The present study identified at least two novel angiotensin I-converting enzyme (ACE) inhibitory peptides in horse gram flour after hydrolysis with alcalase. The ACE inhibitory peptides from horse gram hydrolysate (HGH) were purified by ultrafiltration and different chromatography techniques fol...

Angiotensin converting enzyme (ACE) plays a key role in regulating blood pressure and ACE inhibitors are first-line drugs for treating hypertension. Food protein-derived peptides with ACE inhibitory activity are natural and safe alternatives for both prevention and treatment of hypertension. The...

The association of two pharmacophoric entities generates so-called ‘twin drugs’ or dimer derivatives. We applied this approach for the design of a small compound library for the interaction with α4β2∗ nicotinic acetylcholine receptors (nAChRs). In this compound series, the nAChR ligand N,N-d...

In this paper we describe the design and synthesis of bis(Het)Aryl-1,2,3-triazole quinuclidine α7R ligands using an efficient three-step sequence including a Suzuki-Miyaura cross coupling reaction with commercially available and home-made boron derivatives. The exploration of SAR required the p...

The present paper describes the development of a new series of P2Y12 receptor antagonists based on our previously reported piperazinyl urea series 1 (IC50 binding affinity = 0.33 μM, aq solubility

We have studied the interaction of polyfluorinated (in the benzene moiety) 2-chloroquinolines with liquid and aqueous ammonia as an approach to the synthesis of halogen-containing aminoquinolines. 5,7-Difluoro-, 5,6,8-trifluoro-, and 5,7,8-trifluoro-2-chloroquinolines mostly form products of sub...

Di-n-butyl phthalate (DBP), a plastic-derived, endocrine-disrupting chemical, is regarded as a male reproductive toxicant. In this study, we investigated the in vitro actions of DBP and mono-n-butyl phthalate (MBP, the main metabolite of DBP) on human sperm functions. Human sperm were treated wi...

ObjectivesWound closure is a part of any surgical procedure. Wound care and healing process are concepts, which are usually reliant upon sutures. The suture and non-suture repair of the tissues has been a major concern to surgeons for over four thousand years. The objective of this study is to c...

Ethylene polymerization was carried out with diphenylmethylidene-(cyclopentadienyl)(fluorenyl)zirconium dichloride (Ph2C(Cp)(Flu)ZrCl2) activated with various activators such as methylaluminoxane (MAO), tetrakis(pentafluorophenyl)borates (R·B(C6F5)4, R=Me2PhNH, Ph3C, C7H7, H(Et2O)n), dimethylan...

Partially fluorinated carboxylic acids exhibit rich conformational landscapes. We report the first high-resolution spectroscopic study of 3,3,3-trifluoro-2-(trifluoromethyl)propanoic acid. Its rotational spectrum was measured using both broadband chirped-pulse and narrow-band cavity-based Fourie...

Incorporation of fluorinated heterocyclic framework into organic molecules results in profound changes in their physical, chemical and biological properties. Realizing that the fluorinated thiochroman-4-ones are important scaffolds in medicinal chemistry and are rare in the chemical literature, ...

The bio-based poly(glycerol azelate) (PGAz) polyester was synthesized by catalyst-free polycondensation. Increasing the azelaic acid: glycerol molar ratio in the preparation of the prepolymer from 1.0:1.0 to 1.6:1.0 or increasing the curing time of the PGAz sheets from 24 to 48 h both resulted i...

The free fatty acid receptor 1 (FFA1) has emerged as an attractive anti-diabetic target that mediates glucose-stimulated insulin secretion. Several FFA1 agonists have been reported, but many of them possessed somewhat high lipophilicity and/or molecular weight. Herein, we describe the identifica...

The reaction of rhodium trichloride with β-(tetraphenyl)tetraphenyl porphyrin, H2(tpp)(Ph)4, and β-(tetraphenyl)tetrakismesityl porphyrin, H2(tmp)(Ph)4, in refluxing benzonitrile gave novel rhodium porphyrin chlorides, m-cyanophenyl and imine complexes. The m-cyanophenyl and imine complexes we...

A novel series of tubulin polymerization inhibitors, based on fluorinated derivatives of isocombretastatin A-4 was synthesized with the goal of evaluating the effect of these compounds on the proliferative activity. The introduction of fluorine atom was performed on the phenyl ring or at the lin...

In this study, catecholamides (7a–l) bearing different aromatic rings (such as pyridine-2-yl, pyridine-3-yl, phenyl, and 2-chlorophenyl groups) were synthesized as potent phosphodiesterase (PDE) 4 inhibitors. The inhibitory activities of these compounds were evaluated against the core catalytic...

Using a new simi-rigid multitopic ligand 2-(hydroxymethyl)-1H-benzo[d]imidazole-5-carboxylic acid (H2L), seven new coordination polymers [Zn3(L)2(μ2-OH)2]n (1), {[Zn2(HL)2(H2O)2]·SiF6}n (2), [Zn(HL)(SCN)]n (3), {[Zn2(HL)2(SO4)]·(4,4′-bpy)}n (4) [4,4′-bpy =4,4′-bipyridine], {[Zn(HL)2]·2H2O...

Agricultural production in many emerging economies suffer losses owing to the challenges posed by weeds. Owing to cost, ecological, environmental and other human health safety issues regarding the use and application of chemicals as a control option against invasive weeds, there has been a renew...

A general two-step synthesis of 7-aryl substituted 2,4,5,6-tetrahydro-3H-1,2,4-triazepine-3-thiones from 1-aryl-3-isothiocyanatopropan-1-ones has been developed. The synthesis involved reaction of these isothiocyanato ketones with hydrazines followed by acid-catalyzed heterocyclization of the pr...

The five-component reaction of ethyl 2-[(2-oxopropyl)sulfanyl]acetate, aromatic aldehydes, and ammonium acetate affords two diastereomers of 5,7-diaryl-5,6,7,8-tetrahydro-1H-pyrido[3,4-b][1,4]thiazin-2(3H)-ones via a novel tandem Mannich-enamine-substitution sequence. Presumably, they are genera...