- Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists.
[作者：Ko, Hyojin;Carter, Rhonda L.;Cosyn, Liesbet;Petrelli, Riccardo;de Castro, Sonia;Besada, Pedro;Zhou, Yixing;Cappellacci, Loredana;Franchetti, Palmarisa;Grifantini, Mario;Van Calenbergh, Serge;Harden, T. Kendall;Jacobson, Kenneth A.;,期刊：Bioorganic & Medicinal Chemistry, 页码：6319-6332 , 文章类型： 研究论文，,卷期：2008年16-12]
- The phosphate, uracil, and ribose moieties of uracil nucleotides were varied structurally for evaluation of agonist activity at the human P2Y2, P2Y4, and P2Y6 receptors. The 2-thio modification, found previously to enha...
- Novel Azabicyclo[3.2.2]nonane derivatives and their activities against Plasmodium falciparum K1 and Trypanosoma brucei rhodesiense.
[作者：Berger, Heinrich;Weis, Robert;Kaiser, Marcel;Brun, Reto;Saf, Robert;Seebacher, Werner;,期刊：Bioorganic & Medicinal Chemistry, 页码：6371-6378 , 文章类型： 研究论文，,卷期：2008年16-12]
- New diaryl substituted 2-azabicyclo[3.2.2]nonane derivs. have been synthesized in order to investigate the influence of the arom. substitution and of N substitution on the antiprotozoal activities of those compds. Follo...
- Carbon-11 labeled indolylpropylamine analog as a new potential PET agent for imaging of the serotonin transporter.
[作者：Ben-Daniel, R.;Deuther-Conrad, W.;Scheunemann, M.;Steinbach, J.;Brust, P.;Mishani, E.;,期刊：Bioorganic & Medicinal Chemistry, 页码：6364-6370 , 文章类型： 研究论文，,卷期：2008年16-12]
- The synthesis and structure-activity relationship of a new class of indole derivs. with low-nanomolar affinity for the SERT and high selectivity vs. the 5-HT1A receptor were recently reported. Based on their chem. struc...
- Hybrids of 1-deoxynojirimycin and aryl-1,2,3-triazoles and biological studies related to angiogenesis.
[作者：Zhao, Yunxue;Zhou, Ying;O'Boyle, Kathy M.;Murphy, Paul V.;,期刊：Bioorganic & Medicinal Chemistry, 页码：6333-6337 , 文章类型： 研究论文，,卷期：2008年16-12]
- Hybrids of 1-deoxynojirimycin (DNJ) and aryl-1,2,3-triazole have been synthesized with a view to identifying an inhibitor of both a-glucosidase and methionine aminopeptidase 2 (MetAP2). One compd. was a potent inhibitor...
- Aroyl hydrazones of 2-phenylindole-3-carbaldehydes as novel antimitotic agents.
[作者：Vogel, Susanne;Kaufmann, Doris;Pojarova, Michaela;Mueller, Christine;Pfaller, Tobias;Kuehne, Sybille;Bednarski, Patrick J.;von Angerer, Erwin;,期刊：Bioorganic & Medicinal Chemistry, 页码：6436-6447 , 文章类型： 研究论文，,卷期：2008年16-12]
- Cell cycle arrest of malignant cells is an important option for cancer treatment. In this study, we modified the structure of antimitotic 2-phenylindole-3-carbaldehydes by condensation with hydrazides of various benzoic...
- Synthesis and in vitro biological activity of retinyl retinoate, a novel hybrid retinoid derivative.
[作者：Kim, Hyojung;Kim, Bora;Kim, Hyuk;Um, Soojong;Lee, Joodong;Ryoo, Heechang;Jung, Hyungil;,期刊：Bioorganic & Medicinal Chemistry, 页码：6387-6393 , 文章类型： 研究论文，,卷期：2008年16-12]
- A new hybrid, retinyl retinoate 1, was synthesized with a condensing reaction between retinol and retinoic acid to improve the photo-stability, and the in vitro biol. activity of the hybrid was analyzed. This retinol de...
- Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17b-hydroxysteroid dehydrogenase type 1 (17b-HSD1) for the treatment of estrogen-dependent diseases.
[作者：Bey, Emmanuel;Marchais-Oberwinkler, Sandrine;Kruchten, Patricia;Frotscher, Martin;Werth, Ruth;Oster, Alexander;Alguel, Oztekin;Neugebauer, Alexander;Hartmann, Rolf W.;,期刊：Bioorganic & Medicinal Chemistry, 页码：6423-6435 , 文章类型： 研究论文，,卷期：2008年16-12]
- The 17b-hydroxysteroid dehydrogenase type 1 (17b-HSD1) catalyzes the redn. of the weakly active estrone (E1) into the most potent estrogen, 17b-estradiol (E2). E2 stimulates the growth of hormone-dependent diseases via ...
