摘要:
Novel dicationic 2,5-diaryl selenophene compounds are described. Also described are novel aza analogues of dicationic 2,5-diaryl thiophenes. The presently disclosed dicationic compounds exhibit in vitro activity versus Trypanosoma brucei rhodesiense, Plasmodium falciparum, and/or Leishmania donovani comparable to that of pentamidine and furamidine. Some of the novel dicationic compounds display good activity in vivo in a murine model of a Trypanosoma brucei rhodesiense infection.
摘要:
Disclosed herein are novel dicationic teraryl compounds and their aza analogues, including compounds of Formula (IIe): wherein p and q are each 0 and each A, Y and Z is CR4. An exemplary compound of Formula (IIe) is: Methods for combating microbial infections, such as parasitic Leishmania species, with novel dicationic terphenyl compounds and their aza analogues are included. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues are disclosed along with methods for evaluation of the compounds as potential anti-protozoan agents.
摘要:
Novel dicationic bichalcophene compounds are described. The presently disclosed novel dicationic bichalcophene compounds exhibit in vitro activity versus Trypanosoma brucei rhodesiense, Plasmodium falciparum, or Leishmania donovani comparable to that of pentamidine and furamidine. Some of the novel dicationic bichalcophene compounds displayed good activity in vivo in a murine model of a Trypanosoma brucei rhodesiense infection.
摘要:
Novel aza analogues of dicationic terphenyl compounds for use in combating microbial infections are described. Also described are processes for synthesizing the compounds. The presently disclosed compounds can include those of the formulas: and wherein L1 and L2 are selected from the group consisting of:
摘要:
Novel dicationic terphenyl compounds and their aza analogues. Methods for combating microbial infections with novel dicationic terphenyl compounds and their aza analogues. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues.
摘要:
Novel aza analogues of dicationic terphenyl compounds for use in combating microbial infections are described. The compounds include those of Formula (III): wherein one of A1, Y1, and Z1 is N; Ar1 is phenylene; and Ar3 is a nitrogen-containing aromatic group. An exemplary compound of Formula (III) is:
摘要:
Novel fused ring dicationic anti-protozoan compounds. Representative protozoan species include but are not limited to Trypanosoma brucei rhodesiense (T.b.r.) and Plasmodium falciparum. Prodrugs of these compounds can be used as an oral treatment for malaria and human African trypanosomiasis.
摘要:
A compound of Formula (I): wherein: X is selected from the group consisting of O, S, and NR17, where R17 is hydrogen or lower alkyl; A and Y are CH, N, NR17, O, or S; C1 and C2 are each C or N, wherein C1 and C2 are the same or different; D1 and D2 are each C or N, wherein D1 and D2 are the same or different; B and Z are CH, N, or NR17, provided that B, Z, or both B and Z are not present when A, Y, or both A and Y are O, S, or NR17; R13, R14, R1 and R8 can be present or absent, and when present are selected from the group consisting of H, lower alkyl, halogen, alkoxyl, aryloxyl, aralkoxy and hydroxyl; R15 and Rare selected from the group consisting of H, lower alkyl, halogen, alkoxyl, aryloxyl, aralkoxy and hydroxyl; R3 and R6 are each independently selected from the group consisting of H, hydroxy, lower alkyl, cycloalkyl, aryl, aralkyl, alkoxyl, hydroxycycloalkyl, alkoxycycloalkyl, hydroxyalkyl, aminoalkyl, acyloxy, acetoxy, and alkylaminoalkyl; and R2, R4, R5 and R7 are each independently selected from the group consisting of H, lower alkyl, alkoxyalkyl, cycloalkyl, aryl, aralkyl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl, or R2 and R4 together or R5 and R7 together represent a C2 to C10 alkyl, hydroxyalkyl, or alkylene, or R3 and R4 together or R6 and R7 together are: wherein n is a number from 1 to 3, and R9 is H or —CONHR10NR11R12, wherein R10 is lower alkyl and R11 and R12 are each independently selected from the group consisting of H and lower alkyl.
摘要:
Novel dicationic bichalcophene compounds are described. The presently disclosed novel dicationic bichalcophene compounds exhibit in vitro activity versus Trypanosoma brucei rhodesiense, Plasmodium falciparum, or Leishmania donovani comparable to that of pentamidine and furamidine. Some of the novel dicationic bichalcophene compounds displayed good activity in vivo in a murine model of a Trypanosoma brucei rhodesiense infection.
摘要:
Novel dicationic terphenyl compounds and their aza analogues. Methods for combating microbial infections with novel dicationic terphenyl compounds and their aza analogues. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues.