TECHNICAL PROGRAM - American Chemical Society Publications

MEDI TECHNICAL PROGRAM
383. Identification and structure-activity relationships
of 2,6-disubstituted pyrazines
as antituberculosis agents. Y. Sun,
V. Petukhova, R. S. Giri, L. L. Klein,
Y. Song, N. Zhang, K. Peng, B. Wan,
Y. Wang, S. G. Franzblau
384. Highly potent and selective inhibitors
for Cryptosporidium parvum inosine 5�monophosphate
dehydrogenase: SAR
and anticryptosporidial activity.
S. K. Gorla, M. Kavitha, M. Zhang, X. Liu,
L. Sharling, I. S. MacPherson,
D. R. Gollapalli, B. Striepen, G. Cuny,
L. Hedstrom
385. Antifungal agents from multivalent antimicrobial
peptides design. A. Young,
S. Safir, C. Zhou, N. Kallenbach
386. Synthesis of pyridone-based glucokinase
activators. K. J. Filipski,
C. S. Jones, M. L. Minich, S. W. Wright,
J. Li, A. Guzman-Perez, J. A. Pfefferkorn
387. Development of diaryl ether-based ligands
for estrogen-related receptor � as
potential anti-diabetic agents.
R. J. Patch, L. L. Searle, A. J. Kim, D. De,
X. Zhu, H. B. Askari, J. C. O’Neill,
M. C. Abad, D. Rentzeperis, J. G. Geisler,
J. M. Lenhard, M. R. Player, M. D. Gaul
388. Pyrimidine carboxamides as potent and
selective CCK1R agonists. L. Wang,
Z. Chen, T. G. Holt, J. A. Hubert,
B. V. Karanam, S. J. Lee, J. Pan, S. Qian,
V. B. Reddy, M. L. Reitman, A. M. Strack,
V. Tong, D. T. Weingarth, M. S. Wolff,
D. J. MacNeil, A. E. Weber,
S. D. Edmondson
389. Discovery of new phenylthiazolyl
PPARa/d selective agonists.
M. Dubernet, J. Delhomel,
A. Rubenstrunk, R. Walczak,
K. Bertrand-Caumont, D. W. Hum
390. Discovery of a potent, proteolytically
stable, and cell permeable human SIRT1
and SIRT2 peptidomimetic inhibitor containing
N e -thioacetyl-lysine.
B. M. Hirsch, C. A. Gallo, Z. Du, Z. Wang,
W. Zheng
391. Antileishmanial activities of new histone
deacetylase inhibitors.
C. Erlanson-Albertsson
392. Discovery of aminopyrimidine derivatives
as novel GPR119 receptor agonists.
Y. Yonetoku, K. Negoro, K. Onda,
M. Hayakawa, D. Sasuga, T. Nigawara,
K. Iikubo, K. Yonezawa, H. Moritomo,
T. Matsui, S. Yoshida, H. Tanaka,
T. Ohishi, H. Kayakiri, M. Ohta,
M. Takeuchi
393. 6-Amino-4-(pyrimidin-4-yl)pyridones:
Novel glycogen synthase kinase-3b inhibitors.
K. Coffman, M. Brodney,
J. Cook, L. Lanyon, J. Pandit, S. Sakya,
J. Schachter, E. Tseng-Lovering,
M. Wessel
394. Strategy to control hERG activity of
brain penetrant Melanin-concentrating
hormone 1 receptor (MCH1r) antagonists.
