High-throughput screening was used to find selective inhibitors of human 15-lipoxygenase-1 (15-LOX-1). One hit, a 1-benzoyl substituted pyrazole-3-carboxanilide (1a), was used as a starting point in a program to develop potent and selective 15-LOX-1 inhibitors.

Tubulin-targeting drugs have increasingly become the focus of anticancer drugs research. Twenty-five novel benzimidazole grafted benzsulfamide-containing pyrazole ring derivatives were synthesized and evaluated for bioactivity as potential tubulin polymerization inhibitors. Among them, compound ...

The compound 4-(Phenylsulfonyl) morpholine belongs to the class of sulfonamides, which are widely used in the treatment of a large number of diseases caused by microorganisms. This compound has a morpholine group, which is also known for its antimicrobial properties. The aim of the present study...

Oxidation is a very important class of chemical reactions, and in organic chemistry, it can be defined in several ways. A broad definition by Sheldon and Kochi states oxidation in organic chemistry refers to either (1) the elimination of hydrogen atoms, as in the sequential dehydrogenation of et...

Phytochemical investigation of the leaves of Gymnosporia senegalensis (Lam.) Loes. led to the isolation and characterization of eighteen compounds: one new polyunsaturated fatty acid-derived monoglyceride, (2S)-1-O-(4′Z,7′Z,10′Z-octadecatrienoyl) glycerol (1); four galloylglucoside derivative...

Emergence of drug resistance has created unmet medical need for the development of new classes of antibiotics. Discovery of new antibacterial agents with new mode of action remains a high priority universally. 4(3H)-quinazolinone, a fused nitrogen heterocyclic compound has emerged as a biologica...

Thieno[2,3-b]pyridine-5-carbonitrile 16 with a 4-methyl-5-indolylamine at C-4 and a 5-methoxy-2-(dimethylamino)-methylphenyl group at C-2 had an IC50 value of 16 nM for the inhibition of PKCθ. While moderate inhibition of PKCδ was also observed (IC50 = 130 nM), 16 had IC50 values of greater th...

Diethyl phosphonates were conveniently converted into ethyl 4-aminophenyl and ethyl 4-[amino(hydroxyimino)methyl]phenyl phosphonates as potentially useful intermediates for the preparation of functionalized phenyl phosphonates.

In the present study, six new azocalix[4]arenes have been synthesized by reacting calix[4]arene with p-substituted aniline and ethyl bromoacetate. Characterization of these compounds has been used by elemental analyses, UV–Vis, FT-IR and 1H NMR spectroscopic studies. Their phase transfer studie...

Zika virus (ZIKV), an emerging Flavivirus, was recently associated with severe neurological complications and congenital diseases. Therefore, development of antiviral agents capable of inhibiting ZIKV replication is urgent. Chloroquine is a molecule with a confirmed safety history for use with p...

A library of new chiral thiazolidines was prepared starting from l-cysteine and d-penicillamine in a simple, one-step procedure. 2-Arylthiazolidines were obtained, as diastereoisomeric mixtures, with good yields and in short reaction times, through a new and greener procedure, using microwave ir...

In this paper we report the SAR studies of a series of N-(4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl)amide and N-(4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl)sulfonamide derivatives 6(a–o) and 7(a–o), were synthesized in good yields and characterized by 1H NMR, 13C NMR and mass spectral a...

Endogenous nitrosothiols (SNOs) including S-nitrosoglutathione (GSNO) serve as reservoir for bioavailable nitric oxide (NO) and mediate NO-based signaling, inflammatory status and smooth muscle function in the lung. GSNOR inhibition increases pulmonary GSNO and induces bronchodilation while redu...

We report SAR studies on a novel non-peptidic somatostatin receptor 3 (SSTR3) agonist lead series derived from (4-phenyl-1H-imidazol-2-yl)methanamine. This effort led to the discovery of a highly potent low molecular weight SSTR3 agonist 5c (EC50 = 5.2 nM, MW = 359). The results from molecular o...

The title dithiocarbamate compound was synthesized, and characterised by means of spectroscopic and single-crystal X-ray diffraction methods. Density functional theory method with the 6−311++G(d,p) basis set was employed to affirm the spectroscopic and structural properties and also to study the...

The use of endothiodipeptide anilides, which were obtained in high yields by a variation of the ‘azirine/oxazolone method’, for the synthesis of longer endothiopeptides is described. With this novel methodology, epimerically pure endothiopeptides with the thiocarbonyl group next to the bulky A...

Bifunctional chelating agents (BFCAs) are small molecules containing a chelating unit, able to strongly coordinate a metal ion, and a reactive functional group, devised to form a stable covalent bond with another molecule. BFCAs are widely employed since their conjugation to a suitable biomolecu...

In guinea pig ventricular cardiomyocytes, the R(−)-enantiomer of efonidipine concentration-dependently blocked T-type Ca2+ current with 85% inhibition at 1 μM. In contrast, R(−)-efonidipine (1 μM) had no effect on the L-type Ca2+ current and Ca2+ transient in cardiomyocytes and contractile for...

1.1. We investigated the effect of efonidipine hydrochloride (NZ-105) against acute renal failure (ARF) in male Wistar rats. ARF was produced by ischemia or glycerol.2.2. Ischemia-induced ARF was produced by right nephrectomy and clamping of the left renal artery for 60 min, followed by reperfus...

1.1. We investigated the renal protective effect of efonidipine hydrochloride (NZ-105) in spontaneously hypertensive rats (SHR). SHR were given a diet containing 0.075% NZ-105 from 8 weeks old for 20 weeks.2.2. 24-hr urinary protein excretion in the control SHR (drug-free diet) increased with ag...