- Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38 alpha mitogen-activated protein kinase
[作者：Wurz, RP; Pettus, LH; Xu, SM; Henkle, B; Sherman, L; Plant, M; Miner, K; McBride, H; Wong, LM; Saris, CJM; Lee, MR; Chmait, S; Mohr, C; Hsieh, F; Tasker, AS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4724-4728 , 文章类型： Article，,卷期：2009年19-16]
- A novel class of fused pyrazole-derived inhibitors of p38 alpha mitogen-activated protein kinase (MAPK) is disclosed. These inhibitors were evaluated for their ability to inhibit the p38a enzyme, the secretion of TNF alp...
- Identification of MK-1925: A selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist
[作者：Kobayashi, K; Tsujita, T; Ito, H; Ozaki, S; Tani, T; Ishii, Y; Okuda, S; Tadano, K; Fukuroda, T; Ohta, H; Okamoto, O,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4729-4732 , 文章类型： Article，,卷期：2009年19-16]
- Structure-activity relationship studies directed toward improving the metabolic stability of compound 1 resulted in the identification of 3-[5-(3,5-difluorophenyl)-3-({[(1S,3R)-3-fluorocyclopentyl]amino}methyl)-4-methyl-...
- FXR agonist activity of conformationally constrained analogs of GW 4064
[作者：Akwabi-Ameyaw, A; Bass, JY; Caldwell, RD; Caravella, JA; Chen, LH; Creech, KL; Deaton, DN; Madauss, KP; Marr, HB; McFadyen, RB; Miller, AB; Navas, F; Parks, DJ; Spearing, PK; Todd, D; Williams, SP; Wisely, GB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4733-4739 , 文章类型： Article，,卷期：2009年19-16]
- Two series of conformationally constrained analogs of the FXR agonist GW 4064 1 were prepared. Replacement of the metabolically labile stilbene with either benzothiophene or naphthalene rings led to the identification of...
- The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists
[作者：Bell, IM; Bednar, RA; Corcoran, HA; Fay, JF; Gallicchio, SN; Johnston, VK; Hershey, JC; Miller-Stein, CM; Moore, EL; Mosser, SD; Roller, SA; Salvatore, CA; Theberge, CR; Wong, BK; Zartman, CB; Kane, SA; Williams, TM; Graham, SL; Vacca, JP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4740-4742 , 文章类型： Article，,卷期：2009年19-16]
- A series of tricyclic CGRP receptor antagonists was optimized in order to improve oral bioavailability. Attenuation of polar surface area and incorporation of a weakly basic indoline nitrogen led to compound 5, a potent ...
- Synthesis and optimization of 2-pyridin-3-yl-benzo[d][1,3]oxazin-4-one based inhibitors of human neutrophil elastase
[作者：Shreder, KR; Cajica, J; Du, LL; Fraser, A; Hu, Y; Kohno, Y; Lin, ECK; Liu, SJ; Okerberg, E; Pham, L; Wu, JY; Kozarich, JW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4743-4746 , 文章类型： Article，,卷期：2009年19-16]
- The hit-to-lead optimization of the HNE inhibitor 5-methyl-2-(2-phenoxy-pyridin-3-yl)-benzo[d][1,3]oxazin-4-one is described. A structure-activity relationship study that focused on the 5 and 7 benzoxazinone positions yi...
- Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates - subtype selective, high affinity alpha 7 nicotinic acetylcholine receptor agonists
[作者：O'Donnell, CJ; Peng, LG; O'Neill, BT; Arnold, EP; Mather, RJ; Sands, SB; Shrikhande, A; Lebel, LA; Spracklin, DK; Nedza, FM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4747-4751 , 文章类型： Article，,卷期：2009年19-16]
- The synthesis and SAR studies about the bicyclic amine, carbamate linker and aromatic ring of a 1,4-diazabicyclo[3.2.2]nonane phenyl carbamate series of alpha 7 nAChR agonists is described. The development of the medicin...
- Synthesis, characterization, and anti-melanoma activity of tetra-O-substituted analogs of nordihydroguaiaretic acid
[作者：Meyers, RO; Lambert, JD; Hajicek, N; Pourpak, A; Kalaitzis, JA; Dorr, RT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4752-4755 , 文章类型： Article，,卷期：2009年19-16]
- Synthesis of seven semi-synthetic analogs of NDGA is described. An approach to NDGA derivatization is described in which the ortho-phenolic groups are tethered together by one atom, forming a 5-membered heterocyclic ring...
