Record Details

Modulation of morphology and efficacy of new CB1 receptor antagonist using simple and benign polymeric additives

NOPR - NISCAIR Online Periodicals Repository

View Archive Info
 
 
Field Value
 
Title Modulation of morphology and efficacy of new CB1 receptor antagonist using simple and benign polymeric additives
 
Creator Banerjee, Kaushik
Patel, Darshit R
Kulshrestha, Anchal
Joshipura, Dhawal
Joharapurkar, Amit
Ghoshdastidar, Krishnarup
Jain, Mukul R
Srivastava, Brijesh Kumar
Chakraborty, Mukut
Pattanayak, Sutanuka
Ballabh, Amar
 
Subject Obesity
CB1 antagonist
crystallography
morphology
in vivo efficacy
 
Description 1014-1021
The compound 1, [(1H-[1]benzoxepino[5,4-c]pyrazole-3-carboxamide, 8-chloro-1-(2,4-dichlorophenyl)-4,5-dihydro-N-
1-piperidinyl], a known CB1 modulator has been synthesized and characterized by IR, NMR and single Crystal X-ray study.
The single crystal study of 1 displays a number of halogen bonds leading to 1-D network along with other weak noncovalent
interactions. The CB1 modulator 1 inherently possesses extremely low solubility in water, which makes its
application as drug difficult, and this may be attributed to multiple halogen bonds present in the crystal structure. A series of
polymer additives, which are Generally Regarded As Safe (GRAS), have been explored to investigate whether they can
modulate the halogen bond present in 1 through formation of various non-bonded interactions. Surprisingly, these polymers
are found to change crystal morphology, crystal packing while retaining efficacy and bioavailability. The polymer molecular
weight is found to play a significant role in crystal morphology modification especially in case of polyethylene glycol
(PEG). The formation of new polymorphic forms of 1 and modification of halogen bond has been established using powder
X-ray diffraction and IR study, respectively, in case of PEG 4000, PVPK-30, PVA polymers and compound 1 adducts.
 
Date 2021-09-29T07:14:03Z
2021-09-29T07:14:03Z
2021-07
 
Type Article
 
Identifier 0975-0983(Online); 0376-4699(Print)
http://nopr.niscair.res.in/handle/123456789/58176
 
Language en
 
Publisher NIScPR-CSIR, India
 
Source IJC-B Vol.60B(07) [July 2021]