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October 2010
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22 Reads
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1 Citation
ChemInform
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
September 2010
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12 Reads
ChemInform
For Abstract see ChemInform Abstract in Full Text.
August 2010
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27 Reads
ChemInform
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
June 2010
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12 Reads
ChemInform
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
August 2007
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91 Reads
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4 Citations
Journal of Antimicrobial Chemotherapy
DRF 8417, a novel oxazolidinone, has been evaluated against Gram-positive and fastidious Gram-negative bacteria. In vitro activity of DRF 8417 was determined by broth microdilution method and in vivo efficacy studies were carried out in different murine systemic infection models. DRF 8417 exhibited potent activity against Gram-positive pathogens with MIC(50) and MIC(90) values ranging from 0.06 to 1 mg/L. MICs against Haemophilus influenzae and Moraxella catarrhalis were one to two dilutions lower than those of linezolid. The in vivo efficacy, by oral route, in different susceptible and resistant Gram-positive systemic bacterial infection models ranged from 2.0 to 2.9 mg/kg. These studies displayed the excellent in vitro and in vivo activity of DRF 8417 against Gram-positive pathogens and lower MICs when compared with linezolid against H. influenzae and M. catarrhalis.
September 2006
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26 Reads
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22 Citations
Pharmacological Research
Ragaglitazar is a novel and potent dual peroxisome proliferators activated receptor (PPAR) alpha and gamma activator. The aim of this study is to investigate the effect of ragaglitazar on blood pressure and endothelial function in insulin resistant animal model and non-insulin resistant hypertensive models. The effects ragaglitazar were tested in Zucker fa/fa, spontaneously hypertensive rats (SHR), 2 kidney 1clip rat (2K1C) and Wistar Kyoto rats (WKY). Pioglitazone was taken as a comparative standard. Ragaglitazar showed significant reduction (P<0.001) of systolic blood pressure (SBP) in insulin resistant fa/fa rats, with concomitant reduction in plasma triglycerides (TG) and insulin levels while pioglitazone (10 mg kg(-1)) showed significant (P<0.05) but comparatively less reduction. Ragaglitazar in contrast to pioglitazone showed significant reduction (P<0.05) of SBP in SHR, 2K1C while the same dose did not have any effect on normotensive WKY. Ragaglitazar also showed significant improvement in acetylcholine-induced relaxation in isolated aorta of Zucker fa/fa, SHR, 2K1C and also potentiated the insulin-induced vasorelaxation in Zucker fa/fa rats. These findings summarize that ragaglitazar shows significant reduction of BP and improvement in endothelial function not only in insulin resistant but also in non-insulin resistant hypertensive models where standard thiazolidinediones are ineffective. These data indicates that dual PPARalpha and gamma activator ragaglitazar can be beneficial for the treatment of hypertension and vascular disease commonly associated with type 2 diabetes.
May 2006
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53 Reads
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29 Citations
Journal of Ethnopharmacology
Indigofera mysorens is a shrub used for its antidiabetic activity in rural India. Here, we elucidate the antidiabetic potential of Indigofera mysorensis extract. Ethanolic extract of the whole shrub of Indigofera (EEI) at 300 mg/kg for 10 days, produced a 63% reduction in plasma glucose, 41% reduction in plasma triglyceride and 77% reduction in plasma insulin levels in insulin resistant db/db mice, which is better than insulin sensitizer, troglitazone (400 mg/kg). EEI unlike sulphonylureas failed to show any acute hypoglycemic effect in normoglycemic Swiss albino mice (SAM). Even in a chronic study (10 days) in SAM, EEI (300 mg/kg) like insulin sensitizers showed no effect on plasma glucose, but an 81% reduction in plasma insulin levels. When challenged with 3 gm/kg sucrose, SAM treated with EEI (300 mg/kg, 7 days) failed to show any effect on the absorption of sugar, whereas standard drug, acarbose (10 mg/kg) showed 52% reduction in the area under the plasma glucose curve. EEI failed to show any significant transactivation of PPARgamma, a proposed target of synthetic insulin sensitizers. Taken together, our data indicate that the antidiabetic effect of the ethanolic extract of Indigofera is due to its insulin sensitizing property and is clearly different from that of sulfonylurea or acarbose.
February 2006
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51 Reads
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89 Citations
Bioorganic & Medicinal Chemistry
2,4-Thiazolidinedione derivatives of 1,3-benzoxazinone were synthesized and evaluated for their PPAR-alpha and -gamma dual activation. DRF-2519, a compound obtained through SAR of TZD derivatives of benzoxazinone, has shown potent dual PPAR activation. In ob/ob mice, it showed better efficacy than the comparator molecules. In fat fed rat model, it showed significant improvement in lipid parameters, which was better than fibrates.
March 2005
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14 Reads
ACS National Meeting Book of Abstracts
October 2004
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31 Reads
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32 Citations
ChemInform
Andrographolide 1, the major constituent of the Indian medicinal plant Andrographis paniculata (Acanthaceae) was converted into the key intermediate 4 by selective oxidative degradation of the C-12,13 olefin bond. The aldehyde functional group present in 4 has been utilized for synthesizing a number of structurally diverse labdane diterpenes. Synthesis and in vitro cytotoxic activity results of the compounds prepared are discussed.
... 5 However, while this approach is beneficial, it has limitations, including the side effects of the prescribed medications. 6 Given these challenges, the use of medicinal plants for primary care becomes a viable alternative, considering the abundance of plant resources available. 7 Furthermore, Phyllanthus amarus Schum. ...
