1. Kristina M.K. Kutterer et al :Over 195 4-alkyl and 4,4-dialkyl 1,2-bis(4-

chlorophenyl)pyrazolidine-3,5-dione derivatives were synthesized, utilizing

microwave accelerated synthesis, for evaluation as new inhibitors of

bacterial cell wall biosynthesis. Many of them demonstrated good activity

against MurB in vitro and low MIC values against Gram-positive bacteria,

particularly penicillin-resistant Streptococcus pneumoniae (PRSP).

Derivative 7l demonstrated antibacterial activity against both Gram-positive

and Gram-negative bacteria. Derivatives 7f and 10a also demonstrated

potent nanomolar Kd values in their binding to MurB.

An efficient microwave-assisted synthesis of substituted pyrazolidinediones

was developed. These compounds showed good activity against MurB and

Gram-positive bacteria.

2. Jalal Isaad et al : Simple route to a novel class of pyrazolidine -3,5- dione

based azo dyes

We report an easiest synthesis strategy of a new class of synthetic dyes by

coupling of functionalized pyrazolidine -3,5- dione derivatives via

diazotization reaction with aromatic diamine for the azoic dyes or via

dimerization reaction to synthesize the H chromophore dyes. Electron

delocalization between the two coupled components has been studied using

UV–vis spectroscopy, infrared, and NMR spectroscopy. In addition, the

formation mechanism of such compounds has been discussed.

3. Guanghui Deng et al : Pyrazolidine -3,5- dione derivatives as potent non-

steroidal agonists of farnesoid X receptor: Virtual screening, synthesis, and

biological evaluation

The identification of a novel pyrazolidine -3,5- dione based scaffold

hit compound as Farnesoid X receptor (FXR) partial or full agonist has been

accomplished by means of virtual screening techniques. A series of

pyrazolidine -3,5- dione derivatives (1a–u and 7) was designed,

synthesized, and evaluated by a cell-based luciferase transactivation assay

for their agonistic activities against FXR. Most of them showed agonistic

potencies and 10 of them (1a, 1b, 1d–f, 1j, 1n, 1t, 5b, and 7) exhibited

lower EC50 values than the reference drug CDCA. Molecular modeling

studies for the representative compounds 1a, 1d, 1f, 1j, 1n, 1u, 5b, and 7

were also presented. The novel structural scaffold has provided a new

direction for finding potent and selective FXR partial and full agonists

(referred to as ‘selective bile acid receptor modulators’, SBARMs).

A series of novel non-steroidal compounds as FXR agonists and

partial agonists was discovered by means of virtual screen and chemical

synthesis.

4. Kristina M.K. Kutterer et al : 4-Alkyl and 4,4′-dialkyl 1,2-bis(4-

chlorophenyl)pyrazolidine -3,5- dione derivatives as new inhibitors of

bacterial cell wall biosynthesis

Over 195 4-alkyl and 4,4-dialkyl 1,2-bis(4-chlorophenyl) pyrazolidine -

3,5- dione derivatives were synthesized, utilizing microwave accelerated

synthesis, for evaluation as new inhibitors of bacterial cell wall biosynthesis.

Many of them demonstrated good activity against MurB in vitro and low MIC

values against Gram-positive bacteria, particularly penicillin-resistant

Streptococcus pneumoniae (PRSP). Derivative 7l demonstrated antibacterial

activity against both Gram-positive and Gram-negative bacteria. Derivatives 7f

and 10a also demonstrated potent nanomolar Kd values in their binding to

MurB.

An efficient microwave-assisted synthesis of substituted

pyrazolidinediones was developed. These compounds showed good activity

against MurB and Gram-positive bacteria.

5. I.G. Voigt-Martin et al : The use of maximum entropy and likelihood

ranking to determine the crystal structure of 4-(4′-(N,N-

dimethyl)aminobenzylidene)-pyrazolidine -3,5- dione at 1.4 Å resolution

from electron diffraction and high-resolution electron microscopy image

data

The potential maps obtained by applying the method of combined

entropy maximisation and likelihood ranking to electron diffraction data are

compared with the results obtained from high-resolution electron

microscopy and molecular modelling for the non-linear optical material 4-

(4′-(N,N-dimethyl)aminobenzylidene)- pyrazolidine -3,5- dione,

C12H13N3O2. An excellent agreement has been obtained. This reinforces

claims that the maximum entropy (ME) method is a reliable means of

structure determination from electron diffraction data, and hence of

ascertaining the suitability of organic molecules for second harmonic

generation (SHG).

6. Kyung Ah Koo et al : Christine Herrenknecht :Dependence of the retention

of pyrazolidine -3,5- diones on eluent pH in reversed-phase high-

performance liquid chromatography.QSAR analysis of pyrazolidine -3,5-

diones derivatives as Dyrk1A inhibitors Individuals with Down

syndrome (DS) suffer from mental retardation. Overexpression and the

resulting increased specific activity of Dyrk1A kinase located on

chromosome 21 cause a learning and memory deficit in Dyrk1A transgenic

mice. To search for therapeutic agents with Dyrk1A inhibition activity,

previously we obtained HCD160 as a new hit compound for Dyrk1A

inhibition. In the present study, we synthesized 34 HCD160 derivatives to

investigate the quantitative structure–activity relationship (QSAR). This

analysis could provide important information for novel drug discovery for

treatment of DS related learning and memory deficits.The QSAR analysis of

34 pyrazolidine -3,5- diones derivatives of HCD160 showed that the

presence of the 3 -nitro-4-hydroxyphenyl moiety enhanced the inhibition

activity for Dyrk1A.

