Free fatty acid-2 (FFA2) receptor is a G-protein coupled receptor of interest in the development of therapeutics in metabolic and inflammatory disease areas. The discovery and optimization of an N-thiazolylamide carboxylic acid FFA2 agonist scaffold is described. Dual key objectives were to i) e...

A series of 5′-carbamoyl and 5′-thionocarbamoyl derivatives of 2′-C-methyl analogues of the A1 adenosine receptor (A1AR) full agonists N6-cyclopentyladenosine (CPA), 2-chloro-N6-cyclopentyladenosine (CCPA), N6-[3-(R)-tetrahydrofuranyl]adenosine (tecadenoson), and 2-chloro analogue (2-Cl-tecad...

A copper-catalyzed aerobic oxidative CN bond cleavage reaction was developed for the synthesis of 4-substituted-NH-1,2,3-triazoles. Diverse β-ketotriazoles derivatives, which are the starting materials for the aerobic oxidative CN bond cleavage reaction, were prepared from nine aryl and seven a...

A sensitive and rapid high-performance liquid chromatography (HPLC) method was developed to enantioseparation of N-acetyl-dl-cysteine after precolumn derivatization using o-phthaldialdehyde and primary aliphatic amines. Seven polysaccharide-based chiral columns were tested in a reversed phase mo...

The acylation of substituted 2-aminopropanamides with (2S)-Boc-proline, (2S)-Cbz-proline and (2S)-Bn-proline was used to prepare substituted 1-protected N-(1-carbamoyl-1,1-dialkyl-methyl)-(S)-prolinamides (74–89%), whose subsequent deprotection gave N-(1-carbamoyl-1,1-dialkyl-methyl)-(S)-prolin...

Triterpenoic acids, ursolic acid (1), oleanolic acid (2), glycyrrhetinic acid (3) and betulinic acid (4) were converted into their corresponding methyl 5–8 and benzyl esters 9–12 or benzyl amides 21–24. These derivatives served as starting materials for the synthesis of pink colored rhodamine...

A thermally stable esterase from Klebsiella oxytoca is explored as an excellent enantioselective biocatalyst (E > 100) for the hydrolytic resolution of (R,S)-tropic acid esters and (R,S)-ethyl α-methoxyphenyl acetate in biphasic media. An expanded Michaelis–Menten mechanism for the enzymatic a...

Lipases such as Candida rugosa lipase and Pseudomonas cepacia (Amano Ps) lipase immobilized in gelatin gels (gelozymes) exhibit very high enantioselectivities (E>200) during alcoholysis of racemic 2-acetoxy-4-phenyl-(E)-but-3-enenitrile with n-butanol in hexane and diisopropyl ether. C. rugosa l...

Human kinesin Eg5 is a potential inhibiting site for cancer chemotherapy. Blocking metaphase by binding foreign inhibitors with Eg5 eventually leads to apoptotic cell death. Here, we report the pyrazolopyrimidine derivates as potent inhibitors of Eg5 that prevents mitotic kinesin progression. IC...

A novel series of pyrazolo[1,5-a]pyrimidines were synthesized and proved by their spectral and elemental analysis, some elected of the newly synthesized compounds were examined for their cytotoxic activity employing MTT assay on two cancer cell lines (Breast and Hela cancers). Compounds 5, 7e an...

A series of nine new N-substituted-4-((1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl)amino)benzamides (6a-i) derivatives was synthesized. All the compounds were screened in-vitro for BSA anti-denaturation property, antioxidant assay and p38α MAP kinase inhibition. The in vitro anti-inflammatory ass...

Treatment of the anionic triosmium cluster [N(PPh3)2][Os3(μ-H)(CO)11] with one equivalent of [RhCp*(MeCN)3][{PF6}2] [Cp*=pentamethylcyclopentadiene] yielded three Cp*-containing clusters including [Os3Rh(μ-H)2(μ-CO)(CO)9(η5-Cp*)] 1, [Os3Rh(μ-CO)2(CO)9(η5-Cp*)] 2 and [Os3Rh2(μ-H)(μ-CO)2(C...

The use of potassium osmate, K2[OsO2(OH)4], as a precursor for some cyclopentadienyl-osmium complexes is described. The X-ray structures of OsBr(PPh3)2Cp, OsCl(dppe)Cp and OsX(dppe)Cp∗ (X = Cl, Br) are reported.

The reaction of [CpRu(PPh3)2Cl] and [CpOs(PPh3)2Br] with chelating 2-(2′-pyridyl)imidazole (N ∩ N) ligands and NH4PF6 yields cationic complexes of the type [CpM(N ∩ N)(PPh3)]+ (1: M = Ru, N ∩ N = 2-(2′-pyridyl)imidazole; 2: M = Ru, N ∩ N = 2-(2′-pyridyl)benzimidazole; 3: M = Ru, N ∩ N = ...

Treatment of the osmium(II) hydrides Cp∗Os(P–P)H (Cp∗ = pentamethylcyclopentadienyl) with methyl trifluoromethanesulfonate (MeOTf) affords osmium(II) triflate complexes with the general formula Cp∗Os(P–P)(OTf), where P–P = bis(dimethylphosphino)methane (dmpm), bis(diphenylphosphino)methane (d...

Condensation of 3,6-dichloropyridazine with 3,5-dimethylpyrazole in 1:1 ratio yielded one side substituted pyrazolylpyridazine ligand 3-chloro-6-(3,5-dimethylpyrazolyl)pyridazine (L) while condensation of 3,6-dichloropyridazine with substituted pyrazoles in 1:2 ratio yielded both side substitute...

N-[4-Chloro-2-fluoro-5-{3-(2-fluorophenyl)-5-methyl-4,5-dihydroisoxazol-5-yl-methoxy}-phenyl]-3,4,5,6-tetrahydrophthalimide (EK-5385) is an experimental substituted bicyclic herbicide. Soil-applied EK-5385 showed good rice selectivity and potent herbicidal activity on barnyardgrass (Echinochloa ...

In Gram-positive bacteria, Sortase A (Srt A) is a critical cysteine transpeptidase that is responsible for recognizing and assembling surface virulence proteins through the recognition of a LPXTG (leucine, proline, X, threonine, and glycine, where X is any amino acid) signal. Mutants lacking gen...

A mixture of iso-amyl nitrite/HBr is shown to be a mild and efficient reagent for electrophilic aromatic bromination. The reaction succeeds with slightly activated arenes and heterocyclic compounds. By using HCl instead of HBr, chlorination can also be performed in few cases. The i-amONO2/HBr mi...

The use of methyl 2-(1,3-dithian-2-yl)benzoate as a member of a new group of bidentate synthons in an improved annelation method, yielding polycyclic systems with three differentiated carbonyl groups, is described.