char = T;code = 84 char = -;code = 45 char = t;code = 116 char = y;code = 121 char = p;code = 112 char = e;code = 101 char = ;code = 32 char = c;code = 99 char = a;code = 97 char = l;code = 108 char = c;code = 99 char = i;code = 105 char = u;code = 117 char = m;code = 109 char = ;code = 32 char = c;code = 99 char = h;code = 104 char = a;code = 97 char = n;code = 110 char = n;code = 110 char = e;code = 101 char = l;code = 108 char = ;code = 32 char = b;code = 98 char = l;code = 108 char = o;code = 111 char = c;code = 99 char = k;code = 107 char = e;code = 101 char = r;code = 114 char = s;code = 115 char = :;code = 58 char = ;code = 32 char = s;code = 115 char = p;code = 112 char = i;code = 105 char = r;code = 114 char = o;code = 111 char = -;code = 45 char = p;code = 112 char = i;code = 105 char = p;code = 112 char = e;code = 101 char = r;code = 114 char = i;code = 105 char = d;code = 100 char = i;code = 105 char = n;code = 110 char = e;code = 101 char = ;code = 32 char = a;code = 97 char = z;code = 122 char = e;code = 101 char = t;code = 116 char = i;code = 105 char = d;code = 100 char = i;code = 105 char = n;code = 110 char = e;code = 101 char = s;code = 115 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = a;code = 97 char = z;code = 122 char = e;code = 101 char = t;code = 116 char = i;code = 105 char = d;code = 100 char = i;code = 105 char = n;code = 110 char = o;code = 111 char = n;code = 110 char = e;code = 101 char = s;code = 115 char = -;code = 45 char = o;code = 111 char = p;code = 112 char = t;code = 116 char = i;code = 105 char = m;code = 109 char = i;code = 105 char = z;code = 122 char = a;code = 97 char = t;code = 116 char = i;code = 105 char = o;code = 111 char = n;code = 110 char = ,;code = 44 char = ;code = 32 char = d;code = 100 char = e;code = 101 char = s;code = 115 char = i;code = 105 char = g;code = 103 char = n;code = 110 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = s;code = 115 char = y;code = 121 char = n;code = 110 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = s;code = 115 char = i;code = 105 char = s;code = 115 char = .;code = 46 result sql = T-type calcium channel blockers: spiro-piperidine azetidines and azetidinones-optimization, design and synthesis.
T-type calcium channel blockers: spiro-piperidine azetidines and azetidinones-optimization, design and synthesis.char = A;code = 65 char = ;code = 32 char = s;code = 115 char = e;code = 101 char = r;code = 114 char = i;code = 105 char = e;code = 101 char = s;code = 115 char = ;code = 32 char = o;code = 111 char = f;code = 102 char = ;code = 32 char = s;code = 115 char = p;code = 112 char = i;code = 105 char = r;code = 114 char = o;code = 111 char = -;code = 45 char = a;code = 97 char = z;code = 122 char = e;code = 101 char = t;code = 116 char = i;code = 105 char = d;code = 100 char = i;code = 105 char = n;code = 110 char = e;code = 101 char = s;code = 115 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = a;code = 97 char = z;code = 122 char = e;code = 101 char = t;code = 116 char = i;code = 105 char = d;code = 100 char = i;code = 105 char = n;code = 110 char = o;code = 111 char = n;code = 110 char = e;code = 101 char = s;code = 115 char = ;code = 32 char = h;code = 104 char = a;code = 97 char = s;code = 115 char = ;code = 32 char = b;code = 98 char = e;code = 101 char = e;code = 101 char = n;code = 110 char = ;code = 32 char = e;code = 101 char = v;code = 118 char = a;code = 97 char = l;code = 108 char = u;code = 117 char = a;code = 97 char = t;code = 116 char = e;code = 101 char = d;code = 100 char = ;code = 32 char = a;code = 97 char = s;code = 115 char = ;code = 32 char = n;code = 110 char = o;code = 111 char = v;code = 118 char = e;code = 101 char = l;code = 108 char = ;code = 32 char = b;code = 98 char = l;code = 108 char = o;code = 111 char = c;code = 99 char = k;code = 107 char = e;code = 101 char = r;code = 114 char = s;code = 115 char = ;code = 32 char = o;code = 111 char = f;code = 102 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = ;code = 32 char = T;code = 84 char = -;code = 45 char = t;code = 116 char = y;code = 121 char = p;code = 112 char = e;code = 101 char = ;code = 32 char = c;code = 99 char = a;code = 97 char = l;code = 108 char = c;code = 99 char = i;code = 105 char = u;code = 117 char = m;code = 109 char = ;code = 32 char = c;code = 99 char = h;code = 104 char = a;code = 97 char = n;code = 110 char = n;code = 110 char = e;code = 101 char = l;code = 108 char = ;code = 32 char = (;code = 40 char = C;code = 67 char = a;code = 97 char = (;code = 40 char = V;code = 86 char = );code = 41 char = 3;code = 51 char = .;code = 46 char = 2;code = 50 char = );code = 41 char = ;code = 32 char = w;code = 119 char = h;code = 104 char = i;code = 105 char = c;code = 99 char = h;code = 104 char = ;code = 32 char = i;code = 105 char = s;code = 115 char = ;code = 32 char = a;code = 97 char = ;code = 32 char = n;code = 110 char = e;code = 101 char = w;code = 119 