Y. Jiang, B. Chen, S. Hong,
E. M. Eldemenky, K. Lu, M. R. Marzabadi,
B. Li, H. Zhang, K. A. Jones, A. D. White,
M. Labelle
395. Diamine template as novel Melaninconcentrating
hormone 1 receptor
(MCH1r) antagonists with improved cardiovascular
safety. Y. Jiang, C. Chen,
B. Chen, E. M. Eldemenky, C. G. Mazza,
N. Ray, M. R. Marzabadi, C. Forray, B. Li,
H. Zhang, K. A. Jones, D. Dong,
G. Chandrasena, D. A. Craig, X. Ping,
K. Andersen
396. Design and synthesis of fluorescent
compounds as a new class of antagonists
targeting PPAR�. Y. Liu,A.Wang,
Y. A. Tomita, S. Dakshanamurth,
R. I. Glazer, M. L. Brown, Y. Kong
397. Design, synthesis and QSAR study of
novel 2-(2, 3-dioxo-2, 3-dihydro-1H-indol-1-yl)-N-phenylacetamide
derivatives
as cytotoxic agents. R. J. Shah,
N. R. Modi, L. J. Patel
398. Extraction of chemical information from
documents. H. O. Villar, J. Betancort,
M. R. Hansen
80–TECH
‡ Cooperative Cosponsorship
399. Application of the interligand Overhauser
effect to fragment linking and
screening. P. Sledz,A.W.Hung,
H. L. Silvestre, S. Wen, A. Ciulli,
T. L. Blundell, C. Abell
400. Covalent inhibitor design: Quantum mechanical
calculation of electrophilicity for
optimization of bond-forming functional
groups. z. Zhu, K. N. Houk, E. Krenske,
J. Singh, M. Labenski, K. Lee,
R. C. Petter
401. CoMFA analysis of pyrrolo[2,3-d]pyrimidines
and furo[2,3-d]pyrimidines as multiple
receptor tyrosine kinase inhibitors.
A. Gangjee, S. Raghavan
402. Trainable QSAR model of plasma protein
binding and its application for predicting
volume of distribution.
K. Lanevskij, R. Didziapetris, P. Japertas
403. Approach to quick lead optimization including
physicochemical and ADME profiling.
P. Japertas, A. Sazonovas,
K. Lanevskij, K. Kassam
404. How internal data marries public information
in chemical and biological universes
in drug discovery. P. Liu,
D. Rassokhin, D. K. Agrafiotis
405. Using open source descriptors and algorithms
for modeling ADME properties.
R. R. Gupta, E. M. Gifford, T. Liston,
C. Waller, B. Bunin, S. Ekins
406. Design and synthesis of deuterated erlotinib
analogs with enhanced pharmacokinetic
properties. C. E. Masse,
R. Gallegos, V. Uttamsingh,
A. J. Morales, S. Harbeson, R. Tung
407. Third-generation synthetic inhibitors of
plasminogen activator inhibitor-1.
C. G. Vaghela, J. M. Lisi,
N. C. El-Ayache, P. R. North,
K. L. Sanders, M. Warnock, S. Li,
D. A. Lawrence, C. D. Emal
408. Design, synthesis, structure-activity relationships
and biological evaluation of
phenolic inhibitors of plasminogen activator
inhibitor-1. K. L. Sanders,
H. Y. Saraha, G. A. Abernathy,
N. C. El-Ayache, S. Li, M. Warnock,
D. A. Lawrence, C. D. Emal
409. Discovery of new lead tetrapeptides reversible
inhibitors of thrombin using 2Dtransferred
NOESY NMR. C. C. Clement,
M. Philipp
410. Chemoenzymatic route to uncommon
sugar nucleotides. L. Cai, W. Guan,
P. G. Wang
411. Triarylcarboxylic acid derivatives as
novel xanthine oxidase inhibitors.
J. Miyata, H. Kubota, K. Hattori,
T. Asano, J. Watanabe, R. Munakata,
A. Kamikawa, M. Kageyama, R. Naito,
M. Kawakami, M. Takeuchi, M. Ohta
412. Synthesis of carbon-11-labeled cholesterol-based
cationic lipids as new potential
PET probes for imaging of gene delivery.
M. Gao, M. Wang, G. D. Hutchins,
Q. Zheng
413. Automating gradient method development
in flash chromatography for greater
productivity and minimizing solvent use.
A. Lesniowski, D. McCreary,
S. Anderson, K. Lawrence
414. Biosensor detection of early onset septicemia.
S. K. Hasan, S. Ammu,
S. K. Manohar
415. Synthesis and biological evaluation of
nitroxide-functionalized silica nanoparticles.