- Isolation, enzyme-bound structure and antibacterial activity of platencin A(1) from Streptomyces platensis
[作者：Singh, SB; Ondeyka, JG; Herath, KB; Zhang, CW; Jayasuriya, H; Zink, DL; Parthasarathy, G; Becker, JW; Wang, J; Soisson, SM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4756-4759 , 文章类型： Article，,卷期：2009年19-16]
- Natural products continue to serve as one of the best sources for discovery of antibacterial agents as exemplified by the recent discoveries of platensimycin and platencin. Chemical modifications as well as discovery of ...
- Synthesis of radiolabeled cytarabine conjugates
[作者：Lagisetty, P; Vilekar, P; Awasthi, V,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4764-4767 , 文章类型： Article，,卷期：2009年19-16]
- N4-Modified, novel Ara-C conjugate capable of radiolabeling with gamma ray-emitting (Tc-99m) as well as positron emitting (F-18) radionuclides, that is, N4-hydrazine derivative was synthesized. The radiolabeling of N4-(h...
- Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia
[作者：Schmidt, D; Smenton, A; Raghavan, S; Carballo-Jane, E; Lubell, S; Ciecko, T; Holt, TG; Wolff, M; Taggart, A; Wilsie, L; Krsmanovic, M; Ren, N; Blom, D; Cheng, K; McCann, PE; Waters, MG; Tata, J; Colletti, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4768-4772 , 文章类型： Article，,卷期：2009年19-16]
- Niacin is an effective drug for raising HDL cholesterol and reducing coronary risks, but patients show low compliance with treatment due to severe facial flushing upon taking the drug. A series of bicyclic pyrazole carbo...
- Novel derivatives of ISO-1 as potent inhibitors of MIF biological function
[作者：Balachandran, S; Rodge, A; Gadekar, PK; Yadav, VN; Kamath, D; Chetrapal-Kunwar, A; Bhatt, P; Srinivasan, S; Sharma, S; Vishwakarma, RA; Dagia, NM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4773-4776 , 文章类型： Article，,卷期：2009年19-16]
- A series of novel 1,2,4-oxadiazole, phthalimide, amide and other derivatives of ISO-1 were synthesized and probed for inhibition of macrophage migration inhibitory factor (MIF) activity. Several compounds inhibited MIF e...
- Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists
[作者：Thompson, SK; Washburn, DG; Frazee, JS; Madauss, KP; Hoang, TH; Lapinski, L; Grygielko, ET; Glace, LE; Trizna, W; Williams, SP; Duraiswami, C; Bray, JD; Laping, NJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4777-4780 , 文章类型： Article，,卷期：2009年19-16]
- Using the X-ray crystal structure of an amide-based progesterone receptor (PR) partial agonist bound to the PR ligand binding domain, a novel PR partial agonist class containing a pyrrolidine ring was designed. Members o...
- Design, synthesis and evaluation of a novel cyclohexanamine class of neuropeptide Y Y1 receptor antagonists
[作者：Cho, K; Ando, M; Kobayashi, K; Miyazoe, H; Tsujino, T; Ito, S; Suzuki, T; Tanaka, T; Tokita, S; Sato, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4781-4785 , 文章类型： Article，,卷期：2009年19-16]
- A novel series of cyclohexanamine derivatives was designed and synthesized as potent and selective human neuropeptide Y Y1 receptor antagonists. Modification of high-throughput screening hit compound 1 resulted in the id...
- Efficient synthesis of 3,3-diheteroaromatic oxindole analogues and their in vitro evaluation for spermicidal potential
[作者：Paira, P; Hazra, A; Kumar, S; Paira, R; Sahu, KB; Naskar, S; Saha, P; Mondal, S; Maity, A; Banerjee, S; Mondal, NB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4786-4789 , 文章类型： Article，,卷期：2009年19-16]
- Syntheses of 3,3-diheteroaromatic oxindole derivatives has been achieved by coupling indole-2,3-dione (isatin) with differently substituted indoles and pyrrole in presence of I-2 in i-PrOH. The in vitro spermicidal poten...
- Functionalized 3-amino-imidazo[1,2-a]pyridines: A novel class of drug-like Mycobacterium tuberculosis glutamine synthetase inhibitors
[作者：Odell, LR; Nilsson, MT; Gising, J; Lagerlund, O; Muthas, D; Nordqvist, A; Karlen, A; Larhed, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4790-4793 , 文章类型： Article，,卷期：2009年19-16]
- 3-Amino-imidazo[1,2-a]pyridines have been identified as a novel class of Mycobacterium tuberculosis glutamine synthetase inhibitors. Moreover, these compounds represent the first drug-like inhibitors of this enzyme. A se...
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