Thiazoles

Publication Title: 
Biological & Pharmaceutical Bulletin

The ripe fruit of Terminalia chebula RETZIUS (T. chebula RETZ) (Combretsceae), which is a native plant in India and Southeast Asia, has traditionally been used as a popular folk medicine for homeostatic, antitussive, laxative, diuretic, and cardiotonic treatments. The objective of this study was to evaluate the protective effects of an aqueous extract of fruit of T. chebula on the tert-butyl hydroperoxide (t-BHP)-induced oxidative injury observed in cultured rat primary hepatocytes and rat liver. Both treatment and pretreatment of the hepatocytes with the T.

Author(s): 
Lee, Hyun-Sun
Won, Nam Hee
Kim, Kyoung Heon
Lee, Hojoung
Jun, Woojin
Lee, Kwang-Won
Publication Title: 
Parasitology Research

The absence of a vaccine and the rampant resistance to almost all antimalarial drugs have accentuated the urgent need for new antimalarial drugs and drug targets for both prophylaxis and chemotherapy. The aim of the study was to discover effective plant extracts against Plasmodium falciparum. In the present study, the hexane, chloroform, ethyl acetate, acetone, and methanol extracts of Citrus sinensis (peel), Leucas aspera, Ocimum sanctum, Phyllanthus acidus (leaf), Terminalia chebula (seed) were tested for their antimalarial activity against chloroquine (CQ)-sensitive (3D7) strain of P.

Author(s): 
Bagavan, Asokan
Rahuman, Abdul Abdul
Kamaraj, Chinnaperumal
Kaushik, Naveen Kumar
Mohanakrishnan, Dinesh
Sahal, Dinkar
Publication Title: 
Neurobiology of Disease

An increasing body of evidence indicates a role for oligomers of the amyloid-? peptide (A?) in the neurotoxicity of this peptide and the pathology of Alzheimer's disease (AD). Several neurotoxic oligomeric forms of A? have been noted ranging from the larger Amyloid ?-Derived Diffusible Ligands (ADDLs) to smaller trimers and dimers of A?. More recently a dodecameric form of A? with a 56 kDa molecular weight, denoted A?*56, was shown to cause memory impairment in AD model mice.

Author(s): 
Scherzer-Attali, R.
Farfara, D.
Cooper, I.
Levin, A.
Ben-Romano, T.
Trudler, D.
Vientrov, M.
Shaltiel-Karyo, R.
Shalev, D. E.
Segev-Amzaleg, N.
Gazit, E.
Segal, D.
Frenkel, D.
Publication Title: 
Archives of Gerontology and Geriatrics

Thiazolidine-4-carboxylic acid (TC) is a cyclic sulfur amino acid, a condensation product of cysteine and formaldehyde. The chemistry, biological effects and clinical use of TC are reviewed. Extensive animal experiments and studies on human subjects carried out in Europe indicate that a combination of TC and folic acid, 'Folcysteine', has revitalizing effects on age-related biochemical variables of blood and tissues. Further animal studies confirmed the anti-toxic effects of TC, particularly on the liver.

Author(s): 
Weber, H. U.
Fleming, J. F.
Miquel, J.
Publication Title: 
The Journals of Gerontology. Series A, Biological Sciences and Medical Sciences

BACKGROUND: Aging is a complex multifactorial process characterized by accumulation of deleterious changes in cells and tissues, progressive deterioration of structural integrity and physiological function across multiple organ systems, and increased risk of death. METHODS: We conducted a review of the scientific literature on the relationship of advanced glycation end products (AGEs) with aging. AGEs are a heterogeneous group of bioactive molecules that are formed by the nonenzymatic glycation of proteins, lipids, and nucleic acids.

Author(s): 
Semba, Richard D.
Nicklett, Emily J.
Ferrucci, Luigi
Publication Title: 
Expert Opinion on Drug Discovery

INTRODUCTION: Lurasidone is a novel antipsychotic drug approved for the treatment of schizophrenia in adults. It is formulated into tablets, administered orally once/day (dose range 40-160 mg/day) does not require titration, but needs to be given with food to maximize its plasma exposure. AREAS COVERED: This review focuses on the preclinical discovery of lurasidone. Furthermore, the article provides analysis on the pharmacological, behavioral and molecular mechanisms of lurasidone and their contribution to its therapeutic advantages.

Author(s): 
Tarazi, Frank I.
Riva, Marco A.
Publication Title: 
Journal of Pharmaceutical Sciences

Several 1-aryl-3-(2-pyrimidyl)thiocarbamides and their corresponding cyclized 2-arylimino-3-(2-pyrimidyl)thiazolid-4-ones were synthesized and characterized by their sharp melting points and elemental analyses. These thiocarbamides and thiazolidones possessed anticonvulsant activity against pentylenetetrazol-induced convulsions and potentiated pentobarbital-induced hypnosis in mice. Most of these thiocarbamides and thiazolidones selectively inhibited nicotinamide adenine dinucleotide (NAD)-dependent oxidation of pyruvate, where the use of added NAD dether hand, remained unaltered.

Author(s): 
Chaudhary, M.
Parmar, S. S.
Chaudhary, S. K.
Chaturvedi, A. K.
Sastry, B. V.
Publication Title: 
Pharmaceutical Research

A series of isodithiobiurets, dithiobiurets, and dithiazoles was synthesized and tested for biological activity. Generally, the compounds potentiated the hypnosis induced by pentobarbitone (50 mg/kg ip) in albino mice and exhibited antifungal and insecticidal activity against Fusarium oxysporum and Periplanata americana, respectively. Some compounds showed anticonvulsant and analgesic activity in albino rats.

Author(s): 
Pandeya, S. N.
Kumar, A.
Singh, B. N.
Mishra, D. N.
Publication Title: 
Archiv Der Pharmazie

Conveniently accessible 4-[(2-(3,4-dimethoxyphenyl)ethyl]-3-thiosemicarbazide (2) was converted to new 1-substituted benzylidene/furfurylidene-4- [2-(3,4-dimethoxyphenyl)ethyl]-3-thiosemicarbazides (3) which furnished 2-(substituted benzylidene/furfurylidene) hydrazono-3-[2-(3,4-dimethoxyphenyl)ethyl]thiazolidin-4-ones (4) and 1-(substituted benzylidene/furfurylidene)-amino -3-[2-(3,4-dimethoxyphenyl)ethyl]-2-thioxo-4,5-imidazolidinedio nes (5) on reaction with chloroacetic acid and oxalyl chloride, respectively.

Author(s): 
Ergenç, N.
Capan, G.
Günay, N. S.
Ozkirimli, S.
Güngör, M.
Ozbey, S.
Kendi, E.
Publication Title: 
Arzneimittel-Forschung

The general pharmacological properties of YJA 20379-1 (2-amino-4,5-dihydro-8-phenylimidazo[2,1-b]thiazolo[4,5-g]benzo thi azole), a novel proton pump inhibitor with antiulcer activities, were investigated in mice, rats, guinea pig and rabbits. YJA 20379-1 at oral doses of 50, 100 and 200 mg/kg did not affect the general behaviour, hexobarbital hypnosis, motor coordination and body temperature in mice. The drug does not have analgesic and anticonvulsant action at 200 mg/kg p.o. The locomotor activity was not affected at 100 mg/kg p.o., but at 200 mg/kg, the activity was suppressed.

Author(s): 
Lee, E. B.
Cho, S. I.
Cheon, S. A.
Chang, M. S.
Kim, K. B.
Sohn, S. K.
Chung, Y. K.

Pages

Subscribe to RSS - Thiazoles