Positions

Overview

  • Medicinal Chemist; Manager, CNS Discovery/Computational Chemistry; Southern Research Institute
  • Selected Publications

    Academic Article

    Year Title Altmetric
    2018 Interactions between Cocaine and the Putative Allosteric Dopamine Transporter Ligand SRI-31142.Journal of Pharmacology and Experimental Therapeutics.  367:222-233. 2018
    2017 Discovery of novel frizzled-7 inhibitors by targeting the receptor's transmembrane domain.Oncotarget.  8:91459-91470. 2017
    2017 The role of human dopamine transporter in NeuroAIDS.Pharmacology and Therapeutics.  183:78-89. 2017
    2017 Hu antigen R (HuR) multimerization contributes to glioma disease progression.Journal of Biological Chemistry.  292:16999-17010. 2017
    2017 Allosteric modulatory effects of SRI-20041 and SRI-30827 on cocaine and HIV-1 Tat protein binding to human dopamine transporter.Scientific Reports.  7:3694. 2017
    2016 Discovery of a novel inhibitor of kinesin-like protein KIFC1.Biochemical Journal.  473:1027-1035. 2016
    2016 Identification of quinazoline compounds as novel potent inhibitors of Wnt/β-catenin signaling in colorectal cancer cells.Oncotarget.  7:11263-11270. 2016
    2016 The dopamine D3 receptor antagonist, SR 21502, facilitates extinction of cocaine conditioned place preference.Drug and Alcohol Dependence.  159:263-266. 2016
    2016 Pramipexole at a Low Dose Induces Beneficial Effect in the Harmaline-induced Model of Essential Tremor in Rats.CNS Drug Reviews.  22:53-62. 2016
    2015 The selective dopamine D3 receptor antagonist, SR 21502, reduces cue-induced reinstatement of heroin seeking and heroin conditioned place preference in rats.Drug and Alcohol Dependence.  156:228-233. 2015
    2015 Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.Cell.  161:1252-1265. 2015
    2015 Studies of the biogenic amine transporters 15. Identification of novel allosteric dopamine transporter ligands with nanomolar potency.Journal of Pharmacology and Experimental Therapeutics.  353:529-538. 2015
    2014 Unique functional and structural properties of the LRRK2 protein ATP-binding pocket.Journal of Biological Chemistry.  289:32937-32951. 2014
    2014 Design, synthesis, and structure-activity relationship studies of a series of [4-(4-carboxamidobutyl)]-1-arylpiperazines: insights into structural features contributing to dopamine D3 versus D2 receptor subtype selectivity.Journal of Medicinal Chemistry.  57:7042-7060. 2014
    2014 The novel dopamine D3 receptor antagonist, SR 21502, reduces cocaine conditioned place preference in rats.Neuroscience Letters.  569:137-141. 2014
    2014 The effects of the novel DA D3 receptor antagonist SR 21502 on cocaine reward, cocaine seeking and cocaine-induced locomotor activity in rats.Psychopharmacology.  231:501-510. 2014
    2014 Lifting the mask: identification of new small molecule inhibitors of uropathogenic Escherichia coli group 2 capsule biogenesis.PLoS ONE.  9:e96054. 2014
    2013 A cell based high-throughput screening approach for the discovery of new inhibitors of respiratory syncytial virus.Virology Journal.  10:19. 2013
    2012 Synthesis and SAR of geminal substitutions at the C5' carbosugar position of pyrimidine-derived HCV inhibitors.Bioorganic and Medicinal Chemistry Letters.  22:6967-6973. 2012
    2012 (S)-N-(2,5-Dimethylphenyl)-1-(quinoline-8-ylsulfonyl)pyrrolidine-2-carboxamide as a small molecule inhibitor probe for the study of respiratory syncytial virus infection.Journal of Medicinal Chemistry.  55:8582-8587. 2012
    2012 14-Alkoxy- and 14-acyloxypyridomorphinans: μ agonist/δ antagonist opioid analgesics with diminished tolerance and dependence side effects.Journal of Medicinal Chemistry.  55:8350-8363. 2012
    2012 Synthesis and SAR of pyridothiazole substituted pyrimidine derived HCV replication inhibitors.Bioorganic and Medicinal Chemistry Letters.  22:5652-5657. 2012
