PMID- 26840364
OWN - NLM
STAT- MEDLINE
DCOM- 20161031
LR  - 20191210
IS  - 1768-3254 (Electronic)
IS  - 0223-5234 (Linking)
VI  - 110
DP  - 2016 Mar 3
TI  - Identification of a diverse indole-2-carboxamides as a potent antileishmanial 
      chemotypes.
PG  - 237-45
LID - S0223-5234(16)30029-0 [pii]
LID - 10.1016/j.ejmech.2016.01.028 [doi]
AB  - A novel series of highly diverse indole-2-carboxamides was synthesized utilizing 
      the isocyanide based multicomponent reaction (IMCR)-post modification approach 
      and were identified as potential antileishmanial chemotype. Among the synthesized 
      18 analogues, 12 analogues exhibited better antileishmanial activity against 
      intracellular amastigotes form of Leishmania donovani (IC50 values of 0.6-7.5 muM) 
      as compared to standard drugs miltefosine and sodium stibogluconate. The 
      compounds were also non-toxic towards Vero cells. Compounds 2b, 2m and 2p with 
      significant in vitro activity were then evaluated for their in vivo efficacy 
      following intraperitoneal route. These three compounds at a concentration of 
      50 mg/kg/day for 5 consecutive days showed 70.0, 63.5 and 63.4% inhibition of 
      Leishmania amastigotes, respectively at day 7 post treatment in hamster model of 
      visceral leishmaniasis.
CI  - Copyright (c) 2016 Elsevier Masson SAS. All rights reserved.
FAU - Pandey, Shashi
AU  - Pandey S
AD  - Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, 
      Lucknow 226031, U.P., India.
FAU - Chauhan, Shikha S
AU  - Chauhan SS
AD  - Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, 
      Lucknow 226031, U.P., India.
FAU - Shivahare, Rahul
AU  - Shivahare R
AD  - Division of Parasitology, CSIR-Central Drug Research Institute, Lucknow 226031, 
      U.P., India.
FAU - Sharma, Abhisheak
AU  - Sharma A
AD  - Pharmacokinetics & Metabolism Division, CSIR-Central Drug Research Institute, 
      Lucknow 226031, U.P., India; Academy of Scientific and Innovative Research, New 
      Delhi, India.
FAU - Jaiswal, Swati
AU  - Jaiswal S
AD  - Pharmacokinetics & Metabolism Division, CSIR-Central Drug Research Institute, 
      Lucknow 226031, U.P., India; Academy of Scientific and Innovative Research, New 
      Delhi, India.
FAU - Gupta, Suman
AU  - Gupta S
AD  - Division of Parasitology, CSIR-Central Drug Research Institute, Lucknow 226031, 
      U.P., India.
FAU - Lal, Jawahar
AU  - Lal J
AD  - Pharmacokinetics & Metabolism Division, CSIR-Central Drug Research Institute, 
      Lucknow 226031, U.P., India; Academy of Scientific and Innovative Research, New 
      Delhi, India.
FAU - Chauhan, Prem M S
AU  - Chauhan PM
AD  - Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, 
      Lucknow 226031, U.P., India. Electronic address: prem_chauhan_2000@yahoo.com.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20160120
PL  - France
TA  - Eur J Med Chem
JT  - European journal of medicinal chemistry
JID - 0420510
RN  - 0 (Amides)
RN  - 0 (Antiprotozoal Agents)
RN  - 0 (Indoles)
SB  - IM
MH  - Amides/chemistry/pharmacokinetics/pharmacology/therapeutic use
MH  - Animals
MH  - Antiprotozoal Agents/*chemistry/pharmacokinetics/pharmacology/*therapeutic use
MH  - Cell Line
MH  - Chlorocebus aethiops
MH  - Cricetinae
MH  - Humans
MH  - Indoles/*chemistry/pharmacokinetics/pharmacology/*therapeutic use
MH  - Leishmania donovani/*drug effects
MH  - Leishmaniasis, Visceral/*drug therapy
MH  - Male
MH  - Mice
MH  - Rats, Sprague-Dawley
MH  - Structure-Activity Relationship
MH  - Vero Cells
OTO - NOTNLM
OT  - Hamster model
OT  - Indole-2-carboxamide
OT  - Leishmania donovani
OT  - Multicomponent reaction
EDAT- 2016/02/04 06:00
MHDA- 2016/11/01 06:00
CRDT- 2016/02/04 06:00
PHST- 2015/04/24 00:00 [received]
PHST- 2016/01/15 00:00 [revised]
PHST- 2016/01/16 00:00 [accepted]
PHST- 2016/02/04 06:00 [entrez]
PHST- 2016/02/04 06:00 [pubmed]
PHST- 2016/11/01 06:00 [medline]
AID - S0223-5234(16)30029-0 [pii]
AID - 10.1016/j.ejmech.2016.01.028 [doi]
PST - ppublish
SO  - Eur J Med Chem. 2016 Mar 3;110:237-45. doi: 10.1016/j.ejmech.2016.01.028. Epub 
      2016 Jan 20.