1. Iodine-Catalyzed Diazenylation with Arylhydrazine Hydrochlorides in Air
Shashikant U Dighe, Dinesh S Barak, Sanjay Batra, Ilesha Avasthi J Org Chem . 2018 Apr 6;83(7):3537-3546. doi: 10.1021/acs.joc.7b03149.
A mild approach to diazenylation of active methylene compounds and N-heterocyclic compounds with arylhydrazine hydrochlorides in the presence of iodine under basic aerobic conditions was developed. The reaction could be executed either under heating or in the presence of blue LED light, though the latter condition was found to be relatively efficient. Presumably, the aryldiazene produced by oxidation of arylhydrazine hydrochloride acts as a nitrogen scavenger of the radical intermediate generated from the active methylene compound in the presence of iodine to produce the diazo compounds. The scope and limitations of the protocol are presented.
2. Antiparasitic activities of new lawsone Mannich bases
Rainer Schobert, Bernhard Biersack, Isabel Winter, Klaus Ersfeld, Adil A H Mujawah, Waleed S Koko, Ibrahim Al Nasr, Tariq A Khan, Jana Jentzsch Arch Pharm (Weinheim) . 2019 Nov;352(11):e1900128. doi: 10.1002/ardp.201900128.
A series of new lawsone Mannich bases derived from salicylaldehydes or nitrofurfural were prepared and tested for their activities against Leishmania major, Toxoplasma gondii, and Trypanosoma brucei brucei parasites. The hydrochloride salts 5a and 6a of the Mannich bases 2a and 3a, derived from unsubstituted salicylaldehyde and long-chained alkyl amines, were selectively and strongly active against T. gondii cells and appear to be new promising drug candidates against this parasite. Compound 6a showed an even higher activity against T. gondii than the known lawsone Mannich base 1b. Compound 4a, derived from salicylaldehyde and 2-methylaminopyridine, was also distinctly active against T. gondii cells. The derivatives 3a (salicyl derivative), 3b (3,5-dichloro-2-hydroxyphenyl derivative), and 3d (5-nitrofuranyl derivative) as well as the hydrochlorides 6a and 6b were also efficacious against T. b. brucei cells with compounds 3a and 3b being more selective for T. b. brucei over Vero cells when compared with the known control compound 1b. The derivatives 5a, 5c, 6a, and 6c proved to be up to five times more active than 1b against L. major promastigotes and up to four times more efficacious against L. major amastigotes.
3. Carteolol
No data are available for the use of carteolol during breastfeeding. Because its excretion into breastmilk is probably extensive, other beta-adrenergic blocking drugs are preferred to oral carteolol while breastfeeding a neonate. Infants over 2 months of age have more mature kidney function and are less likely to be affected.Ophthalmic use of carteolol by the mother should pose little risk to the breastfed infant, although some guidelines state that gel formulations are preferred over solutions.[1,2] substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue.
