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A new series of imidazole-5-carboxamide derivatives were prepared and tested for their anti-hyperlipidemic activity in Triton-WR-1339-induced hyperlipidemic Wistar rats. The purpose of this research was to improve benzophenone carboxamides water solubility maintaining at the same time the antihyperlipidemic activity. Compounds 4, 6, 10, and 11 were synthesized through a coupling reaction between imidazoles-5-carbonyl chloride and amino benzophenones. The tested animals (n=48) were divided into six groups: the first group (hyperlipidemic control group; HCG) received an intraperitoneal injection (i.p.) of (300 mg/kg) Triton WR-1339. The second group received i.p. injection of Triton WR-1339 followed by an intra-gastric administration of bezafibrate (100 mg/kg) (bezafibrate; BF). The third, fourth, fifth, and sixth groups received i.p. injection of Triton WR-1339 followed by an intra-gastric administration of (30 mg/kg) of compounds 4, 6, 10, and 11, respectively. At a dose of 30 mg/kg body weight compounds 4, 6, 10, and 11 significantly (p

Hyperlipidemia is a known cause of coronary vascular diseases, which is a major cause of death in many parts of the world. Targeting several pathways that lead to increase in lipid profiles is of great potential to control diseases. 1H-indole-2-carboxamide derivatives were tested for their hypolipidemic activity at the molecular level in comparison with bezafibrate. The gene expression profiles of lipoprotein signaling and cholesterol metabolism and fatty acid metabolism PCR arrays were determined in rats with acute hyperlipidemia induced by Triton WR1339. Lipid profiles of serum from treated rats showed significant hypolipidemic effect by the compounds. Several genes of potential interest were reported to be overexpressed by Triton WR1339 including Apoc3, Apob, Hmgcs2, Apoa1, Apoe, Apof, acsl1, and Decr1. Most of the overexpressed genes were downregulated by N-(3-Benzoylphenyl)-1H-Indole-2-Carboxamide with significant decreases in Apoc3, Apob, Acaa2, Acsl1, and Slc247a5 gene expression levels. N-(4-Benzoylphenyl)-1H-Indole-2-Carboxamide and bezafibrate did not significantly affect the gene expression levels which were increased with acute hyperlipidemia induced by Triton WR1339. In conclusion, gene expression profiling identified the possible mechanism in which Triton WR1339 induces its acute hyperlipidemic effect which was reversed by the use of N-(3-Benzoylphenyl)-1H-Indole-2-Carboxamide.

Inhibition of dipeptidyl peptidase-IV (DPP-IV) prevents the inactivation of gastric inhibitory polypeptide (GIP) and glucagon-like peptide–1 (GLP-1). This increases circulating levels of active GLP-1 and GIP and stimulates insulin secretion, which results in lowering of glucose levels and improvement of the glycemic control in patients with type 2 diabetes. In this study, pharmacophore modeling and docking experiments were carried out and a series of eight novel 2-ethoxy-6,9-disubstituted acridines (13, 15, and 17a–17f) have been designed and synthesized. Then, these compounds were evaluated for their ability to inhibit DPP-IV. Most of the synthesized compounds were proven to have anti-DPP-IV activity where compound 17b displayed the best activity of 43.8% inhibition at 30 μmol/L concentration. Results of this work might be helpful for further optimization to develop more potent DPP-IV inhibitors.

Hyperlipidemia is a medical condition characterized by an increase in one or more of the plasma lipids, including triglycerides, cholesterol, cholesterol esters, phospholipids and or plasma lipoproteins including very low-density lipoprotein and low-density lipoprotein along with reduced high-density lipoprotein levels. This elevation of plasma lipids is among the leading risk factors associated with cardiovascular diseases. In the meantime, statins and fibrates remain the major anti-hyperlipidemic agents for the treatment of elevated plasma cholesterol and triglycerides respectively, with the price of severe side effects on the muscles and the liver. The present review focuses mainly on the types of hyperlipidemias, lipid metabolism, treatments and new drug targets for the treatment of elevated lipid profile. Many agents such as lanosterol synthase inhibitors, squalene epoxidase inhibitors, diacyl glycerol acyl transferase inhibitors, ATP citrate lyase inhibitors have shown a promising potential in the treatment of hyperlipidemia in clinical trials.

