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Synthesis of 1,3,4-oxadiazoles - Organic Chemistry Portal

Liang P, Lv C, Jiang B, et al: MicroRNAprofiling in denatured dermis of deep burn patients. Burns.38:534–540. 2012. : :

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A Novel Series of Thiazoles and 1,3,4-Thiadiazoles …

Teaching and Research Experience: 1. AIMST University, Malaysia, Assoc. Professor (Jan 2009-till date).
2. Farooqia College of Pharmacy, India, Assistant Professor (July 2008-Dec 2008)
3. Bharathi College of Pharmacy, India, Lecturer (Jan 2007-July 2007)
4. Farooqia College of Pharmacy, India, Lecturer (Jan 2002-Jan 2007)
5. KMR College of Pharmacy, India, Lecturer (Jan 1989-Jun 1991)

Highly Efficient 1,4-Addition of 1,3-Diesters to Conjugated Enones by In/TMSCl, 2003,

145. Patel S, Macaulay K, Woodgett JR. Tissue-Specific Analysis of Glycogen Synthase Kinase-3 alpha (GSK-3 alpha) in Glucose Metabolism: Effect of Strain Variation. 2011;6(1):e15845

Synthesis of S -Heterocycles - Organic Chemistry Portal

54. Woodgett JR. Molecular cloning and expression of glycogen synthase kinase-3/factor A.  1990;9:2431-8

Research Interest: 1. Pharmacy Practice & Clinical Pharmacy
2. Pharmaceutical care
3. Pharmacotherapy of cardiovascular diseases
4. Pharmacokinetics
5. Patient education/Patient counselling and compliance monitoring

14. Kuemmerle JF. Endogenous IGF-I protects human intestinal smooth muscle cells from apoptosis by regulation of GSK-3 beta activity. 2005;288:G101-G10

ChemSynthesis - Chemical Database

43. Wisniewska MB. Physiological role of beta-catenin/TCF signaling in neurons of the adult brain.  2013;38:1144-55

GSK-3, glycogen synthase kinase-3; nM, nanomolar; ATP, adenosine triphosphate; GS, glycogen synthase; PI-3 kinase, phosphatidylinositol-4, 5-bisphosphate 3-kinase; PKB, protein kinase B; BD, bipolar disorder; AD, Alzheimer's disease; Wnt pathway, a pathway that transfers signals from the outside of the cell to the inside of the cell through cell surface receptors; β-catenin, cadherin association protein; KDa, kilodalton; IC50, the half maximal inhibitory concentration; SAR, structure activity relationship; HBD, hydrogen bond donor; HBA, hydrogen bond acceptor; PBMC, peripheral blood mononuclear cells; AIDS, acquired immunodeficiency syndrome; Pgp, P-glycoprotein; PET, positron emission tomography; MDR-MDCK assay, a permeability assay using Madin-Darby canine kidney cells with the gene; CDK1, cyclin-dependent kinase 1; ERK2, extracellular signal-regulated kinase 2, also known as mitogen activated protein kinase; IL-8, interleukin 8; ZDF, Zucker diabetic fatty; PIM1, proto-oncogene serine/threonine-protein kinase; PAK1, serine/threonine-protein kinase 1; DAPK1, death-associated protein kinase 1; MLCK, myosin light-chain kinase; FLT4, fms-related tyrosine kinase 4; CK2, casein kinase-II; CLK1, dual specificity protein kinase; PD, Parkinson's disease; HD, Huntington's disease; CNS, central nervous system; TMED, threshold minimum effective dose; TDZD, Thiadiazolidinones; PKA, protein kinase A; PKC, protein kinase C; PSP, progressive supranuclear palsy; MMSE, mini-mental status examination, cGMP, current Good Manufacturing Practice; and ITDZ, 5-imino-1, 2, 4-thiadiazole.

