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<p class="TitleMain">Modulation of morphology and efficacy of new CB1 receptor antagonist using simple and benign polymeric additives</p><br /><br />

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Title Statement <p class="TitleMain">Modulation of morphology and efficacy of new CB1 receptor antagonist using simple and benign polymeric additives</p><br /><br />
 
Added Entry - Uncontrolled Name Banerjee, Kaushik ; Department of Chemistry, Faculty of Science, The Maharaja Sayajirao University of Baroda, Vadodara 390 002, India
Patel, Darshit R; Piramal Healthcare, 403, Patel Avenue, Sarkhej - Gandhinagar Highway, Thaltej, Ahmedabad 380 054, India
Kulshrestha, Anchal ; Zydus Research Centre, Cadila Healthcare Ltd., Ahmedabad 382 213, India
Joshipura, Dhawal ; Zydus Research Centre, Cadila Healthcare Ltd., Ahmedabad 382 213, India
Joharapurkar, Amit ; Zydus Research Centre, Cadila Healthcare Ltd., Ahmedabad 382 213, India
Ghoshdastidar, Krishnarup ; Zydus Research Centre, Cadila Healthcare Ltd., Ahmedabad 382 213, India
Jain, Mukul R; Zydus Research Centre, Cadila Healthcare Ltd., Ahmedabad 382 213, India
Srivastava, Brijesh Kumar; Zydus Research Centre, Cadila Healthcare Ltd., Ahmedabad 382 213, India
Chakraborty, Mukut ; Department of Chemistry, West Bengal University, Barasat, Kolkata 700 126, India
Pattanayak, Sutanuka ; Department of Chemistry, West Bengal University, Barasat, Kolkata 700 126, India
Ballabh, Amar ; Department of Chemistry, Faculty of Science, The Maharaja Sayajirao University of Baroda, Vadodara 390 002, India
 
Uncontrolled Index Term Obesity, CB1 antagonist, crystallography, morphology, in vivo efficacy
 
Summary, etc. <p class="Abstract">The compound <strong>1</strong>, [(1<em>H</em>-[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 <strong>1</strong> displays a number of halogen bonds leading to 1-D network along with other weak non-covalent interactions. The CB1 modulator <strong>1</strong> 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 <strong>1</strong> 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 <strong>1</strong> 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 <strong>1</strong> adducts.</p><p class="Abstract" style="text-align: justify;"> </p>
 
Publication, Distribution, Etc. Indian Journal of Chemistry -Section B (IJC-B)
2021-10-05 10:39:28
 
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http://op.niscair.res.in/index.php/IJCB/article/view/29319
 
Data Source Entry Indian Journal of Chemistry -Section B (IJC-B); ##issue.vol## 60, ##issue.no## 7 (2021): Indian Journal of Chemistry- Section-B, (IJCB)
 
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Nonspecific Relationship Entry http://op.niscair.res.in/index.php/IJCB/article/download/29319/465490135
http://op.niscair.res.in/index.php/IJCB/article/download/29319/465490140
http://op.niscair.res.in/index.php/IJCB/article/download/29319/465490606
 
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