bidentate ligand through the 3-N of imidazole ring and C=O, at 2-position of nitroimidazole, which coordinate the metal ion give rise to 4-coordinate tetrahedral Ni(II) complex. The in vitro antimicrobial activity was determined by using cylinder plate method. The compounds were found to be more active than ligand against Gram-positive bacteria, B. Pumilus ATCC 14884, S. aureus ATCC 29737 and Gram negative bacteria, S. aboney NCTC 6017. [ABSTRACT FROM AUTHOR]

Taking in to consideration of diverse biological activities of coumarin and thiazole derivatives, attempts have been made to attach a thiazole side chain at C-3 position of coumarin. In addition, to expand the structural diversity of synthetic courmarins for biological functions, the morpholine fusion at 2nd position of thiazole was also attempted. The compounds MM3M1 was synthesized keeping coumarin-3-yl constant at fifth position, morpholine at 2nd position and phenyl moiety at 4th position of thiazole nucleus. The compounds MM3M2, MM3M3 and MM3M4 were synthesized keeping coumarin-3- yl constant at fifth position, morpholine at 2nd position and introducing electron withdrawing group (-Cl) at ortho, meta and para position respectively in phenyl moiety at 4th position of thiazole nucleus. All the synthesized compounds were evaluated for their invitro antibacterial and anti-platelet activity. On the basis of structure-activity relationship studies of synthesized MM3M1- MM3M4 it can be concluded that presence of 2-chlorophenyl group at the 4th position of the thiazole contributes significantly to antibacterial and anti-platelet activity profile of the candidates. [ABSTRACT FROM AUTHOR]