December 2002
Current Science
... Recent studies on molecular modification of the later 1H, 3H-thiazolo [3,4-a] benzimidazoles (TBZs) revealed that, dismantling of the imidazole nucleus leading to the design of new 4-oxo-thiazolidine derivatives, maintained the molecular requirements for enzyme inhibition. A literature search revealed that 4-oxo-thiazolidine derivatives may exhibit anti-HIV (Rawal et al., 2005) enzyme murB (Andres et al., 2000), antimicrobial activity , antituberclousis (Babaoglu et al., 2003;Govindarajan et al., 2003) antiproliferative agent (Ottana`et al., 2005), CNS activity (Basu et al., 2008), cytotoxic agent (Gududuru et al., 2005), anticonvulsant activity (Archana et al., 2002), antibacterial activity (Bonde and Gaikwad, 2004;Sayyed et al., 2006), analgesic agent (Moustfa et al., 1989), antiinflammetry agent (Vigorita et al., 2001;Goel et al., 1999), antihypertensive agent (El-subbagh, 1999), and hypolipidemic agent (Lohary et al., 1999) properties. ...
October 2010
ChemInform
... Ademais, observa-se ainda na Figura 1 aril-derivados semisintéticos destacados em estudos de atividade anticâncer tanto a partir do próprio andrografolídeo como o derivado (4) (NANDURI et al., 2004), quanto de outros diterpenos labdanos como o derivado do sclareol (5) (BHAT et al., 2015) e o derivado do ácido labdenoico (6) (SOUZA-FERRARI et al., 2021), um labdano extraído em grande quantidade de uma espécie da flora brasileira, Moldenhawera nutans (DA-VID et al., 2007). Esses compostos têm se apresentado como moléculas protótipos (leads) para estudos e desenvolvimento de potenciais agentes direcionados ao tratamento de cânceres de pulmão, de próstata (para o caso do derivado 5) e de leucemia (para o caso do derivado 6). ...
October 2004
ChemInform
... With the aim to develop a more efficient synthetic process for the synthesis of highly functionalized 5-arylidene rhodanines 3a-v from the building blocks 1a-i and 2a-p, microwave irradiation was employed to shorten the reaction times in comparison to conventional heating. For the reported methods, the Knoevenagel condensations have been realized in the presence of catalyst with various solvents: sodium acetate in glacial acetic acid [48] or in ethanol [46], piperidinium benzoate in toluene [49], tetrabutylammonium bromide in water [50], and piperidine in ethanol [51], using conventional heating in an oil bath. These older protocols suffer from one or more limitations, such as requiring harsh reaction conditions, low moderate yields, cumbersome experimental process, and long reaction time. ...
December 1997
Bioorganic & Medicinal Chemistry Letters
... Type 2 DM is a heterogeneous, progressive disorder initially characterized by impaired glucose tolerance and compensatory hyperinsulinemia, which in the later stages, develops severe insulin resistance and impaired beta cell function [2,3]. This is associated with hyperglycemia, dyslipidemia, hypertension, obesity and in the long term, micro-and macro-vascular complications leading to increased mortality [4]. Hypertension (blood pressure [BP] ≥140/90 mmHg) is an extremely common condition in diabetes, affecting around 20 to 60% of diabetic patients [5]. ...
July 2001
... Taxonomical position:-1 Stem. Chloroform Anti-ulcer [32] 2. PHARMACOLOGICAL POTENTIAL OF ADINA CORDIFOLIA ...
February 1999
Fitoterapia
... The substituents at carbon-2 and carbon-3 of indole significantly reduce the euglycemic and hypolipidemic actions. [16,17] Darwish KM developed, produced, and tested a unique class of thiazolidinediones (TZDs) from benzhydrol and indole for their binding affinity to two receptors: PPAR-E and FFAR1, also known as GPCR40. There are three compounds that have a high affinity for both targets. ...
May 1998
Journal of Medicinal Chemistry
... As a result of its numerous uses, thiazolidine-2,4-dione (TZD) is known as one of the most prospective classes of thiazoles. TZD has a wide range of biological properties, including cancerfighting abilities, [3] antitubercular, [4] antioxidant, [5] antibacterial, [6] antiviral, [7] anti-inflammatory, [8] anti-plasmodial, [9] antidiabetic impacts, [10] antihyperglycemic, [11] Peptide deformylase inhibitors, [12] and GPR-40 agonists. [13] Figure 1 depicts some thiazolidinedione-based antibiotics. ...
June 1998
Bioorganic & Medicinal Chemistry Letters
... TZD derivatives control lipid metabolism and balance glucose by activating PPARs, a group of nuclear receptors with the highest selectivity for PPAR [14]. Due to their adaptability and versatility, thiazolidinediones exhibit a broad range of pharmacological effects, including hypolipidemic activity [15], antihyperglycemic [16], anticancer [17], antimicrobial [18], neuroprotective [19], antiviral effects [20], anti-inflammatory [21], and anti-plasmodial activity [22]. TZDs also interfere with the activity of multiple inhibitors, such as aldose reductase inhibitors [23], alphaglucosidase inhibitors [24], LPS-induced nitric oxide (NO) production inhibitors [25], COX inhibitors, PI3Kγ inhibitors, PPARγ agonists/modulators tyrosinase inhibitor [26], and PTP1B inhibitors [27]. ...
November 1998
Bioorganic & Medicinal Chemistry Letters
... The substituents at carbon-2 and carbon-3 of indole significantly reduce the euglycemic and hypolipidemic actions. [16,17] Darwish KM developed, produced, and tested a unique class of thiazolidinediones (TZDs) from benzhydrol and indole for their binding affinity to two receptors: PPAR-E and FFAR1, also known as GPCR40. There are three compounds that have a high affinity for both targets. ...
July 1999
Journal of Medicinal Chemistry