In the search for new potential antihyperlipidemic agents, the present study focuses on the synthesis and pharmacological activity of a series of novel N-(4-benzoylphenyl)-2-furamides (3a-3e). Hyperlipidemia was induced in rats by single intraperitoneal injection of Triton WR-1339 (300 mg/kg body weight). At a dose of 15 mg/kg body weight, compounds 3b, 3d and bezafibrate (100 mg/kg) significantly (p0.0001) reduced elevated plasma triglyceride levels after 18 h compared to the hyperlipidemic control group. However, only groups treated with compounds 3b, and 3d obviously showed a significant (p0.0001) reduction in plasma total cholesterol levels. Moreover, high density lipoprotein-cholesterol levels were significantly (p0.0001) increased in animals treated with compounds 3b, 3d and bezafibrate. It is therefore reasonable to assume that compounds 3b and 3d may have promising potential in the treatment of hyperlipidemia. This beneficial activity may contribute to their cardioprotective and antiatherosclerotic role.

A novel series of 5-fluoro-N-(9,10-dihydro-9,10-dioxoanthracen-8-yl)-1H-indole-2-carboxamides (3c-3g) were synthesized. The present study was undertaken to investigate the possible antihyperlipidemic effect of these novel compounds on hyperlipidemic rats. Hyperlipidemia was induced by a single intraperitoneal injection of Triton WR-1339 (300 mg/kg). The tested animals were divided into normal control (NCG), hyperlipidemic control (HCG), compounds 3c-, 3d-, 3e-, 3f-, 3g- and bezafibrate (BF)-treated groups. At a dose of 15 mg/kg, compounds 3c-3g and BF (100 mg/kg) significantly (p < 0.0001) reduced elevated plasma triglycerides levels after 12 and 24 h compared to the hyperlipidemic control group. However, only compounds 3e and 3g obviously showed a significant (p < 0.0001) reduction in plasma total cholesterol levels after 12 and 24 h. Moreover, high-density lipoprotein cholesterol levels were significantly increased in all treated groups. The current study demonstrates that 5-fluoro-N-(9,10-dihydro-9,10-dioxoanthracen-8-yl)-1H-indole-2-carboxamides (3c-3g) have a definite antihyperlipidemic potential and these beneficial activities may contribute to their cardioprotective and antiatherosclerotic role.

In the search for new potential antihyperlipidemic agents, the present study focuses on the synthesis of novel N-(benzoylphenyl)-5-substituted-1H-indole-2-carboxamides (compounds 8-12, 15, 16, 18) and investigating their antihyperlipidemic activity using Triton WR-1339-induced hyperlipidemic rats as an experimental model. Hyperlipidemia was developed by intraperitoneal injection of Triton WR-1339 (250 mg/kg body weight). The tested animals were divided into normal control (NCG), hyperlipidemic (HG), compound 8, 9, 15, 16, 18- and bezafibrate treated groups. At a dose of 15 mg/kg body weight, compounds 9, 16, 18 and bezafibrate (100 mg/kg) significantly (p < 0.0001) reduced elevated plasma triglycerides levels after 12 h compared to the hyperlipidemic control group. However, only the group treated with compounds 9, 16 and 18 showed an obviously significant (p < 0.001) reduction in plasma total cholesterol levels after 12 h compared to the hyperlipidemic control group. Moreover, high density lipoprotein-cholesterol levels were significantly (p < 0.0001) increased in all treated groups after 12 h compared to the hyperlipidemic control group, except for compounds 8 and 15 which revealed inactive. It is therefore reasonable to assume that compounds 9, 16 and 18 may have potential in the treatment of hyperlipidemia.

The synthesis of new 7-(halophenylamino)-1-cyclopropyl-6-fluoro-8-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid derivatives is described. Substitution of quinolonic compound 1a with chloro and fluoro aniline derivatives at position 7 produced target compounds 2–9 with relatively low yields. Alternatively, the product of correspondent carboxylate ester 1b subsequent with acid hydrolysis produced satisfactory yield. The prepared targets have shown interesting antibacterial properties against standard and resistant gram-positive strains. In particular, 2-chloro and 3-chloro aniline derivatives (3 and 4) depict MIC values of 6.7 and 0.9 μg/ml, respectively against standard S. aureous. Both compounds showed good activity against resistant strains of S. aureous.