    2012 Pyridofuran substituted pyrimidine derivatives as HCV replication (replicase) inhibitors.Bioorganic and Medicinal Chemistry Letters.  22:5144-5149. 2012
    2012 5-Benzothiazole substituted pyrimidine derivatives as HCV replication (replicase) inhibitors.Bioorganic and Medicinal Chemistry Letters.  22:3229-3234. 2012
    2012 The delta opioid receptor antagonist, SoRI-9409, decreases yohimbine stress-induced reinstatement of ethanol-seeking.Addiction Biology.  17:224-234. 2012
    2012 High-throughput screening identifies a bisphenol inhibitor of SV40 large T antigen ATPase activity.Journal of Biomolecular Screening.  17:194-203. 2012
    2012 Novel substituted pyrimidines as HCV replication (replicase) inhibitors.Bioorganic and Medicinal Chemistry Letters.  22:1160-1164. 2012
    2012 High throughput screening of a library based on kinase inhibitor scaffolds against Mycobacterium tuberculosis H37Rv.Tuberculosis.  92:72-83. 2012
    2011 Recombinant human immunodeficiency virus-1 transactivator of transcription1-86 allosterically modulates dopamine transporter activity.Synapse.  65:1251-1254. 2011
    2011 Discovery of novel benzoquinazolinones and thiazoloimidazoles, inhibitors of influenza H5N1 and H1N1 viruses, from a cell-based high-throughput screen.Journal of Biomolecular Screening.  16:73-81. 2011
    2011 Identification of novel small molecule activators of nuclear factor-κB with neuroprotective action via high-throughput screening.Journal of Neuroscience Research.  89:58-72. 2011
    2010 Antibacterial and antitubercular activities of some diphenyl hydrazones and semicarbazonesIndian Journal of Chemistry : Section B.  49:1384-1388. 2010
    2010 A high-throughput screen for chemical inhibitors of exocytic transport in yeast.ChemBioChem.  11:1291-1301. 2010
    2010 HTS-driven discovery of new chemotypes with West Nile Virus inhibitory activity.Molecules.  15:1690-1704. 2010
    2009 Antituberculosis activity of the molecular libraries screening center network library.Tuberculosis.  89:354-363. 2009
    2009 High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv.Tuberculosis.  89:334-353. 2009
    2009 Synthesis of pyrimidines and condensed pyrimidines through reactions of nitriles with o-aminocarbonyl substrates under acidic conditionsHeterocycles.  78:1627-1665. 2009
    2009 Studies of the biogenic amine transporters. 13. Identification of "agonist" and "antagonist" allosteric modulators of amphetamine-induced dopamine release.Journal of Pharmacology and Experimental Therapeutics.  329:718-728. 2009
    2009 Recent advances in structure-based virtual screening of G-protein coupled receptors.AAPS Journal.  11:178-185. 2009
    2008 A novel delta opioid receptor antagonist, SoRI-9409, produces a selective and long-lasting decrease in ethanol consumption in heavy-drinking rats.Biological Psychiatry.  64:974-981. 2008
    2008 Structure-based approach to pharmacophore identification, in silico screening, and three-dimensional quantitative structure-activity relationship studies for inhibitors of Trypanosoma cruzi dihydrofolate reductase function.Proteins.  73:889-901. 2008
    2008 High-throughput screening of a 100,000-compound library for inhibitors of influenza A virus (H3N2).Journal of Biomolecular Screening.  13:879-887. 2008
    2008 Studies of the biogenic amine transporters. 12. Identification of novel partial inhibitors of amphetamine-induced dopamine release.Journal of Pharmacology and Experimental Therapeutics.  326:286-295. 2008
    2007 Programs to facilitate tuberculosis drug discovery: the tuberculosis antimicrobial acquisition and coordinating facility.Infectious Disorders - Drug Targets.  7:92-104. 2007
    2007 Development and validation of a high-throughput screen for inhibitors of SARS CoV and its application in screening of a 100,000-compound library.Journal of Biomolecular Screening.  12:33-40. 2007
