Use of Lawesson's reagent in organic syntheses.

Arylglyoxals in synthesis of heterocyclic compounds.

Interpenetration in extended three-dimensional (3D) arrays has been investigated by a systematic analysis of the crystallographic structural databases, using an ad hoc version of the program package TOPOS. In this paper we describe the comprehensive results of our investigation of interpenetration in organic hydrogen-bonded 3D arrays from the Cambridge Structural Database. The great interest in the self-assembly of organic molecules into hydrogen-bonded supramolecular arrays has prompted us to investigate these systems at a rather unusual level; that is, beyond the formation of synthons, we have examined the topologies of the resulting networks and looked for their entanglements. Within 3D architectures we have extracted a complete list including 122 different motifs showing the phenomenon of interpenetration (76 unseen by the original authors). These organic networks include species assembled by a single or by different building blocks; they are discussed and classified according to the previously introd...

Interpenetrated Three-Dimensional Networks of Hydrogen-Bonded Organic Species: A Systematic Analysis of the Cambridge Structural Database

Data on the synthetic routes to substituted 1,2,3-triazoles, including those containing functional groups, based on cyclisation of various nitrogen compounds published during the last 15 years are described. Examples of using new triazole derivatives in agrochemistry, medicine and engineering are given.

https://iopscience.iop.org/article/10.1070/RC2005v074n04ABEH000893/pdf

1,2,3-Triazole and its derivatives. Development of methods for the formation of the triazole ring

Corticotropin-releasing factor (CRF) antagonists have formula (I), wherein A, R3, R4 and R5 are as defined herein. They are useful in the treatment of illnesses induced or facilitated by CRF, such as inflammatory disorders, and depression and anxiety related disorders.

Pyrazolopyrimidines as crf antagonists

The synthetic route to N-alkyl-N'-(4-diazo-5-pyrazolyl)ureas (4) starting from pyrazolo[4,3-c][1,2,5] oxadiazin-3(5H)-one (1) is described. Compounds (4) undergo thermal and photochemical reactions affording pyrazolo[3,4-d][1,2,3]triazoles (5) and pyrazolo[3,4-d]oxazoles (7) respectively

Synthesis of N-alkyl-N'-(4-diazo-5-pyrazolyl)ureas and their conversion into pyrazolo[3,4-d][1,2,3]triazole and pyrazolo[3,4-d]oxazole derivatives

4-Nitroso-5-amino-pyrazole derivatives in carboxyl-group activation for peptide synthesis

3-Methyl-5-(acyl/alkyl)aminoisoxazole-4-thiocyanates were prepared by rhodanation of N-acyl/alkyl-3-methyl-5-isoxazolamines. These products were tested for antifungal activity against a series of phytopathogenic fungi of different taxonomic classes. Some of the compounds showed interesting in-vitro activity. The more active compound in the in-vitro test displayed a moderate preventive activity against Plasmopara viticola, Alternaria solani and Pyricularia recondita.

Fungitoxicity of 5‐aminoisoxazole‐4‐thiocyanate derivatives

As a part of an investigation on molecular hybrids as new serine protease inhibitors, the pyrazolo [4,3-c][1,2,5]oxadiazin-3(5H)-one ring system was selected as a model of potential mechanism-based inhibitors. Due to the inherent reactivity of this system an optimal balance between susceptibility to nucleophilic attack and stability in solvents was sought prior to development as therapeutic agents. Substitutions on N5 and C7 of the supporting pyrazole ring with either aliphatic or aromatic groups (compounds 2 a-m) and the replacement of the carbonyl oxygen on the reactive oxadiazinone ring with sulfur (compounds 3a,i) were explored. Two members (2i and 2k) of this class of inhibitors displayed time-dependent inhibition of HLE suggesting mechanism-based inhibition. The observation that HLE generated a product(s) from compound 2i which displayed an identical UV-Visible spectrum to that observed during non-enzymatic hydrolysis further supports this proposal. FlexX-based docking of these compounds into a model of the human leukocyte elastase (HLE) active site produced a molecular model of the inhibitor-enzyme interaction.

https://www.tandfonline.com/doi/pdf/10.1080/14756360109162352

Potential of pyrazolooxadiazinone derivatives as serine protease inhibitors.

Four 5-amino-4-alkylthio-pyrazoles were synthesized and their antifungal activity was evaluated in vitro in Trichophyton mentagrophytes, Microsporum cookei and Candida albicans. The compounds slightly influenced the growth kinetics of the yeast, but at concentrations ranging from 20 to 40 micrograms/ml completely prevented the mycelial growth of the two dermatophytes cultivated on Sabouraud's agar medium. An electron microscopic study, undertaken by using the most active compound, showed that in C. albicans mitochondria were the only cell targets affected whereas in the dermatophytes cell wall, plasmalemma and the main cytoplasmic organelles were damaged in various degrees. Since the most remarkable alterations were connected with membrane abnormalities, the cytological changes observed were tentatively interpreted as a consequence of the compound intrusion into the lipid bilayer of the membranes, since the drug is lipophilic in nature.

Paolo Giori

Papers

Synthesis of N-alkyl-N'-(4-diazo-5-pyrazolyl)ureas and their conversion into pyrazolo[3,4-d][1,2,3]triazole and pyrazolo[3,4-d]oxazole derivatives

4-Nitroso-5-amino-pyrazole derivatives in carboxyl-group activation for peptide synthesis

Fungitoxicity of 5‐aminoisoxazole‐4‐thiocyanate derivatives

Potential of pyrazolooxadiazinone derivatives as serine protease inhibitors.

Antifungal properties of some pyrazolyl-alkyl-sulfides. Electron microscopic evidence in two dermatophytes and Candida albicans