ChemInform Abstract: Relationships Between the Chemical Structure of Substances and Their Antimycobacterial Activity to Atypical Strains. Part 9. A New Pharmacophore of Potential Antimycobacterial Activity: The Disulfide Group in the Ring of Alicyclic Com

ChemInform ◽  
2010 ◽  
Vol 28 (31) ◽  
pp. no-no
Author(s):  
H.-D. STACHEL ◽  
Z. ODLEROVA ◽  
K. WAISSER
Keyword(s):  
Chemical Structure ◽  
Antimycobacterial Activity ◽  
Disulfide Group ◽  
Atypical Strains

Relationships Between the Chemical Structure of Substances and Their Antimycobacterial Activity Against Atypical Strains. Part 18. 3-Phenyl-2H-1,3-benzoxazine-2,4(3H)-diones and Isosteric 3-Phenylquinazoline-2,4(1H,3H)-diones

1999 ◽  
Vol 64 (11) ◽  
pp. 1902-1924 ◽  
Author(s):  
Karel Waisser ◽  
Miloš Macháček ◽  
Hynek Dostál ◽  
Jiří Gregor ◽  
Lenka Kubicová ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Chemical Structure ◽  
Nontuberculous Mycobacteria ◽  
Antimycobacterial Activity ◽  
Diffusion Method ◽  
Significant Activity ◽  
Vector Algebra ◽  
Phenyl Rings ◽  
Agar Diffusion Method ◽  
Atypical Strains

A series of 3-phenyl-2H-1,3-benzoxazine-2,4(3H)-diones 2 and 3-phenylquinazoline-2,4(1H,3H)-diones 5 substituted on the phenyl rings were synthesized. The target compounds as well as the intermediates were tested against Mycobacterium tuberculosis, M. kansasii, and M. avium. The replacement of the oxygen atom by nitrogen resulted in a decrease or loss of antimycobacterial activity. 2-[(Ethoxycarbonyl)amino]benzanilides 4 appeared to be inactive. Salicylanilides 1 and 3-phenyl-2H-1,3-benzoxazine-2,4(3H)-diones 2 exhibit significant activity against both M. tuberculosis and nontuberculous mycobacteria (the MICs within the range of 4-250 μmol/l for all compounds). The antimycobacterial activity of the compounds increases with increasing both electron-withdrawing properties and hydrophobicity of the substituent(s) on the phenyl moiety. The antimycobacterial profile of the compounds was analyzed according to the criteria based on vector algebra, such as cosine coefficients. Moreover, salicylanilides 1 exhibit activity against other microorganisms tested by the agar diffusion method.

New Groups of Potential Antituberculotics: Bis(1-aryltetrazol-5-yl) Disulfides. Structure Activity Relationship

1994 ◽  
Vol 59 (1) ◽  
pp. 234-238 ◽  
Author(s):  
Karel Waisser ◽  
Jiří Kuneš ◽  
Alexandr Hrabálek ◽  
Želmíra Odlerová
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Antimycobacterial Activity ◽  
Activity Relationship ◽  
Active Derivative ◽  
Structure Activity ◽  
Medium Activity ◽  
Substituent Constants ◽  
Atypical Strains

Oxidation of 1-aryltetrazole-5-thiols afforded bis(1-aryltetrazol-5-yl) disulfides. The compounds were tested for antimycobacterial activity against Mycobacterium tuberculosis, M. kansasii, M. avium and M. fortuitum. In the case of M. tuberculosis, the logarithm of minimum inhibitory concentration showed a parabolic dependence on hydrophobic substituent constants. Although the compounds exhibited low to medium activity, the most active derivative, bis(4-chlorophenyltetrazol-5-yl) disulfide (III) was more effective against atypical strains than are the commercial tuberculostatics used as standards.

A New Pharmacophore of Potential Antimycobacterial Activity: The Disulfide Group in the Ring of Alicyclic Compounds

1997 ◽  
Vol 62 (3) ◽  
pp. 510-515 ◽  
Author(s):  
Hans-Dietrich Stachel ◽  
Želmíra Odlerová ◽  
Karel Waisser
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Antimycobacterial Activity ◽  
Disulfide Group ◽  
Structure Activity Relationships ◽  
Structure Activity

A series of thirty 2,3-dithiabicyclo[3.3.0]octa-4,8-diene derivatives was examined for antimycobacterial activity against Mycobacterium tuberculosis, M. kansasii, M. avium, and M. fortuitum. The structure-activity relationships were analysed by Free-Wilson method. The authors consider the disulfide moiety to be the pharmacophore of antimycobacterial activity. To verify the idea, several other monocyclic sulfides, 3,4-dihydro-1,2-dithiolane derivatives, were also evaluated.

scholarly journals THE ANTIMYCOBACTERIAL ACTIVITY OF VARIOUS AMINES RELATED TO SPERMINE IN CHEMICAL STRUCTURE

1953 ◽  
Vol 97 (3) ◽  
pp. 323-325 ◽  
Author(s):  
James G. Hirsch
Keyword(s):  
Liquid Medium ◽  
Chemical Structure ◽  
Antimycobacterial Activity ◽  
Final Concentration ◽  
Chemical Degradation ◽  
Amino Compounds

A final concentration of 3 x 10–5 M spermine or spermidine inhibited the growth of mammalian tubercle bacilli in a modified Dubos liquid medium. Various related amino compounds, including isolated portions of the spermine molecule and the products of its chemical degradation, did not manifest similar antimycobacterial activity.

Inelastic Electron-Matter Interactions

1978 ◽  
Vol 36 (3) ◽  
pp. 259-267
Author(s):  
J. Silcox
Keyword(s):  
Electron Microscope ◽  
Energy Loss ◽  
Chemical Structure ◽  
Inelastic Electron ◽  
Primary Concern ◽  
Unique Probe ◽  
Introductory Paper ◽  
Elastic Processes ◽  
Experimental Level ◽  
Inelastic Processes

In this introductory paper, my primary concern will be in identifying and outlining the various types of inelastic processes resulting from the interaction of electrons with matter. Elastic processes are understood reasonably well at the present experimental level and can be regarded as giving information on spatial arrangements. We need not consider them here. Inelastic processes do contain information of considerable value which reflect the electronic and chemical structure of the sample. In combination with the spatial resolution of the electron microscope, a unique probe of materials is finally emerging (Hillier 1943, Watanabe 1955, Castaing and Henri 1962, Crewe 1966, Wittry, Ferrier and Cosslett 1969, Isaacson and Johnson 1975, Egerton, Rossouw and Whelan 1976, Kokubo and Iwatsuki 1976, Colliex, Cosslett, Leapman and Trebbia 1977). We first review some scattering terminology by way of background and to identify some of the more interesting and significant features of energy loss electrons and then go on to discuss examples of studies of the type of phenomena encountered. Finally we will comment on some of the experimental factors encountered.

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