Читать книгу Successful Drug Discovery, Volume 5 - Группа авторов - Страница 19

Antibiotics figure prominently among the drugs discovered by academicians. Penicillin G represents one of the most influential findings in natural product research, saving the lives of millions of people. On 28 September 1928, Alexander Fleming, University of London, noted that on one of his bacterial culture dishes that was contaminated with a mold and that bacteria would die in proximity to the mold. He concluded that the mold produced an antibiotic substance. He published the results in 1929, [27] but the article and some following work did not receive much attention. The compound was difficult to isolate and it took until 1942 to reach the market [28]. Still today, penicillin G is on the WHO list of essential medicines, and in 1945, Fleming, together with Howard Florey and Ernst Boris Chain, received the Nobel Prize for medicine. Fleming also gave a beautiful description of his scientific finding, reminding us that chance is an essential part of scientific work – something scientists certainly cannot rely on, but should be prepared to spot and realize its potential.

One sometimes finds what one is not looking for. When I woke up just after dawn on September 28, 1928, I certainly didn't plan to revolutionize all medicine by discovering the world's first antibiotic, or bacteria killer. But I suppose that was exactly what I did [29].

Streptomycin is another compound listed on the WHO list of essential medicines. It was isolated for the first time by Albert Schatz, a PhD student in the laboratory of Selman A. Waksman at Rutgers University in 1943. The results were published on 1 January 1944 [30], and the compound was quickly progressed to the clinics. Waksman, who also discovered several other important antibiotic natural products, among them actinomycin and neomycin, received the unshared Nobel Prize for medicine in 1952 “for his discovery of streptomycin, the first antibiotic effective against tuberculosis.” However, it is highly debated, if the role of other contributors, in particular of Schatz, was downplayed [31].

Gramicidin S was discovered by Georgyi Frantsevitch Gause, a Russian microbiologist and his wife in 1942 [32]. By 1943 it was being used to treat wounded Soviet soldiers in World War II. Gramicidin S is produced by Brevibacillus brevis and consists of two identical fivemers, which are coupled to give a cyclic decapeptide.

Figure 1.5 Lead structures isolated from natural sources.