Sixteen new 2-benzylidene-7-methyl-3-oxo-5-(substituted phenyl)-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid methyl esters (1a–4d) have been synthesized by reacting 1,2,3,4-tetrahydropyrimidine-2-thiones (1–4) with chloroacetic acid and appropriate benzaldehydes in a single step. Their structures have been proved by IR, 1H NMR, mass spectra and elemental analysis. The compounds were tested for their anti-inflammatory activities. Test results revealed that compounds 1b, 1c, 4a and 4c exerted moderate anti-inflammatory activity at the 100 mg/kg dose level compared with indomethacin.

Synthesis and anti-inflammatory activities of some thiazolo[3,2-a]pyrimidine derivatives.

Proper nucleosides availability is crucial for the proliferation of living entities (eukaryotic cells, parasites, bacteria, and virus). Accordingly, the uses of inhibitors of the de novo nucleosides biosynthetic pathways have been investigated in the past. In the following we have focused on dihydroorotate dehydrogenase (DHODH), the fourth enzyme in the de novo pyrimidine nucleosides biosynthetic pathway. We first described the different types of enzyme in terms of sequence, structure, and biochemistry, including the reported bioassays. In a second part, the series of inhibitors of this enzyme along with a description of their potential or actual uses were reviewed. These inhibitors are indeed used in medicine to treat autoimmune diseases such as rheumatoid arthritis or multiple sclerosis (leflunomide and teriflunomide) and have been investigated in treatments of cancer, virus, and parasite infections (i.e., malaria) as well as in crop science.

On Dihydroorotate Dehydrogenases and Their Inhibitors and Uses

The present invention provides compounds of formula (4), and their pharmaceutically acceptable salts and solvates, which are useful as inhibitors of the Hepatitis C virus (HCV) polymerase enzyme and are also useful for the treatment of HCV infections in HCV-infected mammals. The present invention also provides pharmaceutical compositions comprising compounds of formula (4), their pharmaceutically acceptable salts and solvates. Furthermore, the present invention provides intermediate compounds and methods useful in the preparation of compounds of formula (4).

Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same

2-Styrylchromones were synthesized as vinylogues of 2-phenylchromones (flavones), a broad class of anti-rhinovirus compounds. The antiviral activity of 2-styrylchromones and 3-hydroxy-1-(2-hydroxyphenyl)-5-phenyl-2,4-pentadien-1-ones, which are intermediates in the synthesis, was evaluated against two selected serotypes of human rhinovirus, 1B and 14, by a plaque reduction assay in HeLa cell cultures. All of the compounds interfered with HRV 1B replication, with the exception of 3-hydroxy-1-(2-hydroxyphenyl)-5-(4-methoxyphenyl)-2,4-pentadien-1-one. The majority of derivatives were also found to be effective against serotype 14, often with a higher potency.

https://journals.sagepub.com/doi/pdf/10.1177/095632020001100604

Synthesis and Anti-Rhinovirus Activity of 2-Styrylchromones:

2-Styrylchromones (2-SC) are chromone derivatives characterized by the attachment of a styryl group to the 2-position of the chromone structure. The 2-styrylchromone structure has been demonstrated to bear important biological activities such as antiallergic, antitumor, affinity and selectivity for A(3) adenosine receptors, antiviral, antioxidant and anti-inflammatory. The aim of the present paper was to review the available information on this field.

Biological activities of 2-styrylchromones

Antiallergic agents. iii. substituted trans-2-ethenyl-4-oxo-4h-1-benzopyran-6-carboxylic acids

Anti allergic agents 6. substituted 2 trans ethenyl 4 oxo 4h pyrido 1 2 a pyrimidine 7 carboxylic acids

A series of 7-trans-(2-pyridylethenyl)-5H-thiazolo[3,2-a]pyrimidine-5-ones was synthesized and evaluated for their pharmacological activity. Some compounds were found to be effective in inhibiting restraint ulcers in the rat. Two of them also showed interesting antiinflammatory activity.

7-trans-(2-Pyridylethenyl)-5H-thiazolo[3,2-a]pyrimidine-5-ones: synthesis and pharmacological activity.

A series of (E)-5-[2-(3-pyridyl)ethenyl]-1H,7H-pyrazolo-[1,5-a]pyrimidine-7-ones were synthesized and evaluated for the inhibition of stress-induced gastric ulcers in the rat after oral administration. Several molecules were found to be very active. The particularly interesting compound (E)-1-(3-chlorophenyl)-5-[2-(3-pyridyl)ethenyl]-1H,7H-pyrazolo[1,5-a]- pyrimidine-7-one was chosen for wider pharmacological investigation.

Synthesis and antiulcer activity of (E)-5-[2-(3-pyridyl)ethenyl]-1H,7H-pyrazolo [1,5-a]pyrimidine-7-ones.

A series of condensed N-aryl-2-cyano-3-oxo-3-pyrazolyl-propanamides were synthesized and evaluated for immunomodulating activity following intraperitoneal administration. These new molecules were found to enhance macrophage cytotoxicity and stimulate host mediated antibacterial defences in mice. The compound 3-cyano-3-(1,4-dihydro-1-phenyl-[1]-benzothiopyrano[4,3-c]pyrazol- 3-yl]-3-oxo-N-phenyl-propanamide, chosen for wider pharmacological investigation, proved effective in preventing adjuvant-induced arthritis development in rats.

G. Doria

Papers

Antiallergic agents. iii. substituted trans-2-ethenyl-4-oxo-4h-1-benzopyran-6-carboxylic acids

Anti allergic agents 6. substituted 2 trans ethenyl 4 oxo 4h pyrido 1 2 a pyrimidine 7 carboxylic acids

7-trans-(2-Pyridylethenyl)-5H-thiazolo[3,2-a]pyrimidine-5-ones: synthesis and pharmacological activity.

Synthesis and antiulcer activity of (E)-5-[2-(3-pyridyl)ethenyl]-1H,7H-pyrazolo [1,5-a]pyrimidine-7-ones.

Synthesis and immunomodulating activity of condensed N-aryl-2-cyano-3-oxo-3-pyrazolyl-propanamides.