The N-(benzoylphenyl)-1H-indole-2-carboxamide derivatives 1 - 6 were synthesized, and the lipid-lowering effects of two of these novel compounds were studied using hyperlipidemic rats as an experimental model. Treatment of ethyl-1H-indole-2-carboxylate with aminobenzophenones in the presence of sodium ethoxide and DMF, followed by purifi cation using column chromatography, gave the target compounds in good yields. The tested animals were divided into control, hyperlipidemic, compounds 2-, 3- and bezafibrate-treated groups. At a dose of 15 mg/kg body weight, compounds 2, 3 and bezafibrate significantly reduced the elevated plasma triglyceride levels after 7 and 24 h. Furthermore, the high-density lipoprotein- cholesterol levels were remarkably increased in all treated groups after 7 and 24 h compared to the hyperlipidemic control group. However, only compounds 2- and 3-treated groups obviously showed a significant reduction in plasma total cholesterol levels after 24 h. It is therefore reasonable to assume that 2 and 3 may have a promising potential in the treatment of hyperlipidemia and coronary heart diseases.

N-Ethylation of substituted ethyl 1H-indole-2-carboxylates with iodoethane and potassium carbonate gave substituted ethyl 1-ethyl-1H-indole-2-carboxylates. The later compounds on treatment with a range of aryl amines with varying structural complexity, gave the desired ethyl 1H-indole-2-carboxamide analogues.

Purpose: To synthesize and evaluate the anti-hyperlipidemic activity of a novel series of N- (benzoylphenyl)-2-furamides ( 3a , 3b , 4a , 4b and 4c ). Methods: Compounds ( 3a , 3b , 4a , 4b and 4c ) were successfully synthesized by reacting activated furan-2-carbonyl-chloride derivatives with aminobenzophenones at 60 °C for 36 h. Hyperlipidemia was induced in overnight fasted rats by intraperitoneal administration of Triton WR-1339 (300 mg/kg). to overnight fasted rats. The rats were divided into six groups: control, hyperlipidemic, hyperlipidemic plus compounds 3b , 4b , 4c , and hyperlipidemic plus bezafibrate-treated. Eighteen hours later, blood samples were collected and plasma lipid profile determined using enzymatic methods. Results: At a dose of 15 mg/kg body weight, the elevated plasma triglyceride (TG) levels, total cholesterol (TC) and low density lipoprotein cholesterol (LDL-C) levels were significantly reduced by compounds 4b (p < 0.001) and 4c (p < 0.0001) 18 h later, compared to the hyperlipidemic group. Furthermore, compounds 4b and 4c significantly increased high density lipoprotein cholesterol (HDL-C) levels by 29 and 34 %, respectively. Conclusion: The findings indicate the high potency of N-(benzolphenyl)-2-furamides ( 4b and 4c ) as lipid-lowering agents. Thus, these compounds 4b and 4c may used as lead compounds for the development of new derivatives and agents for targeting dyslipidemia and cardiovascular diseases. Keywords: Triton WR-1339-induced hyperlipidemic rats, N-(benzoylphenyl)-2-furamides, Lipid-lowering activity, Cardiovascular disease, Synthesis

It is estimated that 2-3% of children in the US have hypertension (HTN) and 8% of children ages 4-17 carry the diagnosis of attention-deficit hyperactivity disorder (ADHD). The prevalence of HTN and cardiovascular (CV) risk factors in children with ADHD on CNS stimulant treatment (stimulants) compared to no treatment and compared to their healthy counterparts is not well described. Using National Health and Nutrition Survey data, we examined demographic, blood pressure (BP) and CV risk factors of 4,907 children aged 12-18 years with and without the diagnosis of ADHD, and further examined the CV risk in a subgroup of ADHD patients on stimulants. Three hundred eighty-three (10.7%) children were reported to have ADHD, of whom 111 (3.4%) were on stimulants. Children with ADHD on stimulants were significantly younger, male, and white compared to those with ADHD not on medication and those without ADHD. Body mass index (BMI), eGFR, cholesterol, the prevalence of albuminuria, and poverty were not significantly different between the three groups. One hundred sixty (2.7%) had BP in the hypertensive and 637 (12.4%) in the pre-hypertensive range. The prevalence of elevated BP (HTN and/or pre-HTN range) was not different between children with ADHD on stimulants compared to ADHD without medication and those without ADHD. Heart rate (HR) was significantly higher in the ADHD group on stimulants vs. the groups ADHD on no stimulants and without ADHD. When the relationship between stimulants and the risk of abnormal BP was examined, there was a significant interaction between having BP in the HTN range and sex. After adjusting for BMI, race, and age, females with ADHD on stimulants tended to be older and had significantly more BP in the hypertensive range. On the other hand, males were more likely to be of a white race and older, but not hypertensive. Children with ADHD on stimulants have significantly higher HR than children with ADHD on no stimulants and children without ADHD. On the other hand, the prevalence of abnormal BP classification is comparable between the three groups.