M. M. Sprachman, A. H. Faraji,
W. Feng, V. Kagan, P. Wipf
416. Synthesis and evaluation of fluorine
substituted CGRP receptor antagonists
for the development of an 18 F PET imaging
agent. J. J. Kim,M.R.Wood,
K. M. Schirripa, E. Hostetler, S. Sanabria,
C. Sur, D. L. Williams, Z. Zeng,
L. L. Gammage, M. Williams, J. J. Cook,
E. L. Moore, M. S. Michener, J. F. Fay,
S. D. Mosser, R. B. White, J. G. Bruno,
C. A. Salvatore, S. A. Kane, H. G. Selnick,
S. L. Graham
417. RevealX technology improves isolation
and purification of natural products
by flash chromatography. R. Bose,
S. Anderson, K. Lawrence
418. RevealX technology improves purification
of lead generation compounds by
flash chromatography. R. Bose,
S. Anderson, K. Lawrence
419. Development of an analytical method
for the production and measurement of
singlet oxygen. S. L. Pena, L. Rivera,
O. Perales, S. Singh
420. Discovery of dihydroindolyl azetidine
derivatives as potent MCH antagonists
with low PgP efflux. S. Hong,
G. Chandrasena, B. Chen, E. Eldemenky,
A. Husain, Y. Jiang, K. Jones, M. Labelle,
B. Li, K. Lu, G. Ma, M. Marzabadi,
C. Mazza, S. Miller, M. Packiarajan,
M. Sabio, D. Smith, A. D. White, L. Wu
421. Novel ammonium prodrug: Synthesis,
pharmacokinetics, mechanism of release
and scope. A. Regueiro-Ren,
S. M. Jenkins, S. Kim, K. Mosure,
S. Rahematpura, J. Simmermacher,
M. Sinz, M. Zheng, K. Johnson,
N. A. Meanwell, J. F. Kadow
422. Hydrolytic properties of thymidine �-Pboranophosphate
analogs. Z. Xu,
B. R. Shaw
423. Synthesis of sulfonyl curcumin mimics
exerting a vasodilatation effect on the
basilar artery of rabbits. C. Ahn,B.Park,
H. Woo, J. Ham, W. Shin, S. Lee
424. Computed tomography (CT) contrast
agents for determining cartilage health.
R. C. Stewart, P. N. Bansal, N. S. Joshi,
V. Entezari, B. C. Malone, B. D. Snyder,
M. W. Grinstaff
425. Design and optimization of benzimidazole-containing
cold menthol receptor
(TRPM8) antagonists. D. J. Parks,
R. R. Calvo, W. H. Parsons, S. Meegalla,
S. K. Ballentine, J. Chen, C. R. Illig,
D. J. Stone, N. Qin, T. L. Hutchinson,
M. Lubin, Y. Liu, J. Baker, R. W. Colburn,
C. M. Flores, M. R. Player
426. Dendrimer based CT contrast agents
for GAG quantification. S. E. Stidham,
M. W. Grinstaff
427. Synthesis, functionalization and photo-
Bergman chemistry of enediyne bioconjugates.
K. M. Wager,G.B.Jones
428. Discovery, synthesis and biological
evaluation of pyrrole derivatives as novel
and highly selective potassium-competitive
acid blockers (P-CABs). H. Nishida,
A. Hasuoka, Y. Arikawa, O. Kurasawa,
K. Hirase, N. Inatomi, Y. Hori, F. Sato,
N. Tarui, A. Imanishi, M. Kondo, S. Endo,
T. Takagi, M. Kajino
429. Drug-like properties of macrocyclic
molecules derived from DNA-programmed
combinatorial libraries.
B. Seigal, F. Favaloro Jr., T. F. Briggs,
R. Sandberg-Diment, J. Furr, S. Hale,
N. Terrett
430. Optimization of affinity and relaxity of
peptide-based fibrin-targeted MRI contrast
agents via N-terminal PNA modification.
Z. Zhang, M. Greenfield,
A. Kolodziej, P. Caravan
431. Electrochemical reactivity and interactions
of quercetin with DNA in the presence
of Cu(II) ions. S. Cutler,
M. Stobiecka, M. Hepel
432. Crystal structures and hydrogen bonding
patterns in some Schiff Bases of
pharmacological importance.
J. P. Jasinski, R. J. Butcher,
A. N. Mayekar, H. S. Yathirajan,
B. Narayna
433. Synthesis of new hybrid materials designed
for iron selective electrodes based
on selective amino spacer organizations.
P. Rouge, M. Becuwe,
A. Dassonville-Klimpt, A. Jonet,
M. Benazza, C. Guery, E. Baudrin,
P. Sonnet
434. Crystal structures and hydrogen bonding
patterns in picrate salts of pharmacologically
active compounds-I.
