PurposeChemoradiation (CRT) is an integral treatment modality for patients with locally advanced lung cancer. It has been hypothesized that current use of an angiotensin-converting enzyme inhibitor during CRT may be protective for treatment-related lung damage and pneumonitis.

We have previously shown that cough potentiation induced by intravenous administration of the AT1 receptor antagonist losartan is lower than that induced by the ACE inhibitor lisinopril in anesthetized and awake rabbits. Since losartan and lisinopril cross the blood–brain barrier, their central...

A new sensitive and discriminating spectrofluorimetric method has been developed and validated for determination of Lisinopril, one of the angiotensin converting enzyme inhibitors, in its pure bulk form and pharmaceutical tablets. The reaction of Lisinopril with ethylacetoacetate and formaldehyd...

BackgroundExposure to chemotherapeutic agents such as acetaminophen may lead to serious liver injury. Calcium deregulation, angiotensin II production and xanthine oxidase activity are suggested to play mechanistic roles in such injury.

Therapeutic interventions are still limited in the treatment of liver fibrosis even though an incredible number of publications related to silymarin are produced. This is due to the complex molecular pathogenesis. Several studies pointed to the role of renin-angiotensin system (RAS) in hepatic f...

BackgroundTrastuzumab is highly effective for human epidermal growth factor receptor type 2 (HER2)–positive breast cancer but is associated with a decline in left ventricular ejection fraction.

A simple and straightforward method for the determination of dolasetron mesylate (DM) in aqueous solution was developed based on the fluorescence quenching of 3-Mercaptopropionic acid (MPA) capped CdS quantum dots (QDs). The structure, morphology, and optical properties of synthesized QDs were c...

The asymmetric amination of anilines to 3-bromooxindoles was developed in the presence of a bis(oxazoline)-Ni(dppp)Cl2 complex, to provide enantiomerically enriched 3-amino-2-oxindoles with quaternary stereocenters in up to 90% yield with 92:8 er. Simultaneously, direct stereoselective amination...

Reaction of 5-arylethynyl-2-methyl-2H-tetrazoles (acetylene tetrazoles) with arenes under the action of Brønsted superacid CF3SO3H or acidic zeolite HUSY CBV-720 gives rise to E-/Z-5-(2,2-diarylethenyl)-2-methyl-2H-tetrazoles, as products of hydroarylation of acetylene bond, in yields up to 98% ...

As part of a program aimed at discovering orally active 2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor antagonists, we screened our compound library and identified 2-[allyl(4-methylphenyl)amino]-4H-pyrido[3,2-e][1,3]thiazin-4-one (7) as a lead compound that inhibited k...

Filamenting temperature-sensitive mutant (FtsZ) is a novel target for the treatment of tuberculosis. A series of (R)-2-(4′-chlorophenyl)-3-(4′-nitrophenyl)-1,2,3,5-tetrahydrobenzo[4,5] imidazo[1,2-c]pyrimidin-4-ol derivatives were designed and docked on the FtsZ protein crystal structure (PDB ...

With the aim of obtaining newer biologically active compounds, a series of 4-(6-substituted-1,3-benzothiazol-2-yl)amino-1,3-thiazole-2-amines (9–12) and 4-(6-substituted-1,3-benzothiazol-2-yl)amino-2-(4-substitutedphenyl-methylidene)amino-1,3-thiazole (13–28) were synthesized. The structures o...

A new organic potential nonlinear optical (NLO) material 1-(3,4-dimethoxyphenyl)-3-(3-fluorophenyl)prop-2-en-1-one (DMP3FP) is crystallized in acetone. The single crystal X-ray diffraction data shows that material crystallizes into centro-symmetric orthorhombic space group Pbca with a = 15.6552(...

Myeloid differentiation primary response protein 88 (MyD88), an essential adapter protein used by toll-like receptors (TLR), is a promising target molecule for the treatment of respiratory inflammatory diseases. Previous studies explored the activities of novel 2-amino-4-phenylthiazole analogue ...

Because Janus kinases (JAKs) play a crucial role in cytokine-mediated signal transduction, JAKs are an attractive target for the treatment of organ transplant rejection and autoimmune diseases such as rheumatoid arthritis (RA). To identify JAK inhibitors, we focused on the 1H-pyrrolo[2,3-b]pyrid...

In an attempt to obtain novel candidate compound for weed control, a series of newly substituted 3-(pyridin-2-yl)benzenesulfonamide derivatives 2 were designed and synthesized using compound II7 as a lead compound by Intermediate Derivatization Methods and their herbicidal activities were evalua...

PI3Kδ, which is mainly expressed in leukocytes, plays a critical role in B-cell receptor mediated signaling pathway and has been extensively studied as a drug discovery target for B cell malignances such as AML, CLL etc. In this manuscript, we report the discovery, SAR optimization and pharmaco...

Fatty acids (FA) are crucial for the maintenance of membrane fluidity and play a central role in metabolic energy storage. Polyunsaturated fatty acids play an essential ecological role since they are key parameters in the nutritional value of algae. Pesticide impacts on fatty acid profiles have ...

An effective synthetic route for preparation of oligo(fluorene-co- dibenzothiophene-S,S-dioxide)s (trimer SOF2, pentamer SOF4, heptamer SOF6 and nonamer SOF8) based on meta- or para-linked dibenzothiophene-S,S-dioxide (SO) unit as the core was developed by convergence method, for which the inter...

(S)-MeO-BIPHEP-metal complexes were firstly used as chiral extractants to separate amino acid enantiomers. Six amino acid enantiomers were employed to evaluate the stereoselectivities of (S)-MeO-BIPHEP-metal complexes. The results revealed that (S)-MeO-BIPHEP-Cu complex exhibited good abilities ...