Five novel derivatives of N-(9,10-dihydro-9,10-dioxoanthracenyl)-1H-indole-2-carboxamide were synthesized and their lipid-lowering effects studied in hyperlipidemic rats. Fusion of the anthraquinone derivatives at high temperature with 5-indole-2-carbonyl chloride, followed by recrystallization from chloroform=methanol gave the desired compounds in excellent yields. Compounds 1 to 5 at a non-toxic dose (1 ml of 57 mM solutions) and bezafibrate as positive control were administered to rats that were hyperlipidemic due to treatment with Triton WR-1339. A decrease in the plasma levels of triglyceride (TG) and low-density lipoprotein-cholesterol (LDL-C) and an increase in the plasma level of high-density lipoprotein-cholesterol (HDL-C) were observed with compounds 1, 3, 4, and 5. Compounds 1, 4, and 5 significantly reduced total cholesterol (TC) levels as well. These compounds may provide agents for targeting dyslipidemia and cardiovascular disease.

A new series of Furan-2-carboxamide derivatives of anthraquinone (compounds N1, N3, N5) were synthesized and tested in vivo using Triton WR-1339-induced hyperlipidemic rat as an experimental model ...

Glycemic goals (hemoglobin A1c7%) are often not achieved in patients with type 2 diabetes despite the availability of many effective treatments and the documented benefits of glycemic control in the reduction of long-term microvascular and macrovascular complications. Several studies have established the important positive effects of pharmacist-led management on achieving glycemic control and other clinical outcomes in patients with diabetes. Diabetes prevalence and mortality are increasing rapidly in Jordan. Nevertheless, clinical pharmacists in Jordan do not typically provide pharmaceutical care; instead, the principal responsibilities of pharmacists in Jordan are dispensing and marketing of medical products to physicians.To assess the primary clinical outcome of glycemic control (A1c) and secondary outcomes, including blood pressure, lipid values, self-reported medication adherence, and self-care activities for patients with type 2 diabetes in an outpatient diabetes clinic randomly assigned to either usual care or a pharmacist-led pharmaceutical care intervention program.Patients with type 2 diabetes attending an outpatient diabetes clinic of a large teaching hospital were recruited over a 4-month period from January through April 2011 and randomly assigned to intervention and usual care groups using the Minim software technique. The intervention group at baseline received face-to-face objective-directed education from a clinical pharmacist about type 2 diabetes, prescription medications, and necessary lifestyle changes, followed by 8 weekly telephone follow-up calls to discuss and review the prescribed treatment plan and to resolve any patient concerns. The primary outcome measure was glycemic control (A1c), and secondary measures included systolic and diastolic blood pressure, complete lipid profile (i.e., total cholesterol, low-density lipoprotein cholesterol [LDL-C], high-density lipoprotein cholesterol [HDL-C], serum triglycerides), and self-reported medication adherence (4-item Morisky Scale) and self-care activities (Summary of Diabetes Self-Care Activities questionnaire). Data were collected at baseline and at 6 months follow-up. Changes from baseline to follow-up were calculated for biomarker values, and between-group differences in the change amounts were tested using the t test for independent samples. A P value of0.05 was considered statistically significant.A total of 77 of 85 patients (90.6%) randomly assigned to the intervention group and 79 of 86 patients (91.9%) assigned to usual care had baseline and 6-month follow-up values. Compared with baseline values, patients in the intervention group had a mean reduction of 0.8% in A1c versus a mean increase of 0.1% from baseline in the usual care group (P = 0.019). The intervention group compared with the usual care group had small but statistically significant improvements in the secondary measures of fasting blood glucose, systolic and diastolic blood pressure, total cholesterol, LDL-C, serum triglycerides, self-reported medication adherence, and self-care activities. Between-group differences in changes in the secondary measures of HDL-C and body mass index were not significant.Patients with type 2 diabetes who received pharmacist-led pharmaceutical care in an outpatient diabetes clinic experienced reduction in A1c at 6 months compared with essentially no change in the usual care group. Six of 8 secondary biomarkers were improved in the intervention group compared with usual care.

