Cannabidiol (CBD) exhibits anticonvulsant activity in experimental animals and in man. As part of a structureactivity study, analogs were prepared wherein the terpene unit, the aryl unit, and/or the side chain were modified. Thus, several pinenyl and carenyl derivatives, aryl ethers and acetates, and a variety of 1",1"-dialkylhexyl and 1",1"dialkylheptyl analogs were synthesized. The compounds ...

tected with a drying tube. A solution of phosgene (55 ml, 12.5% in benzene) was then added with vigorous stirring. The reaction was cooled for an additional 10 min and was then kept at room temperature for 1 hr. The reaction mixture was cooled again, treated with 100-ml portions of 1 N HCl until free of amine, and then rinsed successively with 8% NaHCOs and water, dried, and evaporated, giving ...

Carbohydrate-based surfactants (CBS) are, today, among the most important classes of amphiphilic compounds (Dembintsky, 2004; Queneau et al, 2008; Ruiz, 2009). Their structure is the result of the saccharide and lipid combination, naturally biosynthesized within living cells, or synthetically prepared by sequential reactions using carbohydrate and fatty materials, through one or several bonds. ...

The intact diphtheria toxin molecule, a single polypeptide chain of about 62,000 daltons, has no enzymic activity. However, the transfer in uifro of ADP-ribose from NAD to aminoacyltrensferase II can be catalyzed by any of several fragments of toxin. The smallest active fragment (A, 24,000 daltons) is normally connected to the remainder of the molecule (B, 38,000 daltons) by a peptide bond and ...

Predicting the log of the partition coefficient P is a long-standing benchmark problem in Quantitative Structure-Activity Relationships (QSAR). In this paper we show that a relatively simple molecular representation (using 14 variables) can be combined with leading edge machine learning algorithms to predict logP on new compounds more accurately than existing benchmark algorithms which use comp...

The relationship between the activity and the chemical structure of cadeguomycin (CDM, 7-carboxy-7-deazaguanosine) was studied with six analogs of CDM. Both activities of CDM, enhancing the incorporation of [3H]thymidine in K562 cells and potentiating the cytotoxicity of cytosine arabinoside for K562 cells, were significantly augmented by the replacement of the 7-carboxyl group with cyano (CDM-...

Prostate cancer, acne, seborrhea, hirsutism, and androgenic alopecia are well recognized to depend upon an excess or increased sensitivity to androgens or to be at least sensitive to androgens. It thus seems logical to use antiandrogens as therapeutic agents to prevent androgens from binding to the androgen receptor. The two predominant naturally occurring androgens are testosterone (T) and dih...

The second-order rate constants for the microbial transformation of a series of phenols were correlated with the physicochemical properties of the phenols. The compounds studied were phenol, p-methylphenol, p-chlorophenol, p-bromophenol, p-cyanophenol, p-nitrophenol, p-acetylphenol, and p-methoxyphenol. Phenol-grown cells of Pseudomonas putida U transformed these compounds. Microbial transforma...

The activities of eight cytokinins in promoting callus growth were tested In two Phaseolus genotypes, P. vulgaris L. var. Great Northern, and P. lunatus L. var. Kingston. The structural feature which contributes to the major genotypic difference in cytokinin structure-activity relationships is the presence or absence of a double bond at the 2,3position of the isoprenoid Nf side chain. In Kingst...

activity and a wide spectrum against both Gram-positive and Gram-negative bacteria1~4). This high activity is due to good diffusion through the outer membranein Gram-negative organisms5), high affinities for penicillinbinding proteins (PBPs)6'7) and high stability and inhibitory activity against /Mactamases8). However, carbapenems were hydrolyzed by dehydropeptidase-I (DHP-I) from several anima...