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Antischistosomal agents: state of art and perspectives.

Abstract Praziquantel has remained the drug of choice for schistosomiasis chemotherapy for almost 40 years. The pressing need to develop a new antischistosomal drug may necessitate exploring and filtering chemotherapeutic history to search for the most promising ones. In this context, this review attempts to summarize all progress made in schistosomiasis chemotherapy from the early 20th century (mid-1910s) to 2016. We gathered almost 100 compounds providing information on therapeutic action, specifically covering at least first in vivo studies in animal model and in vitro. Pharmacokinetic and toxicity profiles of antischistosomal agents were also described. Preclinical studies indicate a handful of promising future candidates.
PMID
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Authors

Mayor MeshTerms
Keywords

Hit

chemogenomics

drug discovery

drug repositioning

druggability

high-throughput screening

lead

molecular modeling

Journal Title future medicinal chemistry
Publication Year Start




PMID- 29235368
OWN - NLM
STAT- MEDLINE
DCOM- 20171225
LR  - 20171225
IS  - 1756-8927 (Electronic)
IS  - 1756-8919 (Linking)
VI  - 10
IP  - 1
DP  - 2018 Jan
TI  - Antischistosomal agents: state of art and perspectives.
PG  - 89-120
LID - 10.4155/fmc-2017-0112 [doi]
AB  - Praziquantel has remained the drug of choice for schistosomiasis chemotherapy for
      almost 40 years. The pressing need to develop a new antischistosomal drug may
      necessitate exploring and filtering chemotherapeutic history to search for the
      most promising ones. In this context, this review attempts to summarize all
      progress made in schistosomiasis chemotherapy from the early 20th century
      (mid-1910s) to 2016. We gathered almost 100 compounds providing information on
      therapeutic action, specifically covering at least first in vivo studies in
      animal model and in vitro. Pharmacokinetic and toxicity profiles of
      antischistosomal agents were also described. Preclinical studies indicate a
      handful of promising future candidates.
FAU - Lago, Eloi M
AU  - Lago EM
AD  - Nucleo de Pesquisa em Doencas Negligenciadas, Universidade Universus Veritas
      (UNIVERITAS UNG), Praca Tereza Cristina, 229, Centro, Guarulhos 07023-070, SP,
      Brazil.
FAU - Xavier, Rogerio P
AU  - Xavier RP
AD  - Nucleo de Pesquisa em Doencas Negligenciadas, Universidade Universus Veritas
      (UNIVERITAS UNG), Praca Tereza Cristina, 229, Centro, Guarulhos 07023-070, SP,
      Brazil.
FAU - Teixeira, Thaina R
AU  - Teixeira TR
AD  - Nucleo de Pesquisa em Doencas Negligenciadas, Universidade Universus Veritas
      (UNIVERITAS UNG), Praca Tereza Cristina, 229, Centro, Guarulhos 07023-070, SP,
      Brazil.
FAU - Silva, Livia M
AU  - Silva LM
AD  - Departamento de Ciencias Farmaceuticas, Universidade Federal de Juiz de Fora,
      Juiz de Fora, MG, Brazil.
FAU - da Silva Filho, Ademar A
AU  - da Silva Filho AA
AD  - Departamento de Ciencias Farmaceuticas, Universidade Federal de Juiz de Fora,
      Juiz de Fora, MG, Brazil.
FAU - de Moraes, Josue
AU  - de Moraes J
AD  - Nucleo de Pesquisa em Doencas Negligenciadas, Universidade Universus Veritas
      (UNIVERITAS UNG), Praca Tereza Cristina, 229, Centro, Guarulhos 07023-070, SP,
      Brazil.
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20171213
PL  - England
TA  - Future Med Chem
JT  - Future medicinal chemistry
JID - 101511162
RN  - 0 (Anthelmintics)
RN  - 6490C9U457 (Praziquantel)
SB  - IM
MH  - Animals
MH  - Anthelmintics/*pharmacology
MH  - Humans
MH  - Parasitic Sensitivity Tests
MH  - Praziquantel/*pharmacology
MH  - Schistosoma/*drug effects
MH  - Schistosomiasis/*drug therapy
OTO - NOTNLM
OT  - Hit
OT  - chemogenomics
OT  - drug discovery
OT  - drug repositioning
OT  - druggability
OT  - high-throughput screening
OT  - lead
OT  - molecular modeling
EDAT- 2017/12/14 06:00
MHDA- 2017/12/26 06:00
CRDT- 2017/12/14 06:00
PHST- 2017/12/14 06:00 [pubmed]
PHST- 2017/12/26 06:00 [medline]
PHST- 2017/12/14 06:00 [entrez]
AID - 10.4155/fmc-2017-0112 [doi]
PST - ppublish
SO  - Future Med Chem. 2018 Jan;10(1):89-120. doi: 10.4155/fmc-2017-0112. Epub 2017 Dec
      13.