A new series of N-(benzoylphenyl) and N-(acetylphenyl)-1-benzofuran-2-carboxamides (3a–3d and 4a′–4c′) were synthesized. Compounds (3a, 3b, and 4a′–4c′) were tested in vivo using Triton-WR-1339-induced hyperlipidemic rats as an experimental model for their hypolipidemic activity. The tested animals were divided into eight groups: control, hyperlipidemic, 3a, 3b, 4a′, 4b′, 4c′, and bezafibrate. At a dose of 15 mg/kg, the elevated plasma triglyceride (TG) levels were significantly reduced in compounds 3b (p

Benzothiophene carboxamide derivatives of aminobenzophenone, aminopyridine, aminobenzimidazole, and aniline derivatives (compounds 1 - 9) were synthesized and compounds 3, 6, 7, 8, and 9 tested in vivo for their hypolipidemic activity. Compounds 1 - 8 were prepared adopting the fusion process at 130 - 150°C between benzothiophene-2-carbonyl chloride and aminobenzophenones, aminopyridine, and anilines, respectively, and were obtained in high yield, while compound 9 was obtained from the reaction of benzothiophene acyl chloride with aminobenzimidazole in DMF at 160°C. At a dose of 15 mg/kg body weight compounds 6, 7, and 9 significantly reduced plasma triglyceride levels in Triton WR-1339-induced hyperlipidemic rats in comparison to control rats. Furthermore, they significantly increased high-density lipoprotein levels. It is therefore reasonable to assume that compounds 6, 7, and 9 may have a promising potential in the treatment of hyperlipidemia and atherosclerosis

Direct interaction between 7-chloro-1-cyclopropyl-6-fluoro-8-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid and primary α-amino acids (exemplified by glycine, alanine, and l-valine) in aqueous ethanolic NaHCO(3) at 70-80°C for 24-72 h produced the respective N-(4-oxoquinolin-7-yl)-α-amino acids (6a-c). The latter derivatives underwent reductive lactamization upon treatment with Na(2)S(2)O(4) in aqueous ethanol to afford moderate yields of the corresponding pyrido[2,3-f]quinoxaline-8-carboxylic acids (8a-c). Acetylation of 8a-c using acetyl chloride afforded N(4)-acetylated hexahydro-2,7-dioxopyrido[2,3-f]quinoxaline-8-carboxylic acids (9a-c). The structures, assigned to these new heterocyclic products, are supported by analytical and spectral data. The synthesized compounds (6a-c/9a-c) showed appreciable antibacterial activity as compared with ciprofloxacin.

Using Triton WR-1339-induced hyperlipidemic rats as an experimental model, we investigated whether compound 4 [N-(9,10-dihydro-9,10-dioxoanthracen-2-yl)benzofuran-2-carboxamide] and compound 5 [N-(4-benzoylphenyl)benzofuran-2-carboxamide], two novel anti-hyperlipidemic agents, have any effect on plasma triglyceride (TG), total cholesterol (TC), and high-density lipoprotein cholesterol levels (HDL-C) levels. The tested animals were divided into control (CG), hyperlipidemic (HG), and compounds 4, 5, and bezafibrate (BF) treated groups. At a dose of 15 mg/kg body weight, compounds 4, 5, and BF significantly reduced elevated plasma TG levels after 7 and 24 h. Furthermore, HDL-C levels were remarkably increased in all treated groups after 7 and 24 h compared to the hyperlipidemic control group. However, only compounds 4 and 5 treated groups clearly showed a significant reduction in plasma total cholesterol levels after 7 and 24 h. It is therefore reasonable to assume that compounds 4 and 5 may have promising potential in the treatment of hyperlipidemia and atherosclerosis.

