Synthesis, Molecular Docking Study, and Biological Evaluation of New 4-(2,5-Dimethyl-1-pyrrol-1-yl)-'-(2-(substituted)acetyl)benzohydrazides as Dual Enoyl ACP Reductase and DHFR Enzyme Inhibitors.

In this study, a new series of 4-(2,5-dimethyl-1-pyrrol-1-yl)--(2-(substituted)acetyl) benzohydrazides () were prepared and new heterocycles underwent thorough characterization and evaluation for antibacterial activity; some of them underwent further testing for in vitro inhibition of enoyl ACP reductase and DHFR enzymes. The majority of the synthesized molecules exhibited appreciable action against DHFR and enoyl ACP reductase enzymes. Some of the synthesized compounds also showed strong antibacterial and antitubercular properties.

Ellagic acid restored lead-induced nephrotoxicity by anti-inflammatory, anti-apoptotic and free radical scavenging activities.

Introduction: long-term environmental and occupational exposure to lead, which is a ubiquitous industrial pollutant, causes significant damage to tissues of kidney. This report aims to address this debilitating issue. A natural polyphenolic compound, Ellagic acid (EA) is having numerous potential medicinal properties.

The role of ferric coagulant on gypsum scaling and ion interception efficiency in nanofiltration at different pH values: Performance and mechanism.

Nanofiltration (NF) is extensively applied after coagulation, which is conducive to alleviate organic fouling on NF membranes and improve water purification performance. However, inorganic fouling, which remains the major obstacle to limit the wider application of NF, could be enhanced by even low dosage coagulant. Few researchers realize the existence of coagulant-enhanced scaling, much less control it.

Pyrrolyl Pyrazoline Carbaldehydes as Enoyl-ACP Reductase Inhibitors: Design, Synthesis and Antitubercular Activity.

Introduction: In efforts to develop new antitubercular (anti-TB) compounds, herein we describe cytotoxic evaluation of 15 newly synthesized pyrrolyl pyrazoline carbaldehydes.

Method & Materials: Surflex-Docking method was used to study binding modes of the compounds at the active site of the enzyme enoyl ACP reductase from , which plays an important role in FAS-II biosynthetic pathway of and also it is an important target for designing novel anti-TB agents.

Results: Among the synthesized compounds, compounds and showed H-bonding interactions with MET98, TYR158 and co-factor NAD, all of which fitted well within the binding pocket of InhA.

Design, synthesis and pharmacological analysis of 5-[4'-(substituted-methyl)[1,1'-biphenyl]-2-yl]-1H-tetrazoles.

In the present paper 5-[4'-({4-[(4-aryloxy)methyl]-1H-1,2,3-triazol-1-yl}methyl)[1,1'-biphenyl]-2-yl]-1H-tetrazoles (5a-g) and [2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl-substituted-1-carbodithioates (11h-q) have been designed and synthesized. These compounds were subjected to docking (against AT receptor protein enzyme in complex with Lisinopril), in vitro angiotensin converting enzyme inhibition, anti-proliferative, anti-inflammatory screening (through egg albumin denaturation inhibition and red blood cell membrane stabilization assay) and finally anti-fungal activity analyses. Some of the compounds have shown significant pharmacological properties.

Evaluation of wound healing property of Caesalpinia mimosoides Lam.

Ethnopharmacological Relevance: Caesalpinia mimosoides Lam. is one of the important traditional folk medicinal plants in the treatment of skin diseases and wounds used by healers of Uttara Kannada district of Karnataka state (India). However scientific validation of documented traditional knowledge related to medicinal plants is an important path in current scenario to fulfill the increasing demand of herbal medicine.

In vitro cytotoxicity and in vivo efficacy of 5-fluorouracil-loaded enteric-coated PEG-cross-linked chitosan microspheres in colorectal cancer therapy in rats.

Purpose: Microspheres of chitosan (CS) cross-linked with polyethylene glycol (PEG) were prepared by emulsion-cross-linking followed by the solvent evaporation technique. The formulations were characterized and subjected to in vitro and in vivo tests to assess cell growth, changes in cell morphology, and activities by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on human HT-29 colon cancer cell-lines.

Methods: In vivo activity was evaluated for dimethyl hydrazine-induced colorectal cancer in albino male Wistar rats.

In vitro cytotoxicity and in vivo efficacy of 5-fluorouracil-loaded enteric-coated PEG-crosslinked chitosan microspheres in colorectal cancer therapy in rats.

Purpose: Microspheres of chitosan (CS) crosslinked with polyethylene glycol (PEG) were prepared by emulsion crosslinking followed by solvent evaporation technique. The formulations were characterized and subjected to in vitro and in vivo tests to assess cell growth, changes in cell morphology and activities by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on human HT-29 colon cancer cell lines.

Methods: In vivo activity was evaluated for dimethyl hydrazine-induced colorectal cancer in albino male Wistar rats.

Polymeric hydrogels for oral insulin delivery.

The search for an effective and reliable oral insulin delivery system has been a major challenge facing pharmaceutical scientists for over many decades. Even though innumerable carrier systems that protect insulin from degradation in the GIT with improved membrane permeability and biological activity have been developed, yet a clinically acceptable device is not available for human application. Efforts in this direction are continuing at an accelerated speed.

Cytotoxicity and antitumour activity of 5-fluorouracil-loaded polyhydroxybutyrate and cellulose acetate phthalate blend microspheres.

Pharmacokinetics, biodistribution and antitumour activity of 5-fluorouracil (5-FU)-loaded polyhydroxybutyrate (PHB) and cellulose acetate phthalate (CAP) blend microspheres were investigated in chemically induced colorectal cancer in albino male Wistar rats and compared with pristine 5-FU given as a suspension. The microspheres were characterised for particle size, encapsulation efficiency, in vitro release and in vitro cytotoxicity on human HT-29 colon cancer cell line. Spherical particles with a mean size of 44 ± 11 µm were obtained that showed sustained release of 5-FU.