Md.Taifur Rahman et al : Synthesis of 4,4-bis(2-

hydroperoxyalkyl)pyrazolidine -3,5- diones using manganese(III)-catalyzed

autoxidation The autoxidation of a mixture of 1,2-disubstituted pyrazolidine

-3,5- diones 1 and alkenes 2 in the presence of a catalytic amount of

manganese(III) acetate dihydrate in air gave 4,4-bis(2-hydroperoxyalkyl)

pyrazolidine -3,5- diones 3 in 75–96% yields. The structure of the bis(2-

hydroperoxyethyl) pyrazolidine -3,5- dione 3 (R1=R2=Ph, R 3 =R4=4-FC6H4)

has been corroborated by an X-ray single crystallographic analysis. On the

other hand, the manganese(III) acetate oxidation of a mixture of 1

(R1=R2=Ph) and 2 (R 3 =R4=Ph) at elevated temperature gave 4,4-bis(2,2-

diphenylethenyl)-1,2-diphenylpyrazolidine-3,5- dione (4) in good

yield.Graphic

Md. Taifur Rahman et al : Manganese(III)-based oxidation of 1,2-

disubstituted pyrazolidine -3,5- diones in the presence of alkenes

The manganese(III)-catalyzed aerobic oxidation of 1,2-disubstituted

pyrazolidine -3,5- diones 1 in the presence of alkenes 2 gave the corresponding

pyrazolidinediones 3 which were doubly hydroperoxyalkylated at the 4-position

in high yields. On the other hand, pyrazolidinediones 1 were oxidized with

manganese(III) acetate in the presence of alkenes 2 at elevated temperature to

produce the 4,4-bis(alkenyl)pyrazolidinediones 4 in good yields instead of the

pyrazolidine -fused dihydrofuran analogue IV. A similar cerium(IV)-mediated

oxidation of pyrazolidinedione 1a with an alkene 2a afforded the doubly 4-

methoxyethylated derivative 5. The stability of the free hydroperoxyl group and

the reaction pathway for the aerobic and the metal-mediated oxidation reactions

were also discussed.

7. Yigang He et al : A photoprecursor for difluorocarbene 4,4-

Difluoropyrazolidine-3,5-dione was synthesized as a precursor for the

corresponding pyrazolinedione, envisioned as a photochemical source of

difluorocarbene. However, this azo compound proved to be far too unstable.

In contrast, 10,10-difluorobicyclo[4.3.1]deca-1,3,5-triene, readily

synthesized from indane, was found to be a practical source of

difluorocarbene for photochemical as well as thermal cyclopropanation

reactions.Michel Muehlebach et al : Aryldiones incorporating a

[1,4,5]oxadiazepane ring. Part I: Discovery of the novel cereal herbicide

pinoxaden. Derivatives of the new class of 3 -hydroxy-4-phenyl- 5 -oxo-

pyrazolines were optimized towards both herbicidal activity on key annual

grass weed species and selectivity in small grain cereal crops. The generic

structure can be separated into three parts for the analysis of the structure–

activity relationships, namely the aryl, the dione with its prodrug forms and

the hydrazine moiety. Each area appears to play distinct and different roles

in overall expression of biological performance which is further beneficially

influenced by adjuvant response and safener action. Pinoxaden 6, a novel

graminicide for use in wheat and barley incorporating a [1,4,5]oxadiazepane

ring, eventually emerged as a development candidate from the discovery and

optimization process.

8. M.F. Kasper et al : Defined test reagents for the diagnosis of drug-induced

allergy: Antibody-dependent skin reactions towards pyrazolinone and

pyrazolidinedione derivatives in the guinea pig

Chemically defined haptenic reagents and haptenic conjugates were

synthesized for use in clinical skin testing. One series of reagents was based

on the 1-phenyl-2,3-dimethyl-3 -pyrazolin- 5 -one structure, a second series

on 1,2-diphenyl- pyrazolidine -3,5- dione. Haptens were connected via

flexible spacer molecules which insert considerable distances between

haptenic moieties and carriers. The skin test reagents were hexavalent

conjugates prepared from the bis-penta-L-lysine carrier ‘PAL’. The

methodological details exemplify the application of N-hydroxysuccinimide

activated ester derivatives for the preparation of peptidic conjugates. Rabbit

and guinea-pig antisera against the haptens were obtained by immunization

with human serum albumin conjugates. Efficacy and cross-reactivity

relationshios were assessed by guinea pig PCA and by testing actively

immunized guinea pigs. A striking lack of cross-reactivity was found

between pyrazolinone and pyrazolidinedione haptenic reagents in all test

systems. On the other hand, the elicitation of homologous anaphylaxis was

highly effective with the PAL conjugates. The data presented and discussed

provide a basis for the evaluation of clinical tests performed in order to

define drug-induced allergic reactions. They are relevant for immediate-type

skin reactions as well as for serological methods.