The lipid-lowering activity of a series of novel N-(benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide derivatives has been studied in Triton WR-1339-induced hyperlipidemia in rats. The test animals were divided into four groups: control, hyperlipidemic, compound + 4% DMSO [C1: N-(2-benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide (1), C2: N-(3-benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide (2), C3: N-(4-benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide (3)]-treated and bezafibrate (BF)-treated. At a dose of 15 mg/Kg body weight, compounds 2, 3 and BF significantly reduced elevated plasma triglycerodes levels after 12 h. Moreover, high density lipoprotein-cholesterol levels were significantly increased in all treated groups after 12 h compared to the hyperlipidemic control group, except for C1 which was inactive. In sum, it may be stated that the results of the present study demonstrated new properties of some N-(benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide derivatives as potent lipid lowering agents and these beneficial activities may contribute to their cardioprotective and antiatherosclerotic role.

Background Glycaemic goals are often not achieved in patients with type 2 diabetes despite the availability of many effective treatments and the documented benefits of glycaemic control in the reduction of long-term microvascular and macrovascular complications. Purpose To evaluate, in a randomised, controlled trial, the impact of a clinical pharmacy service on clinical outcomes in patients with type 2 diabetes. Materials and Methods A total of 171 patients (85 interventions vs. 86 usual care) participated in the study. Intervention patients had individualised education and treatment recommendations from a clinical pharmacist while control patients received usual care provided by the clinic. The primary outcome measure was glycaemic control manifested by HbA1c reductions. All other data collected including systolic and diastolic blood pressure, total cholesterol, low density lipoprotein (LDL), high density lipoprotein (HDL), serum triglycerides, medication adherence, and necessary self-care activities formed secondary outcome measures. Between-group differences in the amounts of change from baseline to 6-month follow-up were tested and a p value of Results Compared with baseline values, patients in the intervention group had a mean reduction of 0.8% in HbA1c versus a mean increase of 0.1% from baseline in the usual care group (P = 0.019). The intervention group compared with the usual care group had small but statistically significant improvements in the secondary measures of fasting blood glucose, systolic and diastolic blood pressure, total cholesterol, LDL, serum triglycerides, self-reported medication adherence and self-care activities. Between-group differences in changes in the secondary measures of HDL and body mass index were not significant. Conclusions The enhanced patient clinical outcomes as a result of pharmacist-led pharmaceutical care in an outpatient diabetes clinic in the present study demonstrate the value of an enhanced clinical pharmacy service in improving diabetes care and achieving the desired therapeutic outcomes for patients with type 2 diabetes. No conflict of interest.

Using Triton WR-1339-induced hyperlipidaemic rats as an experimental model, we investigated whether compound 1 (N-(3-benzoylphenyl)-1H-indole-2-carboxamide) and 2 (N-(4-benzoylphenyl)-1H-indole-2-carboxamide) novel anti-hyperlipidaemic agents have any effect on plasma triglyceride, total cholesterol (TC) and high-density lipoprotein cholesterol levels (HDL-C) levels. Hyperlipidaemia was developed by intraperitoneal injection of Triton WR-1339 (200 mg/kg body weight). At a dose of 15 mg/kg body weight, compounds 1, 2 and bezafibrate (BF) significantly reduced the elevated plasma triglyceride levels after 7 and 24 h. Furthermore, HDL-C levels were remarkably increased in all treated groups after 7 and 24 h compared with the hyperlipidaemic control group. However, only compounds 1 and 2-treated groups clearly showed a significant reduction in plasma TC levels after 24 h. It is therefore reasonable to assume that compounds 1 and 2 may have a promising potential in the treatment of hyperlipidaemia and coronary heart diseases.

7-(3-Chlorophenylamino)-1-cyclopropyl-6-fluoro-8-nitro-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid ( 2 ) was prepared and fully characterized by NMR, IR, and MS. Compound 2 exhibited good antibacterial activity against gram-positive standard and resistant strains. Keywords: 7-anilinofluoroquinolone; fluoroquinolone; antibacterial 1. Introduction To date, fluoroquinolones represent successful synthetic antibacterial agents [1–5]. However, increased prescribing has led to the recent emergence of fluoroquinolone-resistant bacteria which has necessitated the search for newer drugs with efficacy against resistant strains [6,7]. The present work aims at the synthesis of a new fluoroquinolone derivative ( 2 ) and screening of its activity. 2. Results and Discussion An earlier study carried out by our team [4] revealed that substitution of lipophilic groups such as aniline at C-7 of 8-nitrofluoroquinolone ( 1 ) produced noticeable increase in gram-positive activity, especially against resistant strains with significant loss of gram-negative activity [4]. This research aims at further investigation of halogenated aniline derivatives exemplified by compound