    2006 Opioid ligands with mixed mu/delta opioid receptor interactions: an emerging approach to novel analgesics.AAPS Journal.  8:E118-E125. 2006
    2005 Potentiation of rat lymphocyte proliferation by novel non-peptidic synthetic opioids.International Immunopharmacology.  5:1271-1278. 2005
    2004 Identification and characterization of a novel allosteric modulator (SoRI-6238) of the serotonin transporter.Synapse.  53:176-183. 2004
    2004 Erratum: Identification of Opioid Ligands Possessing Mixed μ Agonist/δ Antagonist Activity among Pyridomorphinans Derived from Naloxone, Oxymorphone, and Hydromorphone (Journal of Medicinal Chemistry (2004) 47 (1400))Journal of Medicinal Chemistry.  47:2716. 2004
    2004 Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].Journal of Medicinal Chemistry.  47:1400-1412. 2004
    2003 Docking and biological activity of pteridine analogs: Search for inhibitors of pteridine reductase enzymes from Trypanosoma cruziJournal of Molecular Structure: THEOCHEM.  635:37-44. 2003
    2003 Novel ligands for the opioid receptors: synthesis and structure-activity relationships among 5'-aryl and 5'-heteroaryl 17-cyclopropylmethyl-4,5 alpha-epoxypyrido[2',3':6,7]morphinans.Bioorganic and Medicinal Chemistry.  11:4143-4154. 2003
    2003 Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans.Bioorganic and Medicinal Chemistry Letters.  13:529-532. 2003
    2002 Identification of a novel partial inhibitor of dopamine transporter among 4-substituted 2-phenylquinazolines.Bioorganic and Medicinal Chemistry Letters.  12:2225-2228. 2002
    2002 Synthesis and antituberculous activity of N-Mannich bases of 3-[4-(4-chlorophenyl)-6-(4-methylphenyl) pyrimidin-2-yl] iminoisatin derivativesScientia Pharmaceutica.  70:39-48. 2002
    2002 Studies of the biogenic amine transporters. VIII: identification of a novel partial inhibitor of dopamine uptake and dopamine transporter binding.Synapse.  43:268-274. 2002
    2001 Antituberculous activity of norfloxacin mannich bases with isatin derivatives.Chemotherapy.  47:266-269. 2001
    2001 SoRI 9409, a non-peptide opioid mu receptor agonist/delta receptor antagonist, fails to stimulate [35S]-GTP-gamma-S binding at cloned opioid receptors.Brain Research Bulletin.  55:507-511. 2001
    2001 In vivo pharmacological characterization of SoRI 9409, a nonpeptidic opioid mu-agonist/delta-antagonist that produces limited antinociceptive tolerance and attenuates morphine physical dependence.Journal of Pharmacology and Experimental Therapeutics.  297:597-605. 2001
    2000 Antitubercular activity of thioseniicarbazones and semicarbazonesActa Pharmaceutica Turcica.  42:139-145. 2000
    1999 Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.Journal of Medicinal Chemistry.  42:3527-3538. 1999
    1999 Electrocatalytic glycol cleavage by periodate/iodate redox system under phase transfer conditionsBulletin of Electrochemistry.  15:298-299. 1999
    1998 Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety.Journal of Medicinal Chemistry.  41:2872-2881. 1998
    1998 Novel non-peptidic opioid compounds with immunopotentiating effects.Advances in Experimental Medicine and Biology.  437:183-187. 1998
    1998 Opioid peptide receptor studies. 8. One of the mouse brain deltaNCX binding sites is similar to the cloned mouse opioid delta receptor: further evidence for heterogeneity of delta opioid receptors.Peptides.  19:343-350. 1998
    1995 Opioid peptide receptor studies. 1. Identification of a novel delta-opioid receptor binding site in rat brain membranes.Peptides.  16:191-198. 1995
    1994 Additions and Corrections: Structure-Based Design of Inhibitors of Purine Nucleoside Phosphorylase. 3. 9-Arylmethyl Derivatives of 9-Deazaguanine Substituted on the Methylene Group ((J. Med. Chem. (1993) 36(24) (3771–3783) (10.1021/jm00076a004))Journal of Medicinal Chemistry.  37:1034. 1994
    1993 Structure-based design of inhibitors of purine nucleoside phosphorylase. 3. 9-Arylmethyl derivatives of 9-deazaguanine substituted on the methylene group.Journal of Medicinal Chemistry.  36:3771-3783. 1993
    1993 Synthetic and computer-assisted analysis of the structural requirements for selective, high-affinity ligand binding to diazepam-insensitive benzodiazepine receptors.Journal of Medicinal Chemistry.  36:1820-1830. 1993
    1993 Synthesis and structure-activity relationships of 3,5-disubstituted 4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-ones at diazepam-sensitive and diazepam-insensitive benzodiazepine receptors.Journal of Medicinal Chemistry.  36:479-490. 1993
    1990 Reaction of nitriles under acidic conditions. Part VI. Synthesis of condensed 4‐chloro‐ and 4‐aminopyrimidines from ortho‐aminonitrilesJournal of Heterocyclic Chemistry.  27:119-126. 1990
    1989 Reaction of nitriles under acadic conditions: Part IV- Synthesis of some 2-substituted quinazolin-4-ones and thienopyrimidin-4-ones of biological interest and isolation of o-functionalized amidine intermediatesIndian journal of chemistry.  28:1039-1047. 1989
    1989 Mono and bis(bioreductive) alkylating agents: synthesis and antitumor activities in a B16 melanoma model.Journal of Medicinal Chemistry.  32:1636-1642. 1989
    1989 Synthesis of some 2,4-diamino-6-substituted amino-5-arylpyrimidinesIndian journal of chemistry.  28:42-47. 1989
    1988 A facile synthesis of 3‐amino‐5‐substitutedaminoisothiazole‐4‐carboxylic acid derivativesJournal of Heterocyclic Chemistry.  25:759-765. 1988
    1988 Synthesis of 5H‐Triazolo[1,5‐d]‐ and 5H‐ Tetrazolo‐ [1,5‐d]thieno[3,2‐f]‐1,4‐diazepin‐6(7H)‐onesJournal of Heterocyclic Chemistry.  25:615-622. 1988
    1987 Studies on the synthesis and interconversion of isomeric triazolothienopyrimidines. Part III. Cyclization reactions of 2‐amino‐3‐(1H‐1,2,4‐triazol‐3‐yl)thiophenesJournal of Heterocyclic Chemistry.  24:1125-1131. 1987
    1986 Quinoline-2-aldoxime MethiodideJournal of Organic Chemistry.  51:3237-3239. 1986
    1986 Synthesis of indenes from phenylpropanones using alumina catalystTetrahedron.  42:4325-4332. 1986
    1985 Studies on the synthesis and interconversion of isomeric triazolotheinopyrimidines. Part II. Effect of 5‐substituents on the dimroth rearrangement of 1,2,4‐triazolo[4,3‐c]thieno[3,2‐e]pyrimidinesJournal of Heterocyclic Chemistry.  22:831-833. 1985
    1985 Studies on the synthesis of 2‐(2‐arylvinyl)thieno[2,3‐d]pyrimidines and 5‐(2‐arylvinyl)triazolothieno[3,2‐e]pyrimidinesJournal of Heterocyclic Chemistry.  22:825-830. 1985
    1984 Heterocyclization of functionalized ketene acetals: Synthesis of pyrimidines via vinylamidine intermediatesTetrahedron Letters.  25:1291-1292. 1984
    1984 Reaction of benzaldehyde with other carbonyl compounds over thoria and mixed oxides of thoria: Development of an effective catalyst and a process for the conversion of benzaldehyde to phenyl alkyl ketonesJournal of Catalysis.  89:489-497. 1984
    1984 Reaction of nitriles under acidic conditions. Part III. A facile synthesis of thienopyrimidin‐4(3H)‐onesJournal of Heterocyclic Chemistry.  21:375-380. 1984
    1983 Reaction of nitriles under acidic conditions: a novel, direct formation of condensed 4-chloropyrimidinesTetrahedron Letters.  24:4611-4612. 1983
    1981 Studies in the synthesis and interconversion of isomeric triazolothienopyrimidinesJournal of Heterocyclic Chemistry.  18:43-46. 1981
    1980 Reaction of nitriles under acidic conditions. Part I. A general method of synthesis of condensed pyrimidinesJournal of Heterocyclic Chemistry.  17:1497-1500. 1980

    Chapter

    Year Title Altmetric
    2008 Opioid ligands with mixed μ/δ opioid receptor interactions: An emerging approach to novel analgesics.  367-380. 2008

    Research Overview

  • Drug Design and Synthetic Medicinal Chemistry
  • Education And Training

  • Doctor of Philosophy in Medicinal/Pharmaceutical Chemistry, Foreign University
  • Full Name

  • Subramaniam Ananthan
  • Blazerid

  • ananthan