- Design, synthesis and spectroscopic studies of resveratrol aliphatic acid ligands of human serum albumin.
[作者：Jiang, Yu Lin;,期刊：Bioorganic & Medicinal Chemistry, 页码：6406-6414 , 文章类型： 研究论文，,卷期：2008年16-12]
- As one of the natural polyphenols, resveratrol possesses hydroxyl substituted trans-stilbene structure and exerts impact on health by inhibiting multiple human enzymes, such as cyclooxygenase, F1 ATPase, and tyrosinase. ...
- Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.
[作者：Drizin, Irene;Gregg, Robert J.;Scanio, Marc J. C.;Shi, Lei;Gross, Michael F.;Atkinson, Robert N.;Thomas, James B.;Johnson, Matthew S.;Carroll, William A.;Marron, Brian E.;Chapman, Mark L.;Liu, Dong;Krambis, Michael J.;Shieh, Char-Chang;Zhang, XuFeng;Herna,期刊：Bioorganic & Medicinal Chemistry, 页码：6379-6386 , 文章类型： 研究论文，,卷期：2008年16-12]
- The synthesis and pharmacol. characterization of a novel furan-based class of voltage-gated sodium channel blockers is reported. Compds. were evaluated for their ability to block the tetrodotoxin-resistant sodium channe...
- Parallel one-pot synthesis and structure-activity relationship study of symmetric formimidoester disulfides as a novel class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
[作者：Cesarini, Sara;Spallarossa, Andrea;Ranise, Angelo;Schenone, Silvia;Bruno, Olga;La Colla, Paolo;Casula, Laura;Collu, Gabriella;Sanna, Giuseppina;Loddo, Roberta;,期刊：Bioorganic & Medicinal Chemistry, 页码：6353-6363 , 文章类型： 研究论文，,卷期：2008年16-12]
- The mol. duplication of non-nucleoside reverse transcriptase inhibitor (NNRTI) O-(2-phthalimidoethyl)-N-arylthiocarbamates (C-TCs) led to the identification of sym. formimidoester disulfides (DSs) as a novel class of pot...
- Synthesis and analgesic/anti-inflammatory evaluation of fused heterocyclic ring systems incorporating phenylsulfonyl moiety.
[作者：Shaaban, Mohamed R.;Saleh, Tamer S.;Mayhoub, Abdelrahman S.;Mansour, Ahmed;Farag, Ahmad M.;,期刊：Bioorganic & Medicinal Chemistry, 页码：6344-6352 , 文章类型： 研究论文，,卷期：2008年16-12]
- pyrimido[1,2-a]benzimidazole ring systems incorporating phenylsulfonyl moiety were synthesized via the reaction of 3-(N,N-dimethylamino)-1-aryl-2-(phenylsulfonyl)prop-2-en-1-one derivs. 2a,b with appropriate nitrogen nuc...
- Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
[作者：Wang, Chang-lin;Yao, Jin-long;Yu, Ye;Shao, Xuan;Cui, Yun;Liu, Hong-mei;Lai, Lu-hao;Wang, Rui;,期刊：Bioorganic & Medicinal Chemistry, 页码：6415-6422 , 文章类型： 研究论文，,卷期：2008年16-12]
- Endomorphin-2 (EM-2) is a putative endogenous m-opioid receptor ligand. To get insight into the important role of C-terminal amide group of EM-2, we investigated herein a series of EM-2 analogs by substitution of the C-...
- Chemometric and chemoinformatic analyses of anabolic and androgenic activities of testosterone and dihydrotestosterone analogues.
[作者：Alvarez-Ginarte, Yoanna Maria;Crespo-Otero, Rachel;Marrero-Ponce, Yovani;Noheda-Marin, Pedro;Garcia de la Vega, Jose Manuel;Montero-Cabrera, Luis Alberto;Ruiz Garcia, Jose Alberto;Caldera-Luzardo, Jose A.;Alvarado, Ysaias J.;,期刊：Bioorganic & Medicinal Chemistry, 页码：6448-6459 , 文章类型： 研究论文，,卷期：2008年16-12]
- anabolic and androgenic activities for the testosterone and dihydrotestosterone steroid analogs were obtained by means of multiple linear regression using quantum and physicochem. mol. descriptors (MD) as well as a genet...
|