J. P. Jasinski, R. J. Butcher,
Q. Hakim Al-arique, H. S. Yathirajan,
B. Narayana
435. Crystal structures and hydrogen bonding
patterns in picrates salts of pharmacologically
active compounds-II.
J. P. Jasinski, R. J. Butcher,
H. S. Yathirajan, B. Narayana,
K. Prakash Kamath
436. Effect of molecular charge in computed
tomography imaging agents. H. Lusic,
N. S. Joshi, R. C. Stewart, P. N. Bansal,
B. D. Snyder, M. W. Grinstaff
437. Structural characterization and biological
activities of various soluble beta-1,3/
1,6-glucans. N. Bose, A. S. Chan,
M. E. Danielson,C.M.Dudney,
N. Elmasry, K. B. Gorden, F. O. Guerrero,
R. R. Langeslay, A. S. Magee,
C. M. Maristany, J. P. Vasilakos,
R. M. Walsh, P. M. Will, L. R. Wurst
438. Annonacin isolated from Asimina triloba
fruit pulp is toxic to rat primary cortical
neurons. L. F. Potts, F. A. Luzzio,
I. Litvan, M. Hetman
439. Identification of piperazine-bisamide
GHSR antagonists for the treatment of
obesity: Transformation from agonist to
antagonist. M. Yu, M. Lizarzaburu,
H. Beckmann, R. Connors, K. Dai, C. Li,
L. Liang, M. Wanska, L. Li, J. C. Medina
440. Withdrawn
441. N-oxyde aurones as new, potent and
non-toxic tyrosinase inhibitors.
R. Haudecoeur, C. Dubois,
A. Boumendjel, C. Belle, M. Réglier
442. Synthesis and photophysical characterization
of novel lanthanide-ion based luminescent
probes for ultrasensitive detection
of biopolymers. L. A. Wirpsza,
S. A. Marras, M. Kozlov, L. Krasnoperov,
A. Mustaev
443. Oral delivery of insulin through the vitamin
B 12 uptake pathway. S. M. Clardy,
T. J. Fairchild, R. P. Doyle
444. Novel prodrug strategy for intracellular
delivery of bisphosphonates.
M. R. Webster, C. Hann, C. Freel Meyers
445. Synthesis and characterization of a new
generation of �-galactosidase-activated
MRI contrast agents. S. G. Byker,
D. M. Ballweg, A. S. Harney, E. A. Waters,
K. W. MacRenaris, K. Lakhoo, J. Krimmel,
T. J. Meade
446. Novel synthesis of prostamide analogs
for use in the physiological characterization
of a specific target receptor.
E. L. Shelnut, A. Makriyannis
447. Design and synthesis of sortase binding
peptide analogs and an SAR study of
small molecule sortase A inhibitors. S. Yi,
A. Chan, N. Suree, R. T. Clubb,
M. E. Jung
448. Quantitation of prechafuroside A, Isovitexin
2”-sulfate and Isovitexin in teas and
fresh tea leaves from spring to autumn.
H. Ishida, T. Usami, T. Wakimoto,
H. Nukaya
449. Synthesis of folate and siRNA conjugates
derived from a water soluble melittin.
I. R. Vlahov, H. R. Santhapuram,
P. J. Kleindl, J. F. Vaughn, L. Qi,
J. A. Reddy, C. P. Leamon
450. Trainable in-silico screening filter for
various human cytochrome P450 isoforms
inhibition liability. R. Didziapetris,
J. Dapkunas, A. Sazonovas, P. Japertas
451. Screening for inhibitors of superoxide
dismutase and characterization of inhibition
using NMR. M. E. Arrington,
J. S. Summers, J. D. Schmitt, J. Markley,
M. R. Yost, E. Parris
452. Pyrrolo[1,2-a]quinoxalin-4(5H)-ones as
novel adenosine A3 antagonists.
S. MAYER, S. Gardan, S. Schann,
P. Neuville
453. Effect of novel pp60 c-src inhibitors on
mammalian glutathione S-transferase activity.
B. S. I˙s¸gör,Y.G.I˙s¸gör, Z. Kılıç-Kurt,
S. Ölgen
454. Inhibitors of adenosine deaminase containing
5:8-fused imidazo[4,5f][1,4]diazocine
ring system.
S. Tantravedi
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