Novel bisbenzamidines as potential drug candidates for the treatment of Pneumocystis carinii pneumonia.
A series of pentamidine congeners has been synthesized and screened for their in vitro activity against Pneumocystis carinii. Among the tested compounds, bisbenzamidines linked by a flexible pentanediamide or hexanediamide chain (7 and 9) emerged as exceptionally potent agents that were more effective and less toxic than pentamidine in the assays described in this study.
Vanden Eynde
Jean Jacques
JJ
Xavier University of Louisiana, College of Pharmacy, Division of Basic Pharmaceutical Sciences, 1 Drexel Drive, New Orleans 70125, USA.
Mayence
Annie
A
Huang
Tien L
TL
Collins
Margaret S
MS
Rebholz
Sandra
S
Walzer
Peter D
PD
Cushion
Melanie T
MT
D000818:Animals; D001550:Benzamidines / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D045363:Pneumocystis carinii / Q000187:drug effects* / Q000254:growth & development; D011020:Pneumonia, Pneumocystis / Q000188:drug therapy*; D051381:Rats; D011914:Rats, Inbred BN; D020318:Rats, Long-Evans
D001550:Benzamidines