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = r;code = 114 char = a;code = 97 char = p;code = 112 char = e;code = 101 char = u;code = 117 char = t;code = 116 char = i;code = 105 char = c;code = 99 char = ;code = 32 char = t;code = 116 char = a;code = 97 char = r;code = 114 char = g;code = 103 char = e;code = 101 char = t;code = 116 char = ;code = 32 char = f;code = 102 char = o;code = 111 char = r;code = 114 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = ;code = 32 char = p;code = 112 char = o;code = 111 char = t;code = 116 char = e;code = 101 char = n;code = 110 char = t;code = 116 char = i;code = 105 char = a;code = 97 char = l;code = 108 char = ;code = 32 char = t;code = 116 char = r;code = 114 char = e;code = 101 char = a;code = 97 char = t;code = 116 char = m;code = 109 char = e;code = 101 char = n;code = 110 char = t;code = 116 char = ;code = 32 char = o;code = 111 char = f;code = 102 char = ;code = 32 char = b;code = 98 char = o;code = 111 char = t;code = 116 char = h;code = 104 char = ;code = 32 char = i;code = 105 char = n;code = 110 char = f;code = 102 char = l;code = 108 char = a;code = 97 char = m;code = 109 char = m;code = 109 char = a;code = 97 char = t;code = 116 char = o;code = 111 char = r;code = 114 char = y;code = 121 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = n;code = 110 char = e;code = 101 char = u;code = 117 char = r;code = 114 char = o;code = 111 char = p;code = 112 char = a;code = 97 char = t;code = 116 char = h;code = 104 char = i;code = 105 char = c;code = 99 char = ;code = 32 char = p;code = 112 char = a;code = 97 char = i;code = 105 char = n;code = 110 char = .;code = 46 char = ;code = 32 char = C;code = 67 char = o;code = 111 char = n;code = 110 char = f;code = 102 char = i;code = 105 char = r;code = 114 char = m;code = 109 char = a;code = 97 char = t;code = 116 char = i;code = 105 char = o;code = 111 char = n;code = 110 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = o;code = 111 char = p;code = 112 char = t;code = 116 char = i;code = 105 char = m;code = 109 char = i;code = 105 char = z;code = 122 char = a;code = 97 char = t;code = 116 char = i;code = 105 char = o;code = 111 char = n;code = 110 char = ;code = 32 char = o;code = 111 char = f;code = 102 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = ;code = 32 char = p;code = 112 char = o;code = 111 char = t;code = 116 char = e;code = 101 char = n;code = 110 char = c;code = 99 char = y;code = 121 char = ,;code = 44 char = ;code = 32 char = s;code = 115 char = e;code = 101 char = l;code = 108 char = e;code = 101 char = c;code = 99 char = t;code = 116 char = i;code = 105 char = v;code = 118 char = i;code = 105 char = t;code = 116 char = y;code = 121 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = D;code = 68 char = M;code = 77 char = P;code = 80 char = K;code = 75 char = ;code = 32 char = p;code = 112 char = r;code = 114 char = o;code = 111 char = p;code = 112 char = e;code = 101 char = r;code = 114 char = t;code = 116 char = i;code = 105 char = e;code = 101 char = s;code = 115 char = ;code = 32 char = o;code = 111 char = f;code = 102 char = ;code = 32 char = l;code = 108 char = e;code = 101 char = a;code = 97 char = d;code = 100 char = s;code = 115 char = ;code = 32 char = w;code = 119 char = i;code = 105 char = l;code = 108 char = l;code = 108 char = ;code = 32 char = b;code = 98 char = e;code = 101 char = ;code = 32 char = d;code = 100 char = e;code = 101 char = s;code = 115 char = c;code = 99 char = r;code = 114 char = i;code = 105 char = b;code = 98 char = e;code = 101 char = d;code = 100 char = .;code = 46 char = <;code = 60 char = b;code = 98 char = r;code = 114 char = /;code = 47 char = >;code = 62 result sql = A series of spiro-azetidines and azetidinones has been evaluated as novel blockers of the T-type calcium channel (Ca(V)3.2) which is a new therapeutic target for the potential treatment of both inflammatory and neuropathic pain. Confirmation and optimization of the potency, selectivity and DMPK properties of leads will be described.
Publication: Bioorg. Med. Chem. Lett. 2010 Aug 1 ;20(15)::4602-6. :doi: 10.1016/j.bmcl.2010.06.012.
Publication Date: 2010 Aug 1
Study Author(s): Smith, Elizabeth M;Sorota, Steve;Kim, Hyunjin M;McKittrick, Brian A;Nechuta, Terry L;Bennett, Chad;Knutson, Chad;Burnett, Duane A;Kieselgof, Jane;Tan, Zheng;Rindgen, Diane;Bridal, Terry;Zhou, Xiaoping;Jia, Yu-Ping;Dong, Zoe;Mullins, Debbie;Zhang, Xiaoping;Priestley, Tony;Correll, Craig C;Tulshian, Deen;Czarniecki, Michael;Greenlee, William J;
Institution: Department of Medicinal Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, USA.
[email protected]
Shortcut link to this study:
A series of spiro-azetidines and azetidinones has been evaluated as novel blockers of the T-type calcium channel (Ca(V)3.2) which is a new therapeutic target for the potential treatment of both inflammatory and neuropathic pain. Confirmation and optimization of the potency, selectivity and DMPK properties of leads will be described.