2. Summers SA, Kao AW, Kohn AD, Backus GS, Roth RA, Pessin JE. . The role of glycogen synthase kinase 3beta in insulin-stimulated glucose metabolism. 1999;274:17934-40

130. Meijer L, Flajolet M, Greengard P. Pharmacological inhibitors of glycogen synthase kinase 3.  2004;25:471-80
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  • Bioorganic & Medicinal Chemistry Letters | Vol 20, Iss …

    Gold-Catalyzed Sequential Alkyne Activation for the Synthesis of 4,6-Disubstituted Phosphorus 2‑Pyrones, 2013,

  • PDF Downloads : Oriental Journal of Chemistry

    39. Beurel E. Regulation by glycogen synthase kinase-3 of inflammation and T cells in CNS diseases. 2011;4:18

  • Glycogen Synthase Kinase-3 (GSK-3)-Targeted Therapy …

    111. Klein PS, Melton DA. A molecular mechanism for the effect of lithium on development. 1996;93:8455-9

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A number of methyl 2-aryl-4-methylthiazole-5-carboxylates 3 and their derivatives were previously prepared by the condensation of methyl α-chloroacetoacetate (1) with thiobenzamides 2 (). In order to further study the potential of the arylthiazole class of compounds as antiviral agents, the preparation of methyl 4-amino-2-(4-chlorophenyl)thiazole-5-carboxylate (6) was attempted ().

Search Result - International Journal of Advanced …

Aryl thioamides undergo a very rapid condensation in the presence of methyl bromocyanoacetate to provide quantitative yields of 3,5-diaryl-1,2,4-thiadiazoles with easy work-up and a high degree of product purity. The method can be scaled up with no loss in efficiency.


Regioselective Synthesis of Dihydrothiophenes and Thiophenes via the Rhodium-Catalyzed Transannulation of 1,2,3-Thiadiazoles with Alkenes 2016,

Synthesis and Antibacterial Activities of Novel Imidazo…

The goal of the present study was to determine the scope of the reaction of aryl thioamides 2 with methyl bromocyanoacetate (4) to determine if it could constitute a general method for synthesis of 3,5-diaryl-1,2,4-thiadiazoles.

26. Li X, Liu M, Cai Z, Wang G, Li X. Regulation of glycogen synthase kinase-3 during bipolar mania treatment. 2010;12:741-52

Next, a variety of commercially available aryl thioamides 2 were allowed to react with methyl bromocyanoacetate (4) at room temperature (). Among the 1,2,4-thiadiazoles reported in the chemical literature, the ortho-substituted derivatives have been more difficult to prepare and there are fewer examples of them. Therefore, in this study more attention was given to synthesis of products containing substituents in the ortho positions of the phenyl rings and six ortho substituted derivatives 5c, 5d, 5h, 5i, 5j and 5k were prepared. The reaction of o-substituted thiobenzamides 2c, 2h, 2i, 2j and 2k proceeded in quantitative yields; however, the o-trifluoromethyl derivative 5d was obtained in low yield (10%). Most of the other meta, para, and disubstituted thiobenzamide derivatives afforded the corresponding 1,2,4-thiadiazoles in essentially quantitative isolated yields of pure products regardless of differences in electronic and/or steric properties of the substituent(s). The 3- and 4-pyridyl derivatives 5t,u were obtained in moderate yields (65–69%). However, the corresponding 2-pyridyl derivative could not be obtained in any yield and the starting materials decomposed under the reaction conditions. The condensation reaction to produce 3,5-diaryl-1,2,4-thiadiazoles did not work when 2,6-disubstituted thiobenzamides were used. To date, there are no efficient methods reported for the synthesis of 3,5-bis(2,6-dichlorophenyl)-1,2,4-thiadiazole, although it has been obtained as a by-product from the reaction of thioamides with nitrous acid. Moreover, oxidation of 2,6-dichlorothiobenzamide was reported to yield the corresponding isothiocyanate. We are unaware of any efficient methods reported for preparation of 3,5-di(2-pyridyl)-1,2,4-thiadiazole or any 3,5-[(2,6-disubstituted)aryl]-1,2,4-thiadiazole, including the presently reported method. Thioacetamide was tried as an example of an aliphatic thioamide